Resibufogenin | 蟾力苏 | Bufogenin | AmBeed-信号通路专用抑制剂

Resibufogenin/酯蟾毒配基 {[allProObj[0].p_purity_real_show]}

货号：A151203 同义名： 蟾力苏 / Bufogenin; Recibufogenin

Resibufogenin 抑制NF-κB和AP-1信号通路，减少IκBα磷酸化/降解，阻断p65核转位，下调JNK/ERK磷酸化，降低TNF-α、IL-6等炎症因子转录。Resibufogenin还通过PI3K/AKT/GSK3β通路诱导癌细胞凋亡。

Resibufogenin/酯蟾毒配基化学结构
CAS号：465-39-4

Resibufogenin/酯蟾毒配基 3D分子结构
CAS号：465-39-4

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GSK-3 亚型比较

Bcl-2 亚型比较

半胱天冬酶亚型比较

Akt 亚型比较

PI3K 亚型比较

NF-κB 亚型比较

CDK 亚型比较

产品名称	GSK-3 ↓ ↑	GSK-3α ↓ ↑	GSK-3β ↓ ↑	纯度
AZD2858	+ GSK-3, IC50: 68 nM			99%
Bikinin	✔			99%+
GSK 3 Inhibitor IX	++++ GSK-3, IC50: 5 nM			99%+
AZD1080		+++ GSK-3α, IC50: 6.9 nM	++ GSK-3β, IC50: 31 nM	99%+
BIO-acetoxime		+++ GSK-3α, IC50: 10 nM	+++ GSK-3β, IC50: 10 nM	95%
SB-216763		++ GSK-3α, IC50: 34.3 nM	++ GSK-3β, IC50: ~34.3 nM	98%
SB 415286		+ GSK-3α, IC50: 78 nM	+ GSK-3β, IC50: ~78 nM	99%+
CHIR-98014		++++ GSK-3α, IC50: 0.65 nM	++++ GSK-3β, IC50: 0.58 nM	98%
LY2090314		++++ GSK-3α, IC50: 1.5 nM	++++ GSK-3β, IC50: 0.9 nM	99%+
CHIR 99021		+++ GSK-3α, IC50: 10 nM	++++ GSK-3β, IC50: 6.7 nM	99%+
TDZD-8			+ GSK-3β, IC50: 2 μM	99%+
Indirubin			+ GSK-3β, IC50: 0.6 μM	98%
IM-12			++ GSK-3β, IC50: 53 nM	98%
TWS119			++ GSK-3β, IC50: 30 nM	99%
1-Azakenpaullone			+++ GSK-3β, IC50: 18 nM	99%+
AR-A014418			++ GSK-3β, Ki: 38 nM	99%+
Tideglusib			+ GSK-3β, IC50: 60 nM	98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

产品名称	Bax ↓ ↑	Bcl-2 ↓ ↑	Bcl-B ↓ ↑	Bcl-w ↓ ↑	Bcl-xL ↓ ↑	Bfl-1 ↓ ↑	Mcl-1 ↓ ↑	其他靶点	纯度
BTSA1	✔								99%+
HA14-1		+ Bcl-2, IC50: 9 μM							98%
Venetoclax		++++ Bcl-2, Ki: <0.01 nM							99%
Navitoclax									99%+
Obatoclax Mesylate		+++ Bcl-2, Ki: 0.22 μM							99%
ABT-737		+++ Bcl-2, EC50: 30.3 nM	+ Bcl-B, EC50: 1.82 μM	+++ Bcl-w, EC50: 197.8 nM	+++ Bcl-xL, EC50: 78.7 nM				99%+
Gambogic Acid		+ Bcl-2, IC50: 1.21 μM Bfl-1, IC50: 1.06 μM	++ Bcl-B, IC50: 0.66 μM	++++ Bcl-w, IC50: 0.02 μM	+ Bcl-xL, IC50: 1.47 μM	+ Bfl-1, IC50: 1.06 μM	++ Mcl-1, IC50: 0.79 μM	Caspase	99% HPLC
BH3I-1					+ BH3-Bcl-xL interaction, Ki: 2.4 μM				99%
A-1331852					++++ Bcl-xL, Ki: <0.01 nM				99%+
A-1210477							++++ MCL-1, IC50: 26.2 nM		99%+
Maritoclax							✔		97%
TW-37		+++ Bcl-2, Ki: 0.29 μM			+ Bcl-xL, Ki: 1.11 μM		+++ Mcl-1, Ki: 0.26 μM		98%
UMI-77							++ Mcl-1, Ki: 490 nM		97%
(R)-(-)-Gossypol acetic acid		++ Bcl-2, Ki: 0.32 μM			++ Bcl-xL, Ki: 0.48 μM		+++ Mcl-1, Ki: 0.18 μM		99%
Sabutoclax		++ Bcl-2, IC50: 0.32 μM Bfl-1, IC50: 0.62 μM			++ Bcl-xL, IC50: 0.31 μM	++ Bfl-1, IC50: 0.62 μM	+++ Mcl-1, IC50: 0.20 μM		98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

产品名称	Capase-7 ↓ ↑	Caspase ↓ ↑	Caspase-1 ↓ ↑	Caspase-10 ↓ ↑	Caspase-2 ↓ ↑	Caspase-3 ↓ ↑	Caspase-4 ↓ ↑	Caspase-5 ↓ ↑	Caspase-6 ↓ ↑	Caspase-8 ↓ ↑	Caspase-9 ↓ ↑	纯度
Emricasan		✔										99%+
Z-VAD(OMe)-FMK		✔										99%+
Z-VAD-FMK		✔										99%+
Q-VD-OPh												97%
VX-765			++++ Caspase-1, Ki: 0.8 nM				++++ Caspase-4, Ki: <0.6 nM					99%+
Ac-DEVD-CHO	+++ caspase-7, Ki: 1.6 nM		+++ Caspase-1, Ki: 18 nM	+++ caspase-10, Ki: 12 nM	+ caspase-2, Ki: 1.71 μM	++++ Caspase-3, Ki: 230 pM	++ Caspase-4, Ki: 132 nM	++ caspase-5, Ki: 205 nM	+++ caspase-6, Ki: 31 nM	++++ caspase-8, Ki: 0.92 nM	++ Caspase-9, Ki: 60 nM	98%+
Z-DEVD-FMK						✔						98%
Z-IETD-FMK										✔		98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

产品名称	Akt ↓ ↑	Akt1 ↓ ↑	Akt2 ↓ ↑	Akt3 ↓ ↑	其他靶点	纯度
Honokiol	✔				MEK	98%
PF-04691502	++++ P-Akt (T308), IC50: 7.5 nM P-Akt (S473), IC50: 3.8 nM					98+%
PHT-427	+ Akt, Ki: 2.7 μM					99%+
Deguelin	✔				PI3K	99%+
TIC10 isomer	✔				ERK	98+%
Perifosine	+ Akt, IC50: 4.7 μM					98%
Miltefosine	✔				PI3K,PKC	98%
Triciribine	+ Akt, IC50: 130 nM					99%+
Uprosertib		+ Akt1, IC50: 180 nM	+ Akt2, IC50: 328 nM	++ Akt3, IC50: 38 nM		99%+
Afuresertib		++++ Akt1, Ki: 0.08 nM	++++ Akt2, Ki: 2 nM	++++ Akt3, Ki: 2.6 nM		99%+
Miransertib		++++ Akt1, IC50: 5 nM	++++ Akt2, IC50: 4.5 nM	++ Akt3, IC50: 16 nM		98+%
GSK-690693		++++ Akt1, IC50: 2 nM	+++ Akt2, IC50: 13 nM	+++ Akt3, IC50: 9 nM		99%+
AT7867		++ Akt1, IC50: 32 nM	++ Akt2, IC50: 17 nM	++ Akt3, IC50: 47 nM	PKA	99%+
AKT inhibitor VIII		++ Akt1, IC50: 58 nM	+ Akt2, IC50: 210 nM	+ Akt3, IC50: 2119 nM		97%
MK-2206 2HCl		+++ Akt1, IC50: 8 nM	+++ Akt2, IC50: 12 nM	+ Akt3, IC50: 65 nM		99%+
Ipatasertib		++++ Akt1, IC50: 5 nM	++ Akt2, IC50: 18 nM	+++ Akt3, IC50: 8 nM		99%+
AT13148		++ Akt1, IC50: 38 nM	+ Akt2, IC50: 402 nM	++ Akt3, IC50: 50 nM	PKA	95%
Capivasertib		++++ Akt1, IC50: 3 nM	+++ Akt2, IC50: 8 nM	+++ Akt3, IC50: 8 nM		99%+
A-674563 HCl		+++ Akt1, Ki: 11 nM			PKA	99%
CCT128930			+++ Akt2, IC50: 6 nM		PKA	95%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

产品名称	C2β ↓ ↑	p110α ↓ ↑	p110β ↓ ↑	p110γ ↓ ↑	p110δ ↓ ↑	PI3K ↓ ↑	Vps34 ↓ ↑	其他靶点	纯度
A66	+ C2β, IC50: 462 nM	++ p110α, IC50: 32 nM							99%+
Taselisib	+ C2β, IC50: 292 nM	++++ PI3Kα, Ki: 0.29 nM	+++ PI3Kβ, Ki: 9.1 nM	++++ PI3Kγ, Ki: 0.97 nM	++++ PI3Kδ, Ki: 0.12 nM		+ hVps34, IC50: 374 nM		99%+
Gedatolisib		++++ PI3Kα, IC50: 0.4 nM		+++ PI3Kγ, IC50: 5.4 nM				mTOR	99%
HS-173		++++ PI3Kα , IC50: 0.8 nM							99%+
Serabelisib		+++ PI3Kα, IC50: 21 nM							99%+
GNE-477		++++ PI3Kα, IC50: 4 nM						mTOR	99%
YM-201636		+ p110α, IC50: 3.3 μM						PIKfyve	98%
AS-252424		+ PI3Kα, IC50: 935 nM		++ PI3Kγ, IC50: 33 nM					99%
Alpelisib		+++ PI3Kα, IC50: 5 nM							99%+
AS-604850		+ PI3Kα, IC50: 4.5 μM		+ PI3Kγ, IC50: 0.25 μM					99%
SF2523		++ PI3Kα, IC50: 34 nM		++ PI3Kγ, IC50: 158 nM				DNA-PK,mTOR	99%+
Inavolisib		++++ PI3K alpha, IC50: 0.038 nM							99%+
Bimiralisib		++++ PI3Kα, Kd: 1.5 nM	+++ PI3Kβ, Kd: 11 nM	++ PI3Kγ, Kd: 25 nM	++ PI3Kδ, Kd: 25 nM			mTOR	99%+
GSK1059615		++++ PI3Kα, IC50: 0.4 nM	++++ PI3Kβ, IC50: 0.6 nM	+++ PI3Kγ, IC50: 5 nM	++++ PI3Kδ, IC50: 2 nM			mTOR	98%
GSK2636771			✔						99%
Fimepinostat		+++ PI3Kα, IC50: 19 nM	++ PI3Kβ, IC50: 54 nM		++ PI3Kδ, IC50: 39 nM				99%+
VS-5584		++++ PI3Kα, IC50: 2.6 nM	+++ PI3Kβ, IC50: 21 nM	++++ PI3Kγ, IC50: 3.0 nM	++++ PI3Kδ, IC50: 2.7 nM			mTOR	98%
Dactolisib		++++ p110α1, IC50: 4 nM	++ p110β, IC50: 75 nM	+++ p110γ, IC50: 5 nM	+++ p110δ, IC50: 7 nM				98+%
PI-103		++++ p110α, IC50: 2 nM	++++ p110β, IC50: 3 nM	+++ p110γ, IC50: 15 nM	++++ p110δ, IC50: 3 nM			DNA-PK,mTOR	99%+
PI-3065			+ p110β, IC50: 1078 nM		+++ p110δ, IC50: 15 nM				99%+
Voxtalisib		++ PI3Kα, IC50: 39 nM	++ PI3Kβ, IC50: 113 nM	+++ PI3Kγ, IC50: 9 nM	++ PI3Kδ, IC50: 43 nM			DNA-PK,mTOR	99%+
AZD-8835		+++ PI3Kα, IC50: 6.2 nM	+ PI3Kβ, IC50: 431 nM	++ PI3Kγ, IC50: 90 nM	+++ PI3Kδ, IC50: 5.7 nM				99%
Pilaralisib analogue		++ PI3Kα, IC50: 39 nM	++ PI3Kβ, IC50: 36 nM	+++ PI3Kγ, IC50: 23 nM	++ PI3Kδ, IC50: 36 nM				99%+
ZSTK474		+++ PI3Kα, IC50: 16 nM	++ PI3Kβ, IC50: 44 nM	++ PI3Kγ, IC50: 49 nM	+++ PI3Kδ, IC50: 4.6 nM	++ PI3K, IC50: 37 nM			98%
AS-605240		++ PI3Kα, IC50: 60 nM	+ PI3Kβ, IC50: 270 nM	+++ PI3Kγ, IC50: 8 nM	+ PI3Kδ, IC50: 300 nM				98%
TGX-221			+++ p110β, IC50: 5 nM		++ p110δ, IC50: 0.1 μM				99%+
PF-04691502		++++ PI3Kα, Ki: 1.8 nM	++++ PI3Kβ, Ki: 2.1 nM	++++ PI3Kγ, Ki: 1.9 nM	++++ PI3Kδ, Ki: 1.6 nM			mTOR	98+%
GDC-0084		++++ PI3Kα, Ki app: 2 nM	++ PI3Kβ, Ki app: 46 nM	+++ PI3Kγ, Ki app: 10 nM	++++ PI3Kδ, Ki app: 3 nM			mTOR	99%+
Buparlisib		++ p110α, IC50: 52 nM	+ p110β, IC50: 166 nM	+ p110γ, IC50: 262 nM	++ p110δ, IC50: 116 nM		+ Vps34, IC50: 2.4 μM	mTOR	98%
LY294002		+ p110α, IC50: 0.5 μM	+ p110β, IC50: 0.97 μM		+ p110δ, IC50: 0.57 μM			DNA-PK	99%+
AZD 6482		+ PI3Kα, IC50: 870 nM	+++ PI3Kβ, IC50: 10 nM		++ PI3Kδ, IC50: 80 nM			DNA-PK	99%+
Pictilisib		++++ p110α, IC50: 3 nM	++ p110β, IC50: 33 nM	++ p110γ, IC50: 75 nM	++++ p110δ, IC50: 3 nM			mTOR	99%+
PKI-402		++++ PI3Kα, IC50: 2 nM	+++ PI3Kβ, IC50: 7 nM	+++ PI3Kγ, IC50: 16 nM	+++ PI3Kδ, IC50: 14 nM			mTOR	98%
Copanlisib		++++ PI3Kα, IC50: 0.5 nM	++++ PI3Kβ, IC50: 3.7 nM	+++ PI3Kγ, IC50: 6.4 nM	++++ PI3Kδ, IC50: 0.7 nM				99%+
Omipalisib		++++ p110α, Ki: 0.019 nM	++++ p110β, Ki: 0.13 nM	++++ p110γ, Ki: 0.06 nM	++++ p110δ, Ki: 0.024 nM				99%+
Izorlisib		+++ PI3Kα, IC50: 14 nM	++ PI3Kβ, IC50: 0.12 μM	++ PI3Kγ, IC50: 36 nM	+ PI3Kδ, IC50: 0.50 μM				99%+
AZD8186		++ PI3Kα, IC50: 35 nM	++++ PI3Kβ, IC50: 4 nM		+++ PI3Kδ, IC50: 12 nM				99%
KU-0060648		++++ PI3Kα, IC50: 4 nM	++++ PI3Kβ, IC50: 0.5 nM	+ PI3Kγ, IC50: 0.59 μM	++++ PI3Kδ, IC50: 0.1 nM			DNA-PK	98%
Apitolisib		+++ p110α, IC50: 5 nM	++ p110β, IC50: 27 nM	+++ p110γ, IC50: 14 nM	+++ p110δ, IC50: 7 nM			mTOR	98%+
CZC24832			+ PI3Kβ, IC50: 1.1 μM	++ PI3Kγ, IC50: 27 nM					98+%
BGT226 maleate		++++ PI3Kα, IC50: 4 nM	++ PI3Kβ, IC50: 63 nM	++ PI3Kγ, IC50: 38 nM				mTOR	99%+
TG 100713		++ PI3Kα, IC50: 165 nM	+ PI3Kβ, IC50: 215 nM	++ PI3Kγ, IC50: 50 nM	+++ PI3Kδ, IC50: 24 nM				98%+
PI3K-IN-1		++ PI3Kα, IC50: 39 nM	++ PI3Kβ, IC50: 113 nM	+++ PI3Kγ, IC50: 9 nM	++ PI3Kδ, IC50: 43 nM			DNA-PK,mTOR	98+%
TG100-115		+ PI3Kα, IC50: 1.3 μM	+ PI3Kβ, IC50: 1.2 μM	++ PI3Kγ, IC50: 83 nM	+ PI3Kδ, IC50: 235 nM				98%
PIK-90		+++ PI3Kα, IC50: 11 nM	+ PI3Kβ, IC50: 350 nM	+++ PI3Kγ, IC50: 18 nM	++ PI3Kδ, IC50: 58 nM				99%+
PIK-294			+ p110β, IC50: 490 nM	++ p110γ, IC50: 160 nM	+++ p110δ, IC50: 10 nM				99%+
Duvelisib			++++ PI3Kβ, Ki: 1564 pM	++ PI3Kγ, Ki: 243 pM	++++ PI3Kδ, Ki: 23 pM				99%+
GDC-0326		++++ PI3Kα, Ki: 0.2 nM	++ PI3Kβ, Ki: 26.6 nM	+++ PI3Kγ, Ki: 10.2 nM	++++ PI3Kδ, Ki: 4 nM				98%
Quercetin Dihydrate			+ PI3Kβ, IC50: 5.4 μM	+ PI3Kγ, IC50: 2.4 μM	+ PI3Kδ, IC50: 3.0 μM				95%
Quercetin			+ PI3Kβ, IC50: 5.4 μM	+ PI3Kγ, IC50: 2.4 μM	+ PI3Kδ, IC50: 3.0 μM			Src,Sirtuin,PKC	95%
Leniolisib		+ PI3Kα, IC50: 0.244 μM	+ PI3Kβ, IC50: 0.424 μM	+ PI3Kγ, IC50: 2.23 μM	+++ PI3Kδ, IC50: 0.011 μM			DNA-PK	99%+
PIK-108			✔						99%
Eganelisib				+++ PI3Kγ, IC50: 16 nM					99%+
CAY10505				✔					99%
IPI-3063					++++ p110δ, IC50: 2.5 nM				99%
Nemiralisib					++++ PI3Kδ, pKi: 9.9				99%+
PF-4989216		++++ p110α, IC50: 2 nM		++ p110γ, IC50: 65 nM	++++ p110δ, IC50: 1 nM				99%+
PIK-75 HCl		+++ p110α, IC50: 5.8 nM		++ p110γ, IC50: 76 nM	+ p110δ, IC50: 0.51 μM			DNA-PK	99%+
Tenalisib				++ PI3Kγ, IC50: 33.2 nM	++ PI3Kδ, IC50: 24.5 nM				98%
Acalisib					+++ p110δ, IC50: 14 nM				99%+
Umbralisib					+++ PI3Kδ, IC50: 22.2 nM				99%+
AMG319				+ PI3Kγ, IC50: 850 nM	+++ PI3Kδ, IC50: 18 nM				99%
IC-87114				+ PI3Kγ, IC50: 29 μM	+ PI3Kδ, IC50: 0.5 μM				99%+
Idelalisib				++ p110γ, IC50: 89 nM	++++ p110δ, IC50: 2.5 nM				98%
PIK-293				+ p110γ, IC50: 10 μM	+ p110δ, IC50: 0.24 μM				99%+
Vps34-PIK-III					+ PI3Kδ, IC50: 1.2μM		+++ Vps34, IC50: 0.018μM		99%+
GSK2292767					✔				98%
Seletalisib				+ PI3Kγ, IC50: 282 nM	+++ PI3Kδ, IC50: 12 nM				99%+
P110δ-IN-1					++++ P110δ, IC50: 0.6 nM				99%
PI3Kδ-IN-5					++++ PI3Kδ, IC50: 0.9 nM				99%
SRX3207		+ PI3K alpha, IC50: 244 nM		+ PI3K gamma, IC50: 9790 nM	+ PI3K delta, IC50: 388 nM			Syk	98%
Parsaclisib HCl					++++ PI3Kδ, IC50: 1 nM				98%
IHMT-PI3Kδ-372					+++ PI3Kδ, IC50: 14 nM				98%
Trigonelline						✔		Akt	99%+
Wortmannin						++++ PI3K, IC50: 3 nM		MLCK,DNA-PK	99%+
Samotolisib						✔		DNA-PK	99%+
GNE-317						✔			99%+
Oroxin B						✔		PTEN,Akt	99%+
NU 7026						+ PI3K, IC50: 13 μM		DNA-PK	98+%
Deguelin						✔		Akt	99%+
Ailanthone						✔		CDK,Akt,ATM/ATR	98%
Resibufogenin						✔		ROS	98%
KU-57788						+ PI3K, IC50: 5 μM		DNA-PK,mTOR	99%+
Cinobufagine						✔		Akt	99%
α-Linolenic acid						✔			97% (GC)
MTX-211						✔		EGFR	98%
PI3K/mTOR Inhibitor-2						++++ PI3K, IC50: 3.4 nM		mTOR	99%+
SPP-86						✔			99%+
(E)-Akt inhibitor-IV						✔			98%
Vps34-IN-1							++ Vps34, IC50: 25 nM		98%
SAR405							++++ Vps34, IC50: 1.2 nM		98+%
3-Methyladenine				+ PI3Kγ, IC50: 60 μM			+ Vps34, IC50: 25 μM	Autophagy	98%
Vps34-IN-4							+++ VPS34, IC50: 15 nM		98%+
Autophinib							+++ Vps34, IC50: 19 nM	Autophagy	99%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

产品名称	NF-κB ↓ ↑	其他靶点	纯度
Ammonium pyrrolidine-1-carbodithioate	✔		98%
QNZ	++++ NF-κB, IC50: 11 nM		99%+
Sodium 4-Aminosalicylate Dihydrate	✔		98%
Sodium Salicylate	✔		95%
Parthenolide	✔	p53	97% HPLC
JSH-23	+ NF-κB, IC50: 7.1 μM		98%
Phenethyl caffeate	✔		98%
Andrographolide	✔		98+%
Curcumin	✔	HDAC,Nrf2	98%
SC75741	+++ NF-κB, EC50: 200 nM		99%+
CBL0137 HCl	++ NF-κB, EC50: 0.47 μM	p53	99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

产品名称	Cdc ↓ ↑	CDK1 ↓ ↑	CDK19 ↓ ↑	CDK2 ↓ ↑	CDK3 ↓ ↑	CDK4 ↓ ↑	CDK5 ↓ ↑	CDK6 ↓ ↑	CDK7 ↓ ↑	CDK8 ↓ ↑	CDK9 ↓ ↑	CLK ↓ ↑	其他靶点	纯度
XL413 HCl	++++ Cdc7, IC50: 3.4 nM													99%+
SU9516		+++ CDK1, IC50: 40 nM		+++ CDK2, IC50: 22 nM		++ CDK4, IC50: 200 nM								99%+
RO-3306		+++ CDK1, Ki: 20 nM											SGK,ERK	98%
R547		++++ CDK1/CyclinB, Ki: 2 nM		++++ CDK2/CyclinE, Ki: 3 nM		++++ CDK4/CyclinD1, Ki: 1 nM								99%+
BMS-265246		++++ CDK1/CyclinB, IC50: 6 nM		++++ CDK2/CyclinE, IC50: 9 nM		+ CDK4/CyclinD, IC50: 230 nM								99%+
NU6027		+ CDK1, Ki: 2.5 μM		+ CDK2, Ki: 1.3 μM									DNA-PK	98%
Purvalanol A	++++ Cdc2/CyclinB, IC50: 4 nM			+++ CDK2/CyclinE, IC50: 35 nM CDK2/CyclinA, IC50: 70 nM		+ CDK4/CyclinD1, IC50: 850 nM								99%+
SCH900776				++ CDK2, IC50: 0.16 μM										99%+
AUZ 454				++++ CDK2(A144C), Kd: 9.7 nM CDK2(C118L), Kd: 18.6 nM										99%+
A-674563 HCl				++ CDK2, Ki: 46 nM									PKA	99%
JNJ-7706621		++++ CDK1/CyclinB, IC50: 9 nM		++++ CDK2/CyclinE, IC50: 3 nM CDK2/CyclinA, IC50: 4 nM	++ CDK3/CyclinE, IC50: 58 nM	+ CDK4/CyclinD1, IC50: 253 nM		++ CDK6/CyclinD1, IC50: 175 nM						99%+
AT7519		++ CDK1/CyclinB, IC50: 210 nM		++ CDK2/CyclinA, IC50: 47 nM	+ CDK3/CyclinE, IC50: 360 nM	++ CDK4/CyclinD1, IC50: 100 nM	+++ CDK5/p35, IC50: 13 nM	++ CDK6/CyclinD3, IC50: 170 nM			++++ CDK9/CyclinT, IC50: <10 nM			98+%
PHA-793887		++ CDK1/CyclinB, IC50: 60 nM		++++ CDK2/CyclinE, IC50: 8 nM CDK2/CyclinA, IC50: 8 nM		++ CDK4/CyclinD1, IC50: 62 nM	++++ CDK5/p25, IC50: 5 nM		++++ CDK7/CyclinH, IC50: 10 nM		++ CDK9/CyclinT1, IC50: 138 nM			99%+
Milciclib		+ CDK1/CyclinB, IC50: 398 nM		++ CDK2/CyclinE, IC50: 363 nM CDK2/CyclinA, IC50: 45 nM		++ CDK4/CyclinD1, IC50: 160 nM	+ CDK5/p35, IC50: 265 nM		++ CDK7/CyclinH, IC50: 150 nM					99%+
Kenpaullone		+ CDK1/CyclinB, IC50: 0.4μM		+ CDK2/CyclinE, IC50: 7.5μM CDK2/CyclinA, IC50: 0.68μM			+ CDK5/p35, IC50: 0.85μM							98%
SNS-032				+++ CDK2/CyclinE, IC50: 48 nM CDK2/CyclinA, IC50: 38 nM			+ CDK5/p35, IC50: 340 nM		++ CDK7/CyclinH, IC50: 62 nM		++++ CDK9/CyclinT, IC50: 4 nM			99%+
Dinaciclib		++++ CDK1, IC50: 3 nM		++++ CDK2, IC50: 1 nM			++++ CDK5, IC50: 1 nM				++++ CDK9, IC50: 4 nM			99%+
PHA-767491 HCl	++++ Cdc7, IC50: 10 nM	+ CDK1, IC50: 250 nM		+ CDK2, IC50: 240 nM			+ CDK5, IC50: 460 nM				+++ CDK9, IC50: 34 nM		MK2	99%
(R)-Roscovitine	+ Cdc2/CyclinB, IC50: 0.65 μM			+ CDK2/CyclinE, IC50: 0.7 μM CDK2/CyclinA, IC50: 0.7 μM			++ CDK5/p35, IC50: 0.16 μM							99%+
Narazaciclib						++++ CDK4/CyclinD1, IC50: 3.87 nM		++++ CDK6/CyclinD1, IC50: 9.82 nM					RET	99%+
Palbociclib						++++ CDK4/CyclinD3, IC50: 9 nM CDK4/CyclinD1, IC50: 11 nM		+++ CDK6/CyclinD2, IC50: 15 nM						99%
Abemaciclib						++++ CDK4, IC50: 2 nM		++++ CDK6, IC50: 10 nM						99%
Ribociclib						++++ CDK4, IC50: 10 nM		+++ CDK6, IC50: 39 nM						98%
Palbociclib isethionate						++++ CDK4/CyclinD3, IC50: 9 nM CDK4/CyclinD1, IC50: 11 nM		+++ CDK6/CyclinD2, IC50: 15 nM						99%+
BS-181 HCl									+++ CDK7, IC50: 21 nM					99%+
(E/Z)-THZ1 2HCl									++++ CDK7, IC50: 3.2 nM					99%+
LDC4297									++++ CDK7, IC50: 0.13 nM					99%+
Senexin A			+ CDK19, Kd: 0.31 μM							+ CDK8, Kd: 0.83 μM				99%
MSC2530818										++++ CDK8, IC50: 2.6 nM				99%+
Wogonin											✔			99%+
Riviciclib HCl		++ CDK1/CyclinB, IC50: 79 nM		+ CDK2/CyclinE, IC50: 2.54 μM CDK2/CyclinA, IC50: 224 nM		++ CDK4/CyclinD1, IC50: 63 nM		+ CDK6/CyclinD3, IC50: 396 nM	+ CDK7/CyclinH, IC50: 2.87 μM		+++ CDK9/CyclinT1, IC50: 20 nM			98%
LDC000067				+ CDK2, IC50: 2.441 μM							++ CDK9, IC50: 44 nM			98%
Flavopiridol		+++ CDK1, IC50: 40 nM		+++ CDK2, IC50: 40 nM		+++ CDK4, IC50: 40 nM		+++ CDK6, IC50: 40 nM	+ CDK7, IC50: 300 nM		+++ CDK9, IC50: 20 nM			99%+
LY2857785									+ CDK7, IC50: 0.246 μM	+++ CDK8, IC50: 0.016 μM	+++ CDK9, IC50: 0.011 μM			99%+
AZD-5438		+++ CDK1, IC50: 16 nM		++++ CDK2, IC50: 6 nM							+++ CDK9, IC50: 20 nM			99%+
ML167												++ CLK4, IC50: 136 nM Dyrk1B , IC50: 1648 nM		99%+
(E/Z)-TG003												+++ mCLK1, IC50: 200 nM mCLK4, IC50: 15 nM		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Resibufogenin/酯蟾毒配基生物活性

靶点

PI3K

描述

Necrosis can occur in a highly regulated and genetically controlled manner. Necroptotic susceptibility is probably an intrinsic weakness of cancer. Resibufogenin is a major bioactive compound that belongs to bufadienolide family. It is isolated from toad venom. Resibufogenin decreased the cell viability dose-dependently in HCT116 cells. The clonogenic cell survival assay showed that resibufogenin significantly reduced the number of cell clones as compared to the control group, provided further evidence that resibufogenin is an effective antineoplastic agent through inhibiting cell proliferation. Extensive organelle and cell swelling, cytoplasmic vacuolation were observed in resibufogenin-treated SW480 and HCT116. Intracellular ROS (reactive oxygen species) level was also increased in a dose-dependent manner in resibufogenin treated cells. After administration (i.p.) of resibufogenin at 5 and 10 mg/kg/day in mice for 21 days, the weight of tumor in situ were significantly reduced by 27 and 41%, respectively. Vernier caliper measurement showed that resibufogenin decreased the tumor volume in a dose-dependent manner. The weight loss caused by tumor growth was significantly ameliorated by high dose of resibufogenin. These results provide strong evidence that resibufogenin suppresses tumor growth of CRC (colorectal cancer) and ameliorates the weight loss in tumor-bearing mice. Remarkable increase in levels of PYGL, GLUD1 and GLUL as well as increase of RIP3 in resibufogenin-treated mice compared with the control group suggests that resibufogenin inhibits tumor growth through inducing RIP3-mediated activation of PYGL, GLUD1 and GLUL to induce necroptosis in CRC cells^[3].

Resibufogenin/酯蟾毒配基细胞实验

Cell Line Human renal cancer cell Caki-1 HepG2 cells RIP3+/+ and RIP3−/− mouse embryo fibroblasts (MEF) HCT-116 cells SW480 cells HPDE cells Aspc cells Panc-1 cells Human umbilical vein endothelial cells (HUVECs) Human umbilical vein endothelial cells (HUVECs) Human umbilical vein endothelial cells (HUVECs) A172 cells U251 cells P3#GBM cells	Concentration	Treated Time	Description	References
Human renal cancer cell Caki-1	10 nM, 50 nM, 100 nM, 200 nM	12 h and 24 h	Resibufogenin significantly inhibited the proliferation and migration of Caki-1 cells and induced apoptosis and necrosis in a dose-dependent manner.	Biology (Basel). 2024 Dec 19;13(12):1064.
HepG2 cells	1.25, 2.5, 5.0, 10.0, and 20.0 μg/mL	24, 48, and 72 h	To assess the in vitro cytotoxicity of nanoparticles on HepG2 cells. The results showed that the RGPPN group exhibited higher toxic effects than the RPN, RPPN, and RGP&PN groups, which was consistent with the fluorescence intensity and RBG content in the cellular uptake test.	Drug Deliv. 2017 Nov;24(1):1302-1316.
RIP3+/+ and RIP3−/− mouse embryo fibroblasts (MEF)	10 and 20 μM	24 h	To evaluate whether Resibufogenin-induced necrotic death is RIP3-dependent, results showed that RIP3−/− cells had higher viability than wild-type cells.	J Transl Med. 2018 Jul 20;16(1):201.
HCT-116 cells	0.1, 1, 2.5, 5, 10 μM	24–48 h	To evaluate the anti-proliferative activity of Resibufogenin on CRC cells, results showed that Resibufogenin dose-dependently reduced cell viability.	J Transl Med. 2018 Jul 20;16(1):201.
SW480 cells	0.1, 1, 2.5, 5, 10 μM	24–48 h	To evaluate the anti-proliferative activity of Resibufogenin on CRC cells, results showed that Resibufogenin dose-dependently reduced cell viability.	J Transl Med. 2018 Jul 20;16(1):201.
HPDE cells	58.12 μM (IC50)	48 h	To evaluate the cytotoxicity of RB on normal pancreatic epithelial cells HPDE, results showed that RB displayed selective cytotoxicity against tumor cells.	Cancer Sci. 2018 Nov;109(11):3611-3622.
Aspc cells	4.76 μM (IC50)	48 h	To evaluate the effect of RB on Aspc cell viability, results showed that RB significantly inhibited cell growth in a concentration- and time-dependent manner.	Cancer Sci. 2018 Nov;109(11):3611-3622.
Panc-1 cells	2.88 μM (IC50)	48 h	To evaluate the effect of RB on Panc-1 cell viability, results showed that RB significantly inhibited cell growth in a concentration- and time-dependent manner.	Cancer Sci. 2018 Nov;109(11):3611-3622.
Human umbilical vein endothelial cells (HUVECs)	1, 3 μM	24 h	To evaluate the effect of RBF on spheroid sprouting of HUVECs, results showed that RBF significantly inhibited the spheroid sprouting ability of HUVECs.	Front Pharmacol. 2021 Apr 30;12:682735.
Human umbilical vein endothelial cells (HUVECs)	0.3, 1, 3, 10 μM	10 h	To evaluate the effect of RBF on tube formation of HUVECs, results showed that RBF significantly inhibited the tube formation ability of HUVECs.	Front Pharmacol. 2021 Apr 30;12:682735.
Human umbilical vein endothelial cells (HUVECs)	0.3, 1, 3, 10, 30 μM	24 h	To evaluate the effect of RBF on the viability of HUVECs, results showed that RBF inhibited the cell viability of HUVECs in a dose-dependent manner with an IC50 value of 3 μM.	Front Pharmacol. 2021 Apr 30;12:682735.
A172 cells	6.21 μM (IC50)	48 h	RB significantly inhibited GBM cell proliferation and induced G2/M phase arrest	Front Pharmacol. 2022 May 17;13:855626.
U251 cells	3.05 μM (IC50)	48 h	RB significantly inhibited GBM cell proliferation and induced G2/M phase arrest	Front Pharmacol. 2022 May 17;13:855626.
P3#GBM cells	2.29 μM (IC50)	48 h	RB significantly inhibited GBM cell proliferation and induced G2/M phase arrest	Front Pharmacol. 2022 May 17;13:855626.

Cell Line

Concentration

Treated Time

Description

References

Human renal cancer cell Caki-1

10 nM, 50 nM, 100 nM, 200 nM

12 h and 24 h

Resibufogenin significantly inhibited the proliferation and migration of Caki-1 cells and induced apoptosis and necrosis in a dose-dependent manner.

Biology (Basel). 2024 Dec 19;13(12):1064.

HepG2 cells

1.25, 2.5, 5.0, 10.0, and 20.0 μg/mL

24, 48, and 72 h

To assess the in vitro cytotoxicity of nanoparticles on HepG2 cells. The results showed that the RGPPN group exhibited higher toxic effects than the RPN, RPPN, and RGP&PN groups, which was consistent with the fluorescence intensity and RBG content in the cellular uptake test.

Drug Deliv. 2017 Nov;24(1):1302-1316.

RIP3+/+ and RIP3−/− mouse embryo fibroblasts (MEF)

10 and 20 μM

24 h

To evaluate whether Resibufogenin-induced necrotic death is RIP3-dependent, results showed that RIP3−/− cells had higher viability than wild-type cells.

J Transl Med. 2018 Jul 20;16(1):201.

HCT-116 cells

0.1, 1, 2.5, 5, 10 μM

24–48 h

To evaluate the anti-proliferative activity of Resibufogenin on CRC cells, results showed that Resibufogenin dose-dependently reduced cell viability.

J Transl Med. 2018 Jul 20;16(1):201.

SW480 cells

0.1, 1, 2.5, 5, 10 μM

24–48 h

To evaluate the anti-proliferative activity of Resibufogenin on CRC cells, results showed that Resibufogenin dose-dependently reduced cell viability.

J Transl Med. 2018 Jul 20;16(1):201.

HPDE cells

58.12 μM (IC50)

48 h

To evaluate the cytotoxicity of RB on normal pancreatic epithelial cells HPDE, results showed that RB displayed selective cytotoxicity against tumor cells.

Cancer Sci. 2018 Nov;109(11):3611-3622.

Aspc cells

4.76 μM (IC50)

48 h

To evaluate the effect of RB on Aspc cell viability, results showed that RB significantly inhibited cell growth in a concentration- and time-dependent manner.

Cancer Sci. 2018 Nov;109(11):3611-3622.

Panc-1 cells

2.88 μM (IC50)

48 h

To evaluate the effect of RB on Panc-1 cell viability, results showed that RB significantly inhibited cell growth in a concentration- and time-dependent manner.

Cancer Sci. 2018 Nov;109(11):3611-3622.

Human umbilical vein endothelial cells (HUVECs)

1, 3 μM

24 h

To evaluate the effect of RBF on spheroid sprouting of HUVECs, results showed that RBF significantly inhibited the spheroid sprouting ability of HUVECs.

Front Pharmacol. 2021 Apr 30;12:682735.

Human umbilical vein endothelial cells (HUVECs)

0.3, 1, 3, 10 μM

10 h

To evaluate the effect of RBF on tube formation of HUVECs, results showed that RBF significantly inhibited the tube formation ability of HUVECs.

Front Pharmacol. 2021 Apr 30;12:682735.

Human umbilical vein endothelial cells (HUVECs)

0.3, 1, 3, 10, 30 μM

24 h

To evaluate the effect of RBF on the viability of HUVECs, results showed that RBF inhibited the cell viability of HUVECs in a dose-dependent manner with an IC50 value of 3 μM.

Front Pharmacol. 2021 Apr 30;12:682735.

A172 cells

6.21 μM (IC50)

48 h

RB significantly inhibited GBM cell proliferation and induced G2/M phase arrest

Front Pharmacol. 2022 May 17;13:855626.

U251 cells

3.05 μM (IC50)

48 h

RB significantly inhibited GBM cell proliferation and induced G2/M phase arrest

Front Pharmacol. 2022 May 17;13:855626.

P3#GBM cells

2.29 μM (IC50)

48 h

RB significantly inhibited GBM cell proliferation and induced G2/M phase arrest

Front Pharmacol. 2022 May 17;13:855626.

Resibufogenin/酯蟾毒配基动物实验

Species BALB/c-nu mice BALB/c nude mice C57BL/6 mice BALB/c nude mice	Animal Model Heterotropic CRC tumor model Aspc xenograft model Matrigel plug model Orthotopic xenograft model	Administration	Dosage	Frequency	Description	References
BALB/c-nu mice	Heterotropic CRC tumor model	Intraperitoneal injection	5 and 10 mg/kg	Once daily for 21 days	To evaluate the inhibitory effect of Resibufogenin on CRC tumor growth, results showed that Resibufogenin dose-dependently reduced tumor volume and weight.	J Transl Med. 2018 Jul 20;16(1):201.
BALB/c nude mice	Aspc xenograft model	Intragastric injection	10 mg/kg and 20 mg/kg	Once daily for 20 days	To evaluate the inhibitory effect of RB on Aspc xenograft tumor growth, results showed that RB significantly suppressed tumor growth without systemic toxicity.	Cancer Sci. 2018 Nov;109(11):3611-3622.
C57BL/6 mice	Matrigel plug model	Subcutaneous injection	10, 30 μM	7 days	To evaluate the antiangiogenic effect of RBF in vivo, results showed that RBF significantly inhibited VEGF-stimulated angiogenesis.	Front Pharmacol. 2021 Apr 30;12:682735.
BALB/c nude mice	Orthotopic xenograft model	Intraperitoneal injection	10 mg/kg	Daily until the end of the experiment	RB significantly inhibited tumor growth and prolonged the median survival of tumor-bearing mice	Front Pharmacol. 2022 May 17;13:855626.

Species

BALB/c-nu mice BALB/c nude mice C57BL/6 mice BALB/c nude mice

Animal Model

Heterotropic CRC tumor model Aspc xenograft model Matrigel plug model Orthotopic xenograft model

Administration

Dosage

Frequency

Description

References

BALB/c-nu mice

Heterotropic CRC tumor model

Intraperitoneal injection

5 and 10 mg/kg

Once daily for 21 days

To evaluate the inhibitory effect of Resibufogenin on CRC tumor growth, results showed that Resibufogenin dose-dependently reduced tumor volume and weight.

J Transl Med. 2018 Jul 20;16(1):201.

BALB/c nude mice

Aspc xenograft model

Intragastric injection

10 mg/kg and 20 mg/kg

Once daily for 20 days

To evaluate the inhibitory effect of RB on Aspc xenograft tumor growth, results showed that RB significantly suppressed tumor growth without systemic toxicity.

Cancer Sci. 2018 Nov;109(11):3611-3622.

C57BL/6 mice

Matrigel plug model

Subcutaneous injection

10, 30 μM

7 days

To evaluate the antiangiogenic effect of RBF in vivo, results showed that RBF significantly inhibited VEGF-stimulated angiogenesis.

Front Pharmacol. 2021 Apr 30;12:682735.

BALB/c nude mice

Orthotopic xenograft model

Intraperitoneal injection

10 mg/kg

Daily until the end of the experiment

RB significantly inhibited tumor growth and prolonged the median survival of tumor-bearing mice

Front Pharmacol. 2022 May 17;13:855626.

Resibufogenin/酯蟾毒配基参考文献

Resibufogenin/酯蟾毒配基实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.60mL

0.52mL

0.26mL

13.00mL

2.60mL

1.30mL

26.01mL

5.20mL

2.60mL

Resibufogenin/酯蟾毒配基技术信息

CAS号	465-39-4
分子式	C₂₄H₃₂O₄
分子量	384.51
SMILES Code	C[C@]([C@@H](C(C=C1)=COC1=O)C2)(CC[C@@]3([H])[C@@]4([H])CC[C@@]5([H])[C@@]3(CC[C@H](O)C5)C)[C@@]64[C@@H]2O6
MDL No.	MFCD00210361

别名	蟾力苏 ;Bufogenin; Recibufogenin; Bufotenine; RBG; Respigon; NSC 90783
运输	蓝冰

存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Inert atmosphere, 2-8°C

溶解方案

细胞实验：

DMSO: 105 mg/mL(273.08 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验：请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用；以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

方案二

方案三

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