ACBI1 | SMARCA2/SMARCA4/PBRM1 Degrader | AmBeed-信号通路专用抑制剂

ACBI1 {[allProObj[0].p_purity_real_show]}

货号：A1339706

ACBI1 是一种基于 PROTAC 的有效 BAF ATPase 亚基 SMARCA2 和 SMARCA4 以及 PBAF 复合体成员 PBRM1 的降解剂。它表现出抗癌活性并诱导细胞凋亡，对 SMARCA2、SMARCA4 和 PBRM1 的 DC50 值分别为 6 nM、11 nM 和 32 nM。

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Type	HazMat fee for 500 gram (Estimated)
Excepted Quantity	USD 0.00
Limited Quantity	USD 15-60
Inaccessible (Haz class 6.1), Domestic	USD 80+
Inaccessible (Haz class 6.1), International	USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic	USD 100+
Accessible (Haz class 3, 4, 5 or 8), International	USD 200+

ACBI1 化学结构
CAS号：2375564-55-7

ACBI1 3D分子结构
CAS号：2375564-55-7

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表观遗传阅读框亚型比较

产品名称	BET ↓ ↑	bromodomain ↓ ↑	BRPF ↓ ↑	CBP/beta-catenin ↓ ↑	p300/CBP ↓ ↑	其他靶点	纯度
MS436	++ BRD4 (1), Ki: <0.085 μM BRD4 (2), Ki: 0.34 μM						99%+
CPI-203	+++ BRD4, IC50: 37 nM						98+%
GSK1324726A	+++ BRD2, IC50: 31 nM BRD4, IC50: 22 nM						99%+
PFI-1	++ BRD2, IC50: 98 nM BRD4, IC50: 0.22 μM						98%
Apabetalone	+ BD2, IC50: 0.51 μM						99%
(+)-JQ1	+++ BRD4 (1), IC50: 77 nM BRD4 (2), IC50: 33 nM						98%
I-BET151	+ BRD3, IC50: 0.25 μM BRD4, IC50: 0.5 μM						98%
Molibresib	+++ BET proteins, IC50: 35 nM						99%+
I-BRD9	+++ BRD4, pIC50: 5.3 BRD9, pIC50: 7.3						99%+
BI-7273	++++ BRD7, IC50: 117 nM BRD9, IC50: 19 nM						97%
Pelabresib	+++ BRD4-BD1, IC50: 39 nM						98%
ARV-825	+++ BRD4 BD1, Kd: 90 nM BRD4 BD2, Kd: 28 nM						99%+
Birabresib							99%+
BI 2536	+++ BRD4, Kd: 37 nM					c-Myc	99%+
Bromosporine	++ BRD2, IC50: 0.29 μM BRD9, IC50: 0.122 μM	++++ CECR2, IC50: 17 nM					99%+
XMD8-92	++ BRD4 (1), Kd: 170 nM						99%+
Mivebresib	✔						99%+
BI-9564	++++ BRD9, Kd: 5.9 nM BRD7, Kd: 73 nM	++ CECR2, Kd: 77 nM					98%
AZD5153 6-Hydroxy-2-naphthoic acid	++++ FL-BRD4, IC50: 5 nM						99%+
PLX51107	++++ BRD4 BD2, Kd: 1.7 nM BRD3 BD1, Kd: 2.1 nM						99%+
FL-411	+ BRD4(1), IC50: 0.43 μM						99%+
ABBV-744	✔						99%+
dBET6	++++ BRD4, IC50: 14 nM						99%+
dBET1	++++ BRD4, IC50: 20 nM						99%+
MZ1	++++ Brd3(BD2), Kd: 13 nM Brd2(BD2), Kd: 62 nM						99%+
dBET57	+ BRD4_BD1, DC50: 500 nM						99%+
SF2523	+ BRD4, IC50: 241 nM					DNA-PK	99%+
INCB054329	++++ BRD3-BD1, IC50: 9 nM BRD4-BD1, IC50: 119 nM						99%
INCB-057643	✔						99%+
(E/Z)-ZL0420	+++ BRD4 BD1, IC50: 27 nM BRD4 BD2, IC50: 32 nM						99%+
BMS-986158	✔						99%
BRD4 Inhibitor-10	++++ BRD4-BD1, IC50: 5 nM BRD4-BD2, IC50: 41 nM						97%
A1874	✔						99%+
Y06036	++ BRD4 (1), Kd: 82 nM						99%+
Alobresib	✔					NF-κB	95%
ODM-207	✔						98%
GSK778	+++ BRD2-BD1, IC50: 75nM BRD4-BD1, IC50: 143 nM						97%
SRX3207	+ BRD42, IC50: 3070 nM BRD41, IC50: 3070 nM					Syk	98%
GSK046	+++ BRD3_BD2, IC50: 98 nM BRD4_BD2, IC50: 214 nM						98%
GSK620	✔						97%
Trotabresib	✔						99%
NHWD-870	✔						98%
CFT8634	++++ BRD9, DC50: 3 nM						98%
GSK2801		++ BAZ2A, Kd: 257 nM BAZ2B, Kd: 136 nM					99%+
KG-501		✔					99%+
UNC 669		+ L3MBTL3, IC50: 35 μM L3MBTL4, IC50: 6 μM					99%
PFI-3		+++ SMARCA2A, Kd: 72 nM SMARCA4, Kd: 55 nM					99%+
UNC1215		+++ L3MBTL3, IC50: 120 nM L3MBTL3- D274A, IC50: 3.5 μM					99%+
EED226		++ EED, Kd: 82 nM PRC2, Kd: 114 nM					99%+
BRD9539		✔					98%
UNC926		+ L3MBTL1, Kd: 3.9 μM					99%
666-15		++ CREB, IC50: 81 nM					99%+
UNC6852		+ EED, IC50: 247 nM					98%
BAZ1A-IN-1		+ BAZ1A, Kd: 0.52 μM					99%+
PFI-4			++ BRPF2, IC50: 7.9 μM BRPF1, IC50: 80 nM				99%+
OF-1			++ BRPF1B, Kd: 100 nM BRPF2, Kd: 500 nM				99%+
GSK-5959			++ BRPF3, pIC50: 7.1 BRPF2, pIC50: 5.2				99%
GSK6853			++++ BRPF1, pIC50: 8.1				99%+
NI-42			++++ BRPF3, IC50: 260 nM BRPF1, IC50: 48 nM				99%+
E-7386				+++ CBP/beta-catenin, IC50: 0.0484 μM			99%
I-CBP112					++ p300, Kd: 167 nM CBP, Kd: 151 nM		98+%
Histone Acetyltransferase Inhibitor II					+ p300, IC50: 5 μM		98%
C646					+ p300/CBP, Ki: 400 nM		99%+
Anacardic Acid					+ p300/CBP, IC50: 8.5 μM PCAF, IC50: 5 μM		99%+
SGC-CBP30					++++ EP300, IC50: 38 nM CREBBP, IC50: 21 nM		99%+
Nordihydroguaiaretic acid					✔	IGF-1R,HER2	99%+
Curcumin					+ p300, IC50: ~25 μM	Nrf2,Ferroptosis,NF-κB	98%
CPI-637					+++ CBP, IC50: 0.03 μM EP300, IC50: 0.051 μM		99%+
Foscenvivint					✔	β-catenin	99%+
A-485					++ p300 HAT, IC50: 0.06 μM		99%+
GNE-781	+ BRD4(1), IC50: 5100 nM				++++ CBP, IC50: 0.94 nM		99%
NEO2734	+++ BET, IC50: <30 nM				+++ p300/CBP, IC50: <30 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。

ACBI1 生物活性

描述

ACBI1 is a potent and synergistic degrader of SMARCA2, SMARCA4, and PBRM1 with DC50 values of 6, 11, and 32 nM, respectively. It functions as a PROTAC degrader, exhibiting anti-proliferative activity and inducing apoptosis^[1].

体外研究

ACBI1 (1-10000 nM; 3-7 days) exhibits anti-proliferative activity^[1].

ACBI1 (0.3 µM; 100 h) triggers apoptosis in SK-MEL-5 cells^[1].

ACBI1 comprises a bromodomain ligand, a linker, and the E3 ubiquitin ligase von Hippel-Lindau^[1].

ACBI1 细胞实验

Cell Line MV-4-11 cells MV-4-11 cells MV-4-11 cells Rh30 NCI-H1568 cells NCI-H1568 cells Rh30 HEK293T cells HS-SY-II cells G401 cells	Concentration	Treated Time	Description	References
MV-4-11 cells	32 nM	18 h	Degradation of PBRM1	Nat Chem Biol. 2019 Jul;15(7):672-680.
MV-4-11 cells	11 nM	18 h	Degradation of SMARCA4	Nat Chem Biol. 2019 Jul;15(7):672-680.
MV-4-11 cells	6 nM	18 h	Degradation of SMARCA2	Nat Chem Biol. 2019 Jul;15(7):672-680.
Rh30	200 nM	24-48 hours	To evaluate the effect of ACBI1 on PBRM1 protein expression	Oncogene. 2022 Mar;41(11):1647-1656.
NCI-H1568 cells	15.6 nM	18 h	Degradation of PBRM1	Nat Chem Biol. 2019 Jul;15(7):672-680.
NCI-H1568 cells	3.3 nM	18 h	Degradation of SMARCA2	Nat Chem Biol. 2019 Jul;15(7):672-680.
Rh30	50 nM	3 days	To evaluate the effect of ACBI1 on SMARCA4 and SMARCA2 protein expression	Oncogene. 2022 Mar;41(11):1647-1656.
HEK293T cells	500 nM	72 hours	To evaluate the effect of ACBI1 on SMARCA4 protein levels in HEK293T cells, results showed that ACBI1 treatment led to a reduction in SMARCA4 protein levels.	Nat Struct Mol Biol. 2023 Nov;30(11):1640-1652.
HS-SY-II cells	500 nM	72 hours	To evaluate the effect of ACBI1 on SMARCA4 protein levels in HS-SY-II cells, results showed that ACBI1 treatment led to a reduction in SMARCA4 protein levels.	Nat Struct Mol Biol. 2023 Nov;30(11):1640-1652.
G401 cells	250 nM	1 hour to 24 hours	To evaluate the effect of ACBI1 on BRG1 and PBRM1 protein levels, results showed that ACBI1 rapidly reduced BRG1 and PBRM1 levels.	Oncogenesis. 2022 Jun 1;11(1):30.

Cell Line

Concentration

Treated Time

Description

References

MV-4-11 cells

32 nM

18 h

Degradation of PBRM1

Nat Chem Biol. 2019 Jul;15(7):672-680.

MV-4-11 cells

11 nM

18 h

Degradation of SMARCA4

Nat Chem Biol. 2019 Jul;15(7):672-680.

MV-4-11 cells

6 nM

18 h

Degradation of SMARCA2

Nat Chem Biol. 2019 Jul;15(7):672-680.

Rh30

200 nM

24-48 hours

To evaluate the effect of ACBI1 on PBRM1 protein expression

Oncogene. 2022 Mar;41(11):1647-1656.

NCI-H1568 cells

15.6 nM

18 h

Degradation of PBRM1

Nat Chem Biol. 2019 Jul;15(7):672-680.

NCI-H1568 cells

3.3 nM

18 h

Degradation of SMARCA2

Nat Chem Biol. 2019 Jul;15(7):672-680.

Rh30

50 nM

3 days

To evaluate the effect of ACBI1 on SMARCA4 and SMARCA2 protein expression

Oncogene. 2022 Mar;41(11):1647-1656.

HEK293T cells

500 nM

72 hours

To evaluate the effect of ACBI1 on SMARCA4 protein levels in HEK293T cells, results showed that ACBI1 treatment led to a reduction in SMARCA4 protein levels.

Nat Struct Mol Biol. 2023 Nov;30(11):1640-1652.

HS-SY-II cells

500 nM

72 hours

To evaluate the effect of ACBI1 on SMARCA4 protein levels in HS-SY-II cells, results showed that ACBI1 treatment led to a reduction in SMARCA4 protein levels.

Nat Struct Mol Biol. 2023 Nov;30(11):1640-1652.

G401 cells

250 nM

1 hour to 24 hours

To evaluate the effect of ACBI1 on BRG1 and PBRM1 protein levels, results showed that ACBI1 rapidly reduced BRG1 and PBRM1 levels.

Oncogenesis. 2022 Jun 1;11(1):30.

ACBI1 参考文献

ACBI1 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

1.07mL

0.21mL

0.11mL

5.34mL

1.07mL

0.53mL

10.68mL

2.14mL

1.07mL

ACBI1 技术信息

CAS号	2375564-55-7
分子式	C₄₉H₅₈FN₉O₇S
分子量	936.1
SMILES Code	CC(N=CS1)=C1C2=CC=C(CNC([C@@H]3C[C@@H](O)CN3C([C@H](C(C)(C)C)NC(C4(CC4)F)=O)=O)=O)C(OCCOC5=CC=C(CN6CCN(C7=CC(C8=C(O)C=CC=C8)=NN=C7N)CC6)C=C5)=C2
MDL No.	MFCD32689497

别名
运输	蓝冰

存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C

溶解方案

细胞实验：

DMSO: 105 mg/mL(112.17 mM)，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

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