Myricetin | Cannabiscetin;LDN-0014058;HSDB 7682;NSC 407290 | Plant Standard | PI3K

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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			Sirtuin,Src,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		DNA-PK,MLCK	99%+
Samotolisib						✔		DNA-PK	99%+
GNE-317						✔			99%+
Oroxin B						✔		Akt,PTEN	99%+
NU 7026						+ PI3K, IC50: 13 μM		DNA-PK	98+%
Deguelin						✔		Akt	99%+
Ailanthone						✔		Akt,CDK,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。

Cell Line INS-1 cells SK-BR-3 human breast cancer cells Schistosoma japonicum adult worms Rat islets Vero E6 cells THP1 macrophages	Concentration	Treated Time	Description	References
INS-1 cells	20 µM	24 hours	Myricetin significantly inhibited HG-induced apoptosis in INS-1 cells and reduced mitochondrial dysfunction.	Diabetes Metab J. 2019 Apr;43(2):192-205.
SK-BR-3 human breast cancer cells	0, 5, 10, 15, 20, 25 µM	24 hours	Myricetin inhibited the viability of SK-BR-3 cells in a dose-dependent manner. A significant increase in apoptosis was observed through DAPI and Annexin V/PI staining. Western blot analysis showed that myricetin induced the expression of apoptosis-related proteins, such as increased levels of cleaved PARP and Bax proteins, and decreased levels of Bcl-2 protein. Additionally, myricetin induced autophagy by promoting autophagy-related proteins such as LC 3 and beclin 1.	Int J Mol Med. 2022 Apr;49(4):54.
Schistosoma japonicum adult worms	300, 400, 500, 600, 700, 800 µM	24, 48, 72, 96 hours	Myricetin exhibited a time- and dose-dependent helminthicidal effect on adult S. japonicum in vitro, with an LC50 of 600 µM (24 hours). Myricetin significantly reduced the number of eggs laid by female worms.	Front Immunol. 2020 Apr 16;11:593.
Rat islets	20 µM	48 hours	Myricetin significantly inhibited HG-induced apoptosis in rat islets.	Diabetes Metab J. 2019 Apr;43(2):192-205.
Vero E6 cells	55.18 µM	72 hours	To evaluate the effect of Myricetin on SARS-CoV-2 replication, the results showed that Myricetin significantly inhibited SARS-CoV-2 replication.	Phytomedicine. 2023 Jul 25;116:154858.
THP1 macrophages	100, 200, 400 µM		To evaluate the effect of Myricetin on inflammation, the results showed that Myricetin significantly inhibited RIPK1-driven inflammation and NF-κB signaling pathway.	Phytomedicine. 2023 Jul 25;116:154858.

Species BALB/c mice Rats Nude mice Balb/c nu/nu mice Sprague-Dawley (SD) rats	Animal Model S. japonicum infection model Carrageenan-induced paw edema model Orthotopic pancreatic cancer model (MIA PaCa-2 and S2-013 cells) C4-2B xenograft model Carrageenan-induced paw edema model	Administration	Dosage	Frequency	Description	References
BALB/c mice	S. japonicum infection model	Oral	250 mg/kg	Daily for 7 days	Myricetin significantly reduced the liver egg load in S. japonicum-infected mice and alleviated liver fibrosis. Myricetin attenuated liver fibrosis via modulating TGFβ1 and Akt signaling and shifting Th1/Th2 balance.	Front Immunol. 2020 Apr 16;11:593.
Rats	Carrageenan-induced paw edema model	Oral	50, 100, 200 mg/kg	Once daily for 7 days	To evaluate the effect of Myricetin on inflammation, the results showed that Myricetin significantly alleviated carrageenan-induced paw edema.	Phytomedicine. 2023 Jul 25;116:154858.
Nude mice	Orthotopic pancreatic cancer model (MIA PaCa-2 and S2-013 cells)	Intraperitoneal injection	30mg/kg and 50mg/kg	Daily for 35 days (MIA PaCa-2 model) or 18 days (S2-013 model)	Myricetin significantly inhibited tumor growth and loco-regional spread without toxicity	Cancer Lett. 2011 Sep 28;308(2):181-8.
Balb/c nu/nu mice	C4-2B xenograft model	Intraperitoneal injection	20 mg/kg	Three times a week for 3 weeks	To evaluate the effect of PLGA-encapsulated myricetin on tumor growth in C4-2B xenograft model, results showed that PLGA-myricetin significantly inhibited tumor growth.	J Biomed Sci. 2022 May 9;29(1):29.
Sprague-Dawley (SD) rats	Carrageenan-induced paw edema model	Oral	50, 100, 200 mg/kg	Once daily for 7 days	Evaluate the anti-inflammatory effect of Myricetin on carrageenan-induced inflammation, results showed Myricetin significantly reduced inflammatory responses.	Phytomedicine. 2023 Jul 25;116:154858.

Dose	Rat: 5 mg/kg, 10 mg/kg^[3] (i.p.); 0.05 mg/kg - 5 mg/kg^[4] (i.v.) Mice: 10 mg/kg - 100 mg/kg^[5] (p.o.)
Administration	i.p., i.v., p.o.

CAS号	529-44-2
分子式	C₁₅H₁₀O₈
分子量	318.24
SMILES Code	OC1=CC(O)=C2C(=O)C(O)=C(OC2=C1)C1=CC(O)=C(O)C(O)=C1
MDL No.	MFCD00006827

别名	Cannabiscetin; LDN-0014058; HSDB 7682; NSC 407290
运输	蓝冰
InChI Key	IKMDFBPHZNJCSN-UHFFFAOYSA-N
Pubchem ID	5281672

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HCT116 cells		Growth inhibition assay	48 h	Growth inhibition of human HCT116 cells overexpressing PI3Kalpha H1047R mutant after 48 hrs by MTT assay, IC50=4.1 μM	22212721
HeLa cells		Function assay		Inhibition of MRP1 transfected in human HeLa cells assessed as inhibition of [3H]LTC4 transport by rapid filtration assay, Ki=2.4 μM	19725578
HT-29 cells		Function assay		Desensitization of GPR35 receptor in human HT-29 cells assessed as inhibition of zaprinast-induced dynamic mass redistribution after 10 mins, IC50=2.12 μM	24900447
human 22Rv1 cells		Proliferation assay	144 h	Antiproliferative activity against human 22Rv1 cells incubated up to 144 hrs by Coulter particle count and size analyzer, IC50=13.1 μM	22789812
human H9 cells		Function assay	3 days	Antiviral activity against HIV1 3B infected in human H9 cells assessed as inhibition of viral replication after 3 days by p24 antigen capture assay, EC50=35 μM	8158164
human HL60 cells	30 μM	Proliferation assay	48 h	Antiproliferative activity against human HL60 cells at 30 uM after 48 hrs by MTS assay	18258440
human SKBR3 cells		Function assay	24 h	Displacement of GM-cy3B from Hsp90 in human SKBR3 cells after 24 hrs by fluorescence polarization assay, IC50=13.5 μM	24548207
human U2OS cells		Function assay	5 h	Agonist activity at GPR35 receptor in human U2OS cells coexpressing Gal4-VP16-TEV assessed as beta arrestin translocation after 5 hrs by beta lactamase reporter gene assay, EC50=14.7 μM	24900447
mouse L929 cells		Function assay	2 h	Inhibition of recombinant human TNF-alpha-induced cytotoxicity of mouse L929 cells assessed as survivality treated with drug after 2 hrs of TNFalpha treatment	9287415
NCI-60 human tumor cell line		Cytotoxicity assay		In vitro cytotoxic potency against NCI-60 human tumor cell line, GI50=36 μM	9632366

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