Bcl-2 选择性抑制剂 | 拮抗剂 | 调节剂

目录号 产品名 产品描述 Selective / Pan IC50 / Ki
S8048 Venetoclax (ABT-199)

Venetoclax (ABT-199, GDC-0199)是一种Bcl-2选择性抑制剂,无细胞试验中Ki为<0.01 nM,比作用于Bcl-xL和Bcl-w选择性高4800倍以上,对Mcl-1没有抑制活性。Phase 3。

Selective Bcl-2, Ki: <0.01 nM
S8759 S55746

S55746 (S 055746,BCL201) is a novel, orally active BCL-2 specific inhibitor (Ki = 1.3 nM) with poor affinity for BCL-XL and no significant binding to MCL-1, BFL-1 (BCL2A1/A1). The selectivity of S55746 for BCL-2 versus BCL-XL ranges from ~70 to 400 folds.

Selective Bcl-2, Ki: 1.3 nM
S7849 BDA-366

BDA-366是Bcl2-BH4的小分子拮抗剂,能与BH4高亲和力、高选择性地结合。它与Bcl2直接高亲和力结合,Ki值为3.3 ± 0.73 nM。

Selective Bcl2-BH4, Ki: 3.3 nM
S1057 Obatoclax Mesylate (GX15-070)

Obatoclax Mesylate (GX15-070)是一种Bcl-2拮抗剂,无细胞试验中Ki为0.22 μM,可以协助抑制MCL-1介导的抗细胞凋亡作用。Phase 3。

Selective Bcl-2, Ki: 0.22 μM
S1071 HA14-1

HA14-1是一种Bcl-2表面口袋的非肽配体,IC50为9 μM左右。

Selective Bcl-2, IC50: 9 μM
S2606 Mifepristone (RU486)

Mifepristone是一种异常活跃的孕激素受体和糖皮质激素受体拮抗剂,IC50分别为0.2nM和2.6 nM。

Selective
S3224 Cinobufagin

Cinobufagin (Cinobufagine), an active ingredient of Venenum Bufonis, inhibits tumor development. Cinobufagin increases ATM and Chk2 and decreases CDC25C, CDK1, and cyclin B. Cinobufagin inhibits PI3K, AKT and Bcl-2 while increases levels of cleaved caspase-9 and caspase-3. Thus, Cinobufagin induces cell cycle arrest at the G2/M phase and apoptosis.

Selective
S1001 Navitoclax (ABT-263)

Navitoclax (ABT-263)是一种有效的Bcl-xLBcl-2Bcl-w抑制剂,无细胞试验中Ki分别为≤0.5 nM,≤1 nM和≤1 nM,但与Mcl-1和A1结合微弱。Phase 2。

Pan Bcl-2, Ki: <=1 nM
S1002 ABT-737

ABT-737是一种BH3模拟抑制剂,作用于Bcl-xLBcl-2Bcl-w,无细胞试验中EC50分别为78.7 nM,30.3 nM和197.8 nM;但对Mcl-1, Bcl-B及Bfl-1没有抑制作用。Phase 2。

Pan Bcl-2, EC50: 30.3 nM
S1121 TW-37

TW-37是一种新型的非肽类抑制剂,作用于重组Bcl-2Bcl-xLMcl-1,无细胞试验中Ki分别为0.29 μM, 1.11 μM和0.26 μM。

Pan Bcl-2, Ki: 0.29 μM
S2812 (R)-(-)-Gossypol acetic acid

AT101,是醋酸棉酚的R-(-)对映体,与Bcl-2Bcl-xLMcl-1结合,无细胞试验中Ki为0.32 μM,0.48 μM 和 0.18 μM;不抑制BIR3域和BID。Phase 2。

Pan Bcl-2, Ki: 0.32 μM
S8061 Sabutoclax

Sabutoclax是一种pan-Bcl-2抑制剂,作用于Bcl-xLBcl-2Mcl-1Bfl-1IC50分别为0.31 μM, 0.32 μM, 0.20 μM和0.62 μM。

Pan Bfl-1, IC50: 0.62 μM; Bcl-2, IC50: 0.32 μM
S2448 Gambogic Acid

Gambogic Acid激活caspasesEC50为0.78 - 1.64 μM,且完全抑制Bcl-XL, Bcl-2, Bcl-W, Bcl-B, Bfl-1Mcl-1IC50分别为1.47 μM, 1.21 μM, 2.02 μM, 0.66 μM, 1.06 μM 和 0.79 μM。

Pan Bfl-1, IC50: 1.06 μM; Bcl-2, IC50: 1.21 μM
S6852 Gossypol

Gossypol (BL 193) is an orally-active polyphenol isolated from cotton seeds and roots. Gossypol is a potent inhibitor of 5α-reductase 1 and 3α-hydroxysteroid dehydrogenase with IC50 of 3.33 μM and 0.52 μM in cell-free assay, respectively. Gossypol also inhibits the binding of BH3 peptide to Bcl protein with IC50 of 0.4 μM and 10 μM for Bcl-XL and Bcl-2, respectively. Gossypol induces apoptosis and cell growth inhibition in various cancer cells.

Pan Bcl-2, IC50: 10 μM
S3245 Nodakenetin

Nodakenetin (NANI), a plant-derived coumarin isolated from Angelica decursiva, inhibits α-glucosidase, PTP1B, rat lens aldose reductase (RLAR), AChE, BChE, and β-site amyloid precursor protein cleaving enzyme 1 (BACE1). Nodakenetin alters the protein expression of Bax and Bcl-2, and prompts mitochondrial apoptosis. Nodakenetin exhibits anti-tumor activity.

Pan
S5967 Berberine chloride hydrate

Berberine (Natural Yellow 18) chloride hydrate is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of

Pan
S9665 Motixafortide (BL-8040)

Motixafortide (BL-8040, BKT140, TF 14016, 4-fluorobenzoyl, 4F-benzoyl-TN14003, T140) is an antagonist of CXCR4 with IC50 of ~1 nM. BL-8040 induces the apoptosis of AML blasts by down-regulating ERK, BCL-2, MCL-1 and cyclin-D1 via altered miR-15a/16-1 expression.

Pan
S2271 Berberine chloride (NSC 646666)

Berberine chloride是异喹啉类生物碱的季铵盐。

Pan
S3267 Kaempferol-3-O-rutinoside

Kaempferol-3-O-rutinoside (Nicotiflorin, Nikotoflorin, Kaempferol 3-O-β-rutinoside), a flavonoid extracted from Carthamus tinctorius, alters the shape and structure of injured neurons, decreases the number of apoptotic cells, down-regulates expression of p-JAK2, p-STAT3, caspase-3, and Bax and decreases Bax immunoredactivity, and increases Bcl-2 protein expression and immunoreactivity.

Pan