Bcl-2

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研究领域

抑制剂选择性比较

特异性亚型抑制剂

Bcl-2产品

所有产品 Bcl-2抑制剂(17) Bcl-2激活剂(1) Bcl-2拮抗剂(3) Bcl-2调节剂(2) 新Bcl-2产品

产品目录	产品描述	文献引用	实验数据
S1002	ABT-737 ABT-737是一种BH3模拟抑制剂，作用于Bcl-xL，Bcl-2和Bcl-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。	Cancer Res, 2019, 79(9):2339-2351 Cell Rep, 2019, 27(12):3657-3671 Cell Rep, 2019, 27(3):820-834	Cardiomyocytes transduced with or without Ad-Mst1 were treated with ABT-737 (0, 0.1, 1, 10 uM) for 12 hours. Representative immunoblots with antibodies to p62/SQSTM1, LC3 and GAPDH are shown.
S1001	Navitoclax (ABT-263) Navitoclax (ABT-263)是一种有效的Bcl-xL，Bcl-2和Bcl-w抑制剂，无细胞试验中K_i分别为≤0.5 nM，≤1 nM和≤1 nM，但与Mcl-1和A1结合微弱。Phase 2。	Cell, 2019, 178(2):302-315.e23 Cell, 2019, 178(2):361-373 Cell, 2019, 178(2):302-315.e23
S1121	TW-37 TW-37是一种新型的非肽类抑制剂，作用于重组Bcl-2，Bcl-xL和Mcl-1，无细胞试验中K_i分别为0.29 μM， 1.11 μM和0.26 μM。	BMC Cancer, 2019, 19(1):243 Cancer Res, 2018, 78(16):4704-4715 PLoS One, 2018, 13(1):e0190682	(a) H23 cells exposed for 0–24 h to TW-37 (10 uM) with and without ZVAD.fmk (50 uM) were monitored for apoptotic morphology using electron microscopy (scale bar, 5 mm). % PS positive cells indicate the percentage of apoptotic cells, characterised by PS externalisation.
S8048	Venetoclax (ABT-199, GDC-0199) Venetoclax (ABT-199, GDC-0199)是一种Bcl-2选择性抑制剂，无细胞试验中K_i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。	Cell, 2019, 178(2):302-315.e23 Cell, 2019, 178(2):302-315.e23 Cancer Discov, 2019, 9(7):890-909	THP-1 cells were treated with cytarabine alone and in combination with ABT-199 for 8 h. Whole cell lysates were extracted and subjected to Western blotting, and probed with anti-γH2AX or -β-actin antibody. Densitometry for γH2AX expression was measured, normalized to β-actin, and graphed as fold change compared to the no drug control. The data are presented as mean ± standard error from at least 3 independent Western blots. * indicates p < 0.05.
S8643^New	AZD5991 AZD5991是MCL-1抑制剂，Ki值为0.13 nM。AZD5991对小鼠源Mcl-1的结合亲和力比对人源Mcl-1低25倍，而之比对大鼠源Mcl-1的亲和力低4倍。
S8836^New	S64315 (MIK665) S64315 (MIK665)是Mcl的抑制剂，Ki值为1.2 nM。它具有潜在的促凋亡和抗肿瘤活性。
S8759^New	S55746 (S 055746,BCL201) S55746 (S 055746,BCL201)是一种新型的、具有口服活性的BCL-2特异性抑制剂，Ki值为1.3 nM。它对Bcl-XL的亲和力弱，而对MCL-1、BFL-1(BCL2A1/A1)没有显著结合。S55746对BCL-2的选择性是对BCL-XL的70-400倍。
S2812	AT101 AT101，是醋酸棉酚的R-(-)对映体，与Bcl-2，Bcl-xL和Mcl-1结合，无细胞试验中K_i为0.32 μM，0.48 μM 和 0.18 μM；不抑制BIR3域和BID。Phase 2。	Invest New Drugs, 2019, 10.1007/s10637-019-00827-y Front Pharmacol, 2018, 9:1269 Cell Death Dis, 2016, 7:e2177	(B and C) assessment of antimigration capacity in each group by transwell migration assay. Abbreviations: CDDP, cisplatin; DMSO, dimethyl sulfoxide.
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。	Biochem Biophys Res Commun, 2015, 463(4):870-5 Oncotarget, 2015, 6(34):36113-25 J Biol Chem, 2014, 289(38):26481-91	ABT-737, Obatoclax, and HA14-1 eradicated the H1975 early tumor prosurvival resistance against dual-TKIs inhibition by erlotinib/SU11274 (ERL/SU). The experiment was carried out with H1975 cells , cells were pretreated with dual EGFR-MET inhibitors here, i.e., erlotinib (1 μmol/L)/SU11274 (1 μmol/L). BH3-mimetic used in treatment days 7-9 were all 2 μmol/L in concentration. Top, crystal violet cell survival staining assay. Bottom, BH3-mimetic treatment of the dual ERL/SU-resistant tumor cells induced a proapoptotic response.
S8061	Sabutoclax Sabutoclax是一种pan-Bcl-2抑制剂，作用于Bcl-xL， Bcl-2， Mcl-1和Bfl-1，IC50分别为0.31 μM， 0.32 μM， 0.20 μM和0.62 μM。	Cancer Res, 2018, 78(4):1097-1109 Cancer Lett, 2018, 423:47-59 Cell Death Differ, 2016, 23(10):1681-90	(e) Abs (490 nm) was measured by MTS assay in siControl or siPTBP1 treated PC3 cells with DMSO, 1000 nM ABT737, or 100 nM Sabutoclax for 48 h, showing no significant change in cell viability following siPTBP1 treatment in DMSO control, ABT737, or Sabutoclax treated cells. (f) PC3 cells transfected with siControl or a mixture of two siPTBP1 were treated with 1000 nM ABT737 or 100 nM Sabutoclax combined with various doses of docetaxel for 48 h and cell viability was assessed by MTS assay. The viability of cells with 1000 nM ABT737 or 100 nM Sabutoclax alone was set as 100%. All data are presented as mean±S.E.M., n=3. The statistical significance was determined by unpaired student t-test where P<0.05; P<0.01; **P<0.001.
S7790	A-1210477 A-1210477是一种有效的选择性MCL-1抑制剂，K_i和IC50分别为0.454 nM 和 26.2 nM，选择性比作用于其他Bcl-2家族成员高100多倍。	Cancer Cell, 2019, 35(5):752-766 EMBO Mol Med, 2019, 11(10):e10769 Haematologica, 2019, haematol.2019.220525	U251 glioblastoma (F) or MeWo melanoma (G) cells were treated with selective BH-3 mimetics, GTPP or the combination of both for 24 h (U251) or 48 h (MeWo). Thereafter, cells were stained with annexin V and propidium iodide and analyzed by flow cytometry. Shown are representative flow plots.
S2448	Gambogic Acid Gambogic Acid激活caspases，EC50为0.78 - 1.64 μM，且完全抑制Bcl-XL, Bcl-2, Bcl-W, Bcl-B, Bfl-1 和 Mcl-1，IC50分别为1.47 μM, 1.21 μM, 2.02 μM, 0.66 μM, 1.06 μM 和 0.79 μM。
S8383	S63845 S63845是一种新型的、选择性的MCL-1抑制剂，Kd值为0.19 nM。对其他Bcl-2成员，如Bcl-2或Bcl-xL，没有明显结合能力。	Cell, 2019, 178(2):302-315.e23 Cell, 2019, 178(2):302-315.e23 Nat Commun, 2019, 10(1):1444
S8177	BH3I-1 BH3I-1是Bcl-X_L-BH3 domain interaction抑制剂，Ki值为2.4 μM。它是一种Bcl-2家族蛋白的选择性抑制剂。
S7800	A-1155463 A-1155463是一种高度有效、选择性的BCL-XL抑制剂。其对BCL-XL的亲和力属于皮摩尔级别，对BCL-2、BCL-W（Ki=19 nM）、MCL-1（Ki>440 nM）的结合比对BCL-XL弱1000倍以上。	Nat Commun, 2019, 10(1):2556 Haematologica, 2019, haematol.2019.220525 Haematologica, 2018, 10.3324/haematol.2018.204958	Tumor growth rate (TGR) of tumors orthotopically implanted in rats on day 3, 7 and 10 compared to day 0. Rats were treated with doxorubicin, A-1155463 or a combination. Treatment with A-1155463 resulted in a significant decrease in TGR compared to control mice.
S7801	A-1331852 A-1331852是一种有效的、选择性的BCL-XL抑制剂，对Bcl-xL的Ki值小于0.01 nM，对Bcl-2, Bcl-W, MCL-1的Ki值分别为6 nM, 4 nM, 142 nM。它可能在治疗癌症、免疫和自体免疫疾病中有所作用。	Cancer Cell, 2019, 35(5):752-766 Nat Commun, 2019, 10(1):2556 Haematologica, 2019, haematol.2019.220525	Cells were treated with 0.5 μM A-1331852 and 1.5 nM VCR (RD), 0.5 nM VCR (RH30) for 72 h. Apoptosis was determined by analysis of DNA fragmentation of PI-stained nuclei using flow cytometry. Mean and SD of three independent experiments performed in triplicate are shown; **P < 0.01.
S7531	UMI-77 UMI-77是一种选择性Mcl-1抑制剂，Ki为490 nM，表现出高于Bcl-2家族其它成员的选择性。	Cell Death Dis, 2019, 10(3):185 BMC Cancer, 2017, 17(1):449 Mol Cell Biochem, 2017, 10.1007/s11010-017-2997-x	U87 and A172 cells were treated with UMI-77 (8 μM) for 24h and further treated with TRAIL (30 ng/ml) for indicated period of time. Levels of apoptosis-associated proteins were analyzed by Western blot. GAPDH was used as a loading control.
S7105	BAM7 BAM7是一种直接的，选择性的促凋亡Bax激动剂，EC50为3.3 μM。
S1057	Obatoclax Mesylate (GX15-070) Obatoclax Mesylate (GX15-070)是一种Bcl-2拮抗剂，无细胞试验中K_i为0.22 μM，可以协助抑制MCL-1介导的抗细胞凋亡作用。Phase 3。	Cancer Cell, 2019, 36(1):68-83 Cell Chem Biol, 2019, 10.1016/j.chembiol.2019.04.011 Int J Mol Sci, 2019, 20(6)	In vivo antitumor efﬁcacies of AZD2281 and GX15-070 alone or in combination in a BxPC-3 xenograft model. Tumor specimens were fixed in 10% formalin, embedded in paraffin, and cut into 4 lm-thick slides for H&E, PCNA, and CD34 staining.
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。
S7126	Marinopyrrole A (Maritoclax) Marinopyrrole A (Maritoclax)是一种选择性的Mcl-1拮抗剂。它能够结合Mcl-1，而不是Bcl-XL，引起其发生蛋白酶体降解。Maritoclax能够破坏Bim和Mcl-1的相互作用，IC50为10.1 μM。	Leukemia, 2019, 33(2):319-332
S8865^New	BAI1 BAI1是一种直接的BAX变构抑制剂，Kd值为15.0 ± 4 μM。
S8650	BTSA1 BTSA1是BAX激活剂，与其N端激活位点以高亲和力和特异性结合，诱导BAX发生构象变化，引起BAC介导的凋亡反应。BTSA1在白血病细胞系和病患样本中有效地促进凋亡，而不影响健康细胞。

产品目录	产品描述	文献引用	实验数据
S1002	ABT-737 ABT-737是一种BH3模拟抑制剂，作用于Bcl-xL，Bcl-2和Bcl-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。	Cancer Res,2019, 79(9):2339-2351 Cell Rep,2019, 27(12):3657-3671 Cell Rep,2019, 27(3):820-834	Cardiomyocytes transduced with or without Ad-Mst1 were treated with ABT-737 (0, 0.1, 1, 10 uM) for 12 hours. Representative immunoblots with antibodies to p62/SQSTM1, LC3 and GAPDH are shown.
S1001	Navitoclax (ABT-263) Navitoclax (ABT-263)是一种有效的Bcl-xL，Bcl-2和Bcl-w抑制剂，无细胞试验中K_i分别为≤0.5 nM，≤1 nM和≤1 nM，但与Mcl-1和A1结合微弱。Phase 2。	Cell,2019, 178(2):302-315.e23 Cell,2019, 178(2):361-373 Cell,2019, 178(2):302-315.e23
S1121	TW-37 TW-37是一种新型的非肽类抑制剂，作用于重组Bcl-2，Bcl-xL和Mcl-1，无细胞试验中K_i分别为0.29 μM， 1.11 μM和0.26 μM。	BMC Cancer,2019, 19(1):243 Cancer Res,2018, 78(16):4704-4715 PLoS One,2018, 13(1):e0190682	(a) H23 cells exposed for 0–24 h to TW-37 (10 uM) with and without ZVAD.fmk (50 uM) were monitored for apoptotic morphology using electron microscopy (scale bar, 5 mm). % PS positive cells indicate the percentage of apoptotic cells, characterised by PS externalisation.
S8048	Venetoclax (ABT-199, GDC-0199) Venetoclax (ABT-199, GDC-0199)是一种Bcl-2选择性抑制剂，无细胞试验中K_i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。	Cell,2019, 178(2):302-315.e23 Cell,2019, 178(2):302-315.e23 Cancer Discov,2019, 9(7):890-909	THP-1 cells were treated with cytarabine alone and in combination with ABT-199 for 8 h. Whole cell lysates were extracted and subjected to Western blotting, and probed with anti-γH2AX or -β-actin antibody. Densitometry for γH2AX expression was measured, normalized to β-actin, and graphed as fold change compared to the no drug control. The data are presented as mean ± standard error from at least 3 independent Western blots. * indicates p < 0.05.
S8643^New	AZD5991 AZD5991是MCL-1抑制剂，Ki值为0.13 nM。AZD5991对小鼠源Mcl-1的结合亲和力比对人源Mcl-1低25倍，而之比对大鼠源Mcl-1的亲和力低4倍。
S8836^New	S64315 (MIK665) S64315 (MIK665)是Mcl的抑制剂，Ki值为1.2 nM。它具有潜在的促凋亡和抗肿瘤活性。
S8759^New	S55746 (S 055746,BCL201) S55746 (S 055746,BCL201)是一种新型的、具有口服活性的BCL-2特异性抑制剂，Ki值为1.3 nM。它对Bcl-XL的亲和力弱，而对MCL-1、BFL-1(BCL2A1/A1)没有显著结合。S55746对BCL-2的选择性是对BCL-XL的70-400倍。
S2812	AT101 AT101，是醋酸棉酚的R-(-)对映体，与Bcl-2，Bcl-xL和Mcl-1结合，无细胞试验中K_i为0.32 μM，0.48 μM 和 0.18 μM；不抑制BIR3域和BID。Phase 2。	Invest New Drugs,2019, 10.1007/s10637-019-00827-y Front Pharmacol,2018, 9:1269 Cell Death Dis,2016, 7:e2177	(B and C) assessment of antimigration capacity in each group by transwell migration assay. Abbreviations: CDDP, cisplatin; DMSO, dimethyl sulfoxide.
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。	Biochem Biophys Res Commun,2015, 463(4):870-5 Oncotarget,2015, 6(34):36113-25 J Biol Chem,2014, 289(38):26481-91	ABT-737, Obatoclax, and HA14-1 eradicated the H1975 early tumor prosurvival resistance against dual-TKIs inhibition by erlotinib/SU11274 (ERL/SU). The experiment was carried out with H1975 cells , cells were pretreated with dual EGFR-MET inhibitors here, i.e., erlotinib (1 μmol/L)/SU11274 (1 μmol/L). BH3-mimetic used in treatment days 7-9 were all 2 μmol/L in concentration. Top, crystal violet cell survival staining assay. Bottom, BH3-mimetic treatment of the dual ERL/SU-resistant tumor cells induced a proapoptotic response.
S8061	Sabutoclax Sabutoclax是一种pan-Bcl-2抑制剂，作用于Bcl-xL， Bcl-2， Mcl-1和Bfl-1，IC50分别为0.31 μM， 0.32 μM， 0.20 μM和0.62 μM。	Cancer Res,2018, 78(4):1097-1109 Cancer Lett,2018, 423:47-59 Cell Death Differ,2016, 23(10):1681-90	(e) Abs (490 nm) was measured by MTS assay in siControl or siPTBP1 treated PC3 cells with DMSO, 1000 nM ABT737, or 100 nM Sabutoclax for 48 h, showing no significant change in cell viability following siPTBP1 treatment in DMSO control, ABT737, or Sabutoclax treated cells. (f) PC3 cells transfected with siControl or a mixture of two siPTBP1 were treated with 1000 nM ABT737 or 100 nM Sabutoclax combined with various doses of docetaxel for 48 h and cell viability was assessed by MTS assay. The viability of cells with 1000 nM ABT737 or 100 nM Sabutoclax alone was set as 100%. All data are presented as mean±S.E.M., n=3. The statistical significance was determined by unpaired student t-test where P<0.05; P<0.01; **P<0.001.
S7790	A-1210477 A-1210477是一种有效的选择性MCL-1抑制剂，K_i和IC50分别为0.454 nM 和 26.2 nM，选择性比作用于其他Bcl-2家族成员高100多倍。	Cancer Cell,2019, 35(5):752-766 EMBO Mol Med,2019, 11(10):e10769 Haematologica,2019, haematol.2019.220525	U251 glioblastoma (F) or MeWo melanoma (G) cells were treated with selective BH-3 mimetics, GTPP or the combination of both for 24 h (U251) or 48 h (MeWo). Thereafter, cells were stained with annexin V and propidium iodide and analyzed by flow cytometry. Shown are representative flow plots.
S2448	Gambogic Acid Gambogic Acid激活caspases，EC50为0.78 - 1.64 μM，且完全抑制Bcl-XL, Bcl-2, Bcl-W, Bcl-B, Bfl-1 和 Mcl-1，IC50分别为1.47 μM, 1.21 μM, 2.02 μM, 0.66 μM, 1.06 μM 和 0.79 μM。
S8383	S63845 S63845是一种新型的、选择性的MCL-1抑制剂，Kd值为0.19 nM。对其他Bcl-2成员，如Bcl-2或Bcl-xL，没有明显结合能力。	Cell,2019, 178(2):302-315.e23 Cell,2019, 178(2):302-315.e23 Nat Commun,2019, 10(1):1444
S8177	BH3I-1 BH3I-1是Bcl-X_L-BH3 domain interaction抑制剂，Ki值为2.4 μM。它是一种Bcl-2家族蛋白的选择性抑制剂。
S7800	A-1155463 A-1155463是一种高度有效、选择性的BCL-XL抑制剂。其对BCL-XL的亲和力属于皮摩尔级别，对BCL-2、BCL-W（Ki=19 nM）、MCL-1（Ki>440 nM）的结合比对BCL-XL弱1000倍以上。	Nat Commun,2019, 10(1):2556 Haematologica,2019, haematol.2019.220525 Haematologica,2018, 10.3324/haematol.2018.204958	Tumor growth rate (TGR) of tumors orthotopically implanted in rats on day 3, 7 and 10 compared to day 0. Rats were treated with doxorubicin, A-1155463 or a combination. Treatment with A-1155463 resulted in a significant decrease in TGR compared to control mice.
S7801	A-1331852 A-1331852是一种有效的、选择性的BCL-XL抑制剂，对Bcl-xL的Ki值小于0.01 nM，对Bcl-2, Bcl-W, MCL-1的Ki值分别为6 nM, 4 nM, 142 nM。它可能在治疗癌症、免疫和自体免疫疾病中有所作用。	Cancer Cell,2019, 35(5):752-766 Nat Commun,2019, 10(1):2556 Haematologica,2019, haematol.2019.220525	Cells were treated with 0.5 μM A-1331852 and 1.5 nM VCR (RD), 0.5 nM VCR (RH30) for 72 h. Apoptosis was determined by analysis of DNA fragmentation of PI-stained nuclei using flow cytometry. Mean and SD of three independent experiments performed in triplicate are shown; **P < 0.01.
S7531	UMI-77 UMI-77是一种选择性Mcl-1抑制剂，Ki为490 nM，表现出高于Bcl-2家族其它成员的选择性。	Cell Death Dis,2019, 10(3):185 BMC Cancer,2017, 17(1):449 Mol Cell Biochem,2017, 10.1007/s11010-017-2997-x	U87 and A172 cells were treated with UMI-77 (8 μM) for 24h and further treated with TRAIL (30 ng/ml) for indicated period of time. Levels of apoptosis-associated proteins were analyzed by Western blot. GAPDH was used as a loading control.

产品目录	产品描述	文献引用	实验数据
S7105	BAM7 BAM7是一种直接的，选择性的促凋亡Bax激动剂，EC50为3.3 μM。

产品目录

产品描述

文献引用

实验数据

S7105

BAM7

BAM7是一种直接的，选择性的促凋亡Bax激动剂，EC50为3.3 μM。

产品目录	产品描述	文献引用	实验数据
S1057	Obatoclax Mesylate (GX15-070) Obatoclax Mesylate (GX15-070)是一种Bcl-2拮抗剂，无细胞试验中K_i为0.22 μM，可以协助抑制MCL-1介导的抗细胞凋亡作用。Phase 3。	Cancer Cell, 2019, 36(1):68-83 Cell Chem Biol, 2019, 10.1016/j.chembiol.2019.04.011 Int J Mol Sci, 2019, 20(6)	In vivo antitumor efﬁcacies of AZD2281 and GX15-070 alone or in combination in a BxPC-3 xenograft model. Tumor specimens were fixed in 10% formalin, embedded in paraffin, and cut into 4 lm-thick slides for H&E, PCNA, and CD34 staining.
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。
S7126	Marinopyrrole A (Maritoclax) Marinopyrrole A (Maritoclax)是一种选择性的Mcl-1拮抗剂。它能够结合Mcl-1，而不是Bcl-XL，引起其发生蛋白酶体降解。Maritoclax能够破坏Bim和Mcl-1的相互作用，IC50为10.1 μM。	Leukemia, 2019, 33(2):319-332

产品目录

产品描述

文献引用

实验数据

S1057

Obatoclax Mesylate (GX15-070)

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

Cancer Cell, 2019, 36(1):68-83

Cell Chem Biol, 2019, 10.1016/j.chembiol.2019.04.011

Int J Mol Sci, 2019, 20(6)

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。

S7126

Marinopyrrole A (Maritoclax)

Marinopyrrole A (Maritoclax)是一种选择性的Mcl-1拮抗剂。它能够结合Mcl-1，而不是Bcl-XL，引起其发生蛋白酶体降解。Maritoclax能够破坏Bim和Mcl-1的相互作用，IC50为10.1 μM。

Leukemia, 2019, 33(2):319-332

产品目录	产品描述	文献引用	实验数据
S8865^New	BAI1 BAI1是一种直接的BAX变构抑制剂，Kd值为15.0 ± 4 μM。
S8650	BTSA1 BTSA1是BAX激活剂，与其N端激活位点以高亲和力和特异性结合，诱导BAX发生构象变化，引起BAC介导的凋亡反应。BTSA1在白血病细胞系和病患样本中有效地促进凋亡，而不影响健康细胞。

产品目录

产品描述

文献引用

实验数据

S8865^New