Bcl-2
信号通路图
研究领域
- 抑制剂选择性比较
- 溶解性比较
| 目录号 | 产品目录 | 溶解度(25°C) | ||
|---|---|---|---|---|
| 水 | DMSO | 酒精 | ||
| S1002 | ABT-737 | <1 mg/mL | 100 mg/mL | <1 mg/mL |
| S1001 | Navitoclax (ABT-263) | <1 mg/mL | 100 mg/mL | <1 mg/mL |
| S1121 | TW-37 | <1 mg/mL | 115 mg/mL | 4 mg/mL |
| S8048 | Venetoclax (ABT-199, GDC-0199) | <1 mg/mL | 100 mg/mL | <1 mg/mL |
| S8759 | S55746 (S 055746,BCL201) | <1 mg/mL | 100 mg/mL | <1 mg/mL |
| S2812 | AT101 | <1 mg/mL | 116 mg/mL | 89 mg/mL |
| S1071 | HA14-1 | <1 mg/mL | 82 mg/mL | 82 mg/mL |
| S8061 | Sabutoclax | <1 mg/mL | 100 mg/mL | 54 mg/mL |
| S7790 | A-1210477 | <1 mg/mL | 3 mg/mL | <1 mg/mL |
| S2448 | Gambogic Acid | <1 mg/mL | 100 mg/mL | 100 mg/mL |
| S8383 | S63845 | 100 mg/mL | ||
| S8177 | BH3I-1 | <1 mg/mL | 64 mg/mL | 13 mg/mL |
| S7800 | A-1155463 | <1 mg/mL | 80 mg/mL | <1 mg/mL |
| S7801 | A-1331852 | <1 mg/mL | 100 mg/mL | <1 mg/mL |
| S7531 | UMI-77 | <1 mg/mL | 93 mg/mL | 93 mg/mL |
| S7105 | BAM7 | <1 mg/mL | 2 mg/mL | <1 mg/mL |
| S1057 | Obatoclax Mesylate (GX15-070) | <1 mg/mL | 83 mg/mL | <1 mg/mL |
| S7849 | BDA-366 | <1 mg/mL | 84 mg/mL | 5 mg/mL |
| S7100 | WEHI-539 | -1 mg/mL | 100 mg/mL | -1 mg/mL |
| S7126 | Marinopyrrole A (Maritoclax) | <1 mg/mL | 100 mg/mL | 45 mg/mL |
| S8650 | BTSA1 | <1 mg/mL | 81 mg/mL | <1 mg/mL |
- Bcl-2抑制剂（21）
- 新Bcl-2产品
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1002 |
ABT-737ABT-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。 |
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. |
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| 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Ki分别为≤0.5 nM，≤1 nM和≤1 nM，但与Mcl-1和A1结合微弱。Phase 2。 |
KP cells (A) and A549 cells (B) were treated with increasing doses of ATN-224 alone or with the BCL2 inhibitor ABT-263, and cell death (96 hours) was determined.
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| S1121 |
TW-37TW-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Ki分别为0.29 μM， 1.11 μM和0.26 μM。 |
(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.
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| 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。 |
(b) MV4-11 cells were treated in vitro with ABT-199 (0.01, 0.1, 1 or 10 μM) with or without BL-8040 (20 μM) for 24 h in 1% FCS RPMI medium. The percentage of dead cells (PI+ cells) was evaluated by FACS. (c) miR-15a and miR-16-1 transfections were performed using Lipofectamine 2000 transfection reagent. At 72 h post-transfection, cells were stained with Annexin-V and PI. FACS plots and numerical data of % cells are shown. The results are expressed as the mean±s.d. and were analyzed using Student’s t-test (*P ⩽0.05 compared with control).
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| S8759New |
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。 |
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| S2812 |
AT101AT101，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Ki为0.32 μM，0.48 μM 和 0.18 μM；不抑制BIR3域和BID。Phase 2。 |
The cellular autophagy induced by the concentration of AT101 (5 μM) and APE1 siRNA was examined by confocal microscopy with the application of Cyto-IDr autophagy detection kit.
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| S1071 |
HA14-1HA14-1是一种Bcl-2表面口袋的非肽配体，IC50为9 μM左右。 |
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. |
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| S8061 |
SabutoclaxSabutoclax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。 |
(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.
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| S7790 |
A-1210477A-1210477是一种有效的选择性MCL-1抑制剂，Ki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。 |
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.
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| S2448 |
Gambogic AcidGambogic 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。 |
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| S8383 |
S63845S63845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。 |
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| S8177 |
BH3I-1BH3I-1是Bcl-XL-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。 |
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| S7800 |
A-1155463A-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。 |
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| S7801 |
A-1331852A-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。 |
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.
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| S7531 |
UMI-77UMI-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。 |
MCL-1 pharmacological inhibitor UMI-77 induces apoptosis of ESCC cells. a, b KYSE150 (a) and KYSE510 (b) cells were starved in 0.1% FBS/RPMI 1640 medium overnight and then cultured without (DMSO) or with different concentrations of UMI-77 in 10% FBS/RPMI 1640 medium for 48 h. After treatment, attached and floating cells were harvested. Cleavage of caspase-3 and PARP were analyzed by Western blotting. β-actin was used as a loading control. c KYSE150 and KYSE510 cells were starved in 0.1% FBS/RPMI 1640 medium overnight and then cultured without (DMSO) or with 10 μM UMI-77 in 10% FBS/RPMI 1640 medium for 48 h. After treatment, attached and floating cells were harvested. Cleavage of PARP was analyzed by Western blotting. β-actin was used as a loading control. Arrow head: 17KD or 19 KD of cleaved caspase-3
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| S7105 |
BAM7BAM7是一种直接的，选择性的促凋亡Bax激动剂，EC50为3.3 μM。 |
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| 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。 |
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.
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| S7849 |
BDA-366BDA-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。 |
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| S7100 |
WEHI-539WEHI-539对BCL-XL具有高亲和力（IC50=1.1 nM）和选择性，能有效地杀伤细胞。它对Bcl-XL的亲和性是对其他BCL-2家族成员的400倍。 |
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| 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。 |
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| S8650New |
BTSA1BTSA1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。 |
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