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Bcl-2
| 货号 | 产品名 | CAS号 | 信息 |
|---|---|---|---|
| CSN18313 | UMI-77 | 518303-20-3 | UMI-77 is a selective Mcl-1 SMI inhibitor, binding to the BH3 binding groove of Mcl-1 with Ki of 490 nM. |
| CSN19712 | S63845 | 1799633-27-4 | S63845 specifically binds with high affinity to the BH3-binding groove of MCL1. S63845 potently kills MCL1-dependent cancer cells, including multiple myeloma, leukaemia and lymphoma cells, by activating the BAX/BAK-dependent mitochondrial apoptotic pathway. |
| CSN14611 | Isochamaejasmine | 93859-63-3 | Isochamaejasmine, a natural product isolated and purified from the roots of Stellera chamaejasme Linn., has inhibition of NF-kappaB activation reversed the anti-apoptotic effect, shows antiplasmodial activity, with an IC(50) of 7.3+/-3.8 mM, but the selectivity was rather limited, and induces apoptosis in leukemia cells by inhibiting the activity of Bcl-2 family proteins, providing evidence for further studying the underlying anti-cancer mechanism of S. |
| CSN11133 | HA14-1 | 65673-63-4 | HA14-1 inhibits Bcl-2 with IC50 of ~9 μM by binding to the surface pocket and disturb the interaction of Bax/Bcl-2, it's cell-permeable. |
| CSN12617 | Gossypol | 303-45-7 | Gossypol has been known to exert a potential for anti-cancer, anti-inflammatory and other important therapeutic activities, gossypol binds and antagonizes anti-apoptotic effect of Bcl-2 family proteins |
| CSN13795 | Gambogic Acid | 2752-65-0 | Gambogic acid activates caspases with EC50 of 0.78-1.64 μM and competitively inhibits Bcl-XL, Bcl-2, Bcl-W, Bcl-B, Bfl-1 and Mcl-1 with IC50 of 1.47, 1.21, 2.02, 0.66, 1.06 and 0.79 μM, respectively. |
| CSN22317 | FX1 | 1426138-42-2 | FX1 is a BCL6 inhibitor that effectively blocks BCL6 N-terminal BTB domain-mediated corepressors chromosome recruitment (by 61-87%/SMRT and 67-82%/BCOR; 50 μM FX1 for 30 min) and selectively suppresses BCL6-depenent growth (GI50 16-54 μM; >125 μM against BCL6-independent cells) in diffuse large B cell lymphoma (DLBCL) cultures, exhibiting greater affinity than its structure analog 79-6 or BCL6 corepressor SMRT for BTB domain (KD = 7 μM/FX1, 30 μM/SMRT, 129 μM/79-6). FX1 shows greater efficacy than 79-6 in reversing BCL6/corepressors-mediated target genes repression in vitro (IC50 = 35 μM vs. 318 μM with 79-6 by HEK293T-based reporter assay) and in suppressing OCI-Ly7 DLBCL xenograft tumor growth mice in vivo (100% vs. 45% suppression with respective compound via 25 mg/kg/day i.p.). |
| CSN20561 | CID5721353 | 301356-95-6 | CID5721353 is a B-Cell Lymphoma 6 inhibitor (BCL6 inhibitor). |
| CSN23343 | BTSA1 | 314761-14-3 | BTSA1 is a BAX activator that binds to the N-terminal activation site with high affinity and specificity, induces conformational changes to BAX leading to BAX-mediated apoptosis. |
| CSN27381 | BT2 | 34576-94-8 | BT2 is a BCKDC kinase (BDK) inhibitor with an IC50 of 3.19 μM. BT2 binding to BDK triggers helix movements in the N-terminal domain, resulting in the dissociation of BDK from the branched-chain α-ketoacid dehydrogenase complex (BCKDC). BT2 (compound 4) is also a potent and selective Mcl-1 inhibitor with a Ki value of 59 μM. |
| CSN22358 | BI-3802 | 2166387-65-9 | BI-3802 is a highly potent BCL6 degrader, inhibiting the BTB domain of BCL6, with an IC50 of ≤3 nM; BI-3802 has antitumor activity. |
| CSN18193 | BH3I-1 | 300817-68-9 | BH3I-1 is an inhibitor of Bcl-xL with IC50 of 293.95 μM. |
| CSN18845 | BDA-366 | 1909226-00-1 | BDA-366 is a small-molecule Bcl2-BH4 domain antagonist and binds BH4 with high affinity and selectivity. |
| CSN18341 | Bax Inhibitor Peptide V5 | 579492-81-2 | Bax inhibitor peptide V5 is a Bax-mediated apoptosis inhibitor, used for cancer treatment. |
| CSN16589 | BAM7 | 331244-89-4 | BAM 7 is a direct and selective activator of proapoptotic Bax with EC50 of 3.3 μM. |
| CSN23881 | BAI1 | 335165-68-9 | BAI1 is an inhibitor of Bax-mediated mitochondrial cytochrome c release (IC50 = 0.52 μM). |
| CSN18551 | AT-101 | 90141-22-3 | AT101, the R-(-) enantiomer of Gossypol acetic acid, binds with Bcl-2, Bcl-xL and Mcl-1 with Ki of 0.32 μM, 0.48 μM and 0.18 μM. |
| CSN18501 | AT-101 Acetic Acid | 866541-93-7 | AT101 acetic acid, the R-(-) enantiomer of gossypol acetic acid, binds with Bcl-2, Bcl-xL and Mcl-1 with Ki of 0.32 μM, 0.48 μM and 0.18 μM. |
| CSN12426 | ABT-737 | 852808-04-9 | ABT-737 is a BH3 mimetic inhibitor of Bcl-xL, Bcl-2 and Bcl-w with EC50 of 78.7 nM, 30.3 nM and 197.8 nM, respectively, showing no inhibition observed against Mcl-1, Bcl-B or Bfl-1. |
| CSN16885 | A-1210477 | 1668553-26-1 | A-1210477 is a potent and selective inhibitor of MCL-1, and weakly binds to BCL-2 and BCL-XL, with Ki of 0.45 nM, 132 nM and > 660 nM, respectively. |
| CSN17536 | (S)-Gossypol Acetic Acid | 1189561-66-7 | (S)-Gossypol acetic acid is an inhibitor of Bcl-2, potently induce cell death in Jurkat cells overexpressing Bcl-2 (IC50, 18.1μM) or Bcl-xL (IC50, 22.9μM). |