Bcl-2
| 货号 | 产品名 | CAS号 | 信息 |
|---|---|---|---|
| FB03218 | WEHI-539 | 1431866-33-9 | WEHI-539 is a selective inhibitor of Bcl-XL with IC50 of 1.1 nM. |
| FB10026 | WEHI-539 HCl | 2070018-33-4 | WEHI-539 HCl is a selective inhibitor of Bcl-XL with IC50 of 1.1 nM. |
| FB06172 | 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. |
| FB04421 | TW-37 | 877877-35-5 | TW-37 is a nonpeptide inhibitor to recombinant Bcl-2, Bcl-xL and Mcl-1 with Ki of 0.29 μM, 1.11 μM and 0.26 μM, respectively. |
| FB12656 | SMBA 1 | 906440-37-7 | SMBA1 is a selective activator of Bax, a central death regulator. It acts by potently suppressing lung tumour growth via apoptosis. |
| FB17707 | SAH-MS1-18 | 2241745-49-1 | SAH-MS1-18 is a Mcl-1–targeting stapled peptide with IC50 value of 25nM. It engages Mcl-1 in a distinctive binding mode, selectively activates caspase 3/7 in Mcl-1–dependent cancer cells and dissociates Mcl-1/Bak complexes. |
| FB10215 | Sabutoclax | 1228108-65-3 | Sabutoclax is a pan-Bcl-2 inhibitor, including Bcl-xL, Bcl-2, Mcl-1 and Bfl-1 with IC50 of 0.31 μM, 0.32 μM, 0.20 μM and 0.62 μM, respectively. |
| FB10918 | 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. |
| FB10025 | Pyridoclax | 1651890-44-6 | Pyridoclax is a potent Mcl-1 inhibitor with Kd value of 25 nM. |
| FB07790 | Obatoclax | 803712-67-6 | Obatoclax, a Bcl-2 homology domain-3 mimetic, antagonize all antiapoptotic Bcl-2 family proteins (average IC50, 3 μMol/L), including Mcl-1 (IC50, 2.9 μMol/L) and Bfl-1 (IC50, 5 μMol/L). |
| FB15279 | AML311 | 315698-17-0 | ML311, also known as EU-5346, is a selective inhibitor of the interaction of Mcl-1 and Bim. |
| FB06167 | MIM1 | 509102-00-5 | MIM1 is a selective small molecule inhibitor of Mcl-1(IC50= 4.8 uM) that overcomes Mcl-1-dependent leukemia cell survival. |
| FB11542 | MIK 665 | 1799631-75-6 | MIK665 is an inhibitor of induced myeloid leukemia cell differentiation protein (Mcl-1; Bcl2-L-3), with potential pro-apoptotic and antineoplastic activities. |
| FB12053 | Mcl1-IN-4 | 1580484-04-3 | Mcl1-IN-4 is an inhibitor of Mcl1 with an IC50 of 0.2 μM. |
| FB12052 | Mcl1-IN-3 | 1814891-79-6 | Mcl1-IN-3 is an inhibitor of Mcl1 extracted from patent WO2015153959A2, compound example 57; has an IC50 and Ki of 0.67 and 0.13 μM, respectively. |
| FB04866 | Mcl1-IN-2 | 292057-76-2 | Mcl1-IN-2 is a Mcl-1 inhibitor without reported IC50 value. |
| FB06257 | Mcl1-IN-1 | 713492-66-1 | Mcl1-IN-1 is a potent Mcl-1-selective inhibitor relative to the related Bcl-2 family protein Bcl-xL and demonstrates good Mcl-1 inhibition (IC50 = 2.4 uM) with no appreciable inhibition of Bcl-xL at 100 uM. |
| FB02384 | Marinopyrrole A | 1227962-62-0 | Marinopyrrole A is a selective Mcl-1 inhibitor with IC50 of 10.1 μM and proapoptosis properties in some cancer cells. |
| FB05173 | 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. |
| FB02208 | 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. |
| FB08033 | 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 |
| FB09787 | 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. |
| FB11929 | 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.). |
| FB10911 | CID5721353 | 301356-95-6 | CID5721353 is a B-Cell Lymphoma 6 inhibitor (BCL6 inhibitor). |
| FB12836 | 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. |
| FB17815 | 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. |
| FB17717 | BIM SAHBA | 1403993-87-2 | BIM SAHBA is a hydrocarbon-stapled peptide modeled after the BIM BH3 helix broadly. It targeted BCL-2 family proteins (with Kd values of 3.2, 10.7, 2.7 and 1.4nM for affinity to Bcl-xL, Mcl-1, Bcl-w and Bfl-1, respectively), blocked inhibitory antiapoptotic interactions, directly triggered proapoptotic activity, and induced dose-responsive and BH3 sequence–specific cell death of hematologic cancer cells. |
| FB17716 | Bim BH3 peptide 19 | 2346598-16-9 | Bim BH3 peptide 19 is a Bim BH3 mimetic, platelet-permeable, stapled peptide which confirms the part of Bim in phosphatidyl-serine (PS) exposure and is able to engage with Bcl-xL protein (relative KDapp 7.3 and 26 nM, respectively). |
| FB17714 | Bim BH3 | 1403836-51-0 | BIM BH3 is a peptide which could insert into the BIM protein and could rescue the leukocyte accumulation and autoimmune phenotype of Bim–/– mice. |
| FB11815 | BI-3812 | 2166387-64-8 | BI-3812 is a BCL6 inhibitor, inhibiting the BTB domain of BCL6, with an IC50 of ≤3 nM. |
| FB11969 | 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. |
| FB04873 | BH3I-1 | 300817-68-9 | BH3I-1 is an inhibitor of Bcl-xL with IC50 of 293.95 μM. |
| FB10762 | BDA-366 | 1909226-00-1 | BDA-366 is a small-molecule Bcl2-BH4 domain antagonist and binds BH4 with high affinity and selectivity. |
| FB17739 | BCL6-IN-5 | 2253878-09-8 | BCL6-IN-5 is a potent BCL6 inhibitor exacted from patent WO2018215801A1 with pIC50 of 5.82. |
| FB06198 | Bax Inhibitor Peptide V5 | 579492-81-2 | Bax inhibitor peptide V5 is a Bax-mediated apoptosis inhibitor, used for cancer treatment. |
| FB15296 | Bax channel blocker | 329349-20-4 | Bax channel blocker inhibits Bax-mediated mitochondrial cytochrome c release with IC50 of 0.52 μM. |
| FB08541 | BAM7 | 331244-89-4 | BAM 7 is a direct and selective activator of proapoptotic Bax with EC50 of 3.3 μM. |
| FB15394 | BAI1 | 335165-68-9 | BAI1 is an inhibitor of Bax-mediated mitochondrial cytochrome c release (IC50 = 0.52 μM). |
| FB11560 | AZD5991 | 2143061-81-6 | AZD5991 is a potent and selective Mcl-1 inhibitor for treatment of hematologic cancers （a phase I trial of Haematological malignancies）. |
| FB06921 | 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. |
| FB06872 | 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. |
| FB00618 | Apogossypolone | 886578-07-0 | Apogossypolone is an inhibitor of Bcl-2, Mcl-1 and Bcl-XL with Ki values of 35nM, 25nM and 660nM, respectively. |
| FB11323 | AMG-176 | 1883727-34-1 | AMG-176 is an inhibitor of induced myeloid leukemia cell differentiation protein MCL-1 (myeloid cell leukemia-1), with potential pro-apoptotic and antineoplastic activities. |
| FB05363 | 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. |
| FB09559 | ABT-263 | 923564-51-6 | ABT-263 is a potent inhibitor of Bcl-xL, Bcl-2 and Bcl-w with Ki of ≤ 0.5 nM, ≤1 nM and ≤1 nM in cell-free assays, but binds more weakly to Mcl-1 and A1. |
| FB07570 | ABT-199 | 1257044-40-8 | ABT-199 is a Bcl-2-selective inhibitor with Ki of < 0.01 nM, > 4800-fold selective versus Bcl-xL and Bcl-w, and showing no activity to Mcl-1. |
| FB02397 | A-1155463 | 1235034-55-5 | A1155463 is a highly potent and selective BCL-XL inhibitor with an EC50 value of 70 nM in Molt-4 cell. |
| FB01477 | 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. |
| FB02329 | (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). |
| FB06232 | (+)-Apogossypol | 66389-74-0 | (+)-Apogossypol is a potent inhibitor of Bcl-2 family proteins and competes with the BH3 peptide-binding sites on Bcl-2, Bcl-XL, Mcl-1, Bcl-W, and Bcl-B, but not Bfl-1, with IC50s of 0.5 to 2 μM. |