Bcl-2 Inhibitors

Cat.No.	Product Name	Information	Product Use Citations
S8048	ABT-199 (Venetoclax)	Venetoclax (ABT-199, GDC-0199) is a Bcl-2-selective inhibitor with K_i of <0.01 nM in cell-free assays, >4800-fold more selective versus Bcl-xL and Bcl-w, and no activity to Mcl-1. Venetoclax is reported to induce cell growth suppression, apoptosis, cell cycle arrest, and autophagy in triple negative breast cancer MDA-MB-231 cells. Phase 3.	Cell, 2025, S0092-8674(25)00689-0 Cell, 2025, S0092-8674(25)01233-4 Signal Transduct Target Ther, 2025, 10(1):161
S1001	Navitoclax (ABT-263)	A potent inhibitor of Bcl-xL, Bcl-2 and Bcl-w with K_i of ≤ 0.5 nM, ≤1 nM and ≤1 nM in cell-free assays, Navitoclax (ABT-263) binds more weakly to Mcl-1 and A1. Phase 2.	Cell, 2025, S0092-8674(25)00689-0 Nat Cancer, 2025, 6(2):259-277 Nat Metab, 2025, 7(12):2474-2488.
S1002	ABT-737	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 in cell-free assays, respectively; no inhibition observed against Mcl-1, Bcl-B or Bfl-1. ABT-737 induces mitochondrial pathway apoptosis and mitophagy. Phase 2.	Signal Transduct Target Ther, 2025, 10(1):161 J Hepatol, 2025, S0168-8278(24)02830-7 Cell Rep Med, 2025, S2666-3791(25)00057-6
S8383	S63845	S63845 is a new, selective MCL-1 inhibitor with the Kd value of 0.19 nM and has no discernible binding to the other BCL-2 members, BCL-2 or BCL-XL.	Mol Cancer, 2025, 24(1):154 Nat Commun, 2025, 16(1):7853 Nat Commun, 2025, 16(1):4563
S7801	A-1331852	A-1331852 is a potent and selectiveBCL-XL inhibitor with Ki value less than 0.01 nM for BCL-XL and 6 nM, 4 nM, 142 nM for Bcl-2, Bcl-W, MCL-1 respectively. It may be useful in the treatment of cancer, immune and autoimmune diseases.	Cell, 2025, S0092-8674(25)00689-0 Mol Cancer, 2025, 24(1):154 Haematologica, 2025, 110(1):78-91
S7790	A-1210477	A-1210477 is a potent and selective MCL-1 inhibitor with K_i and IC50 of 0.454 nM and 26.2 nM, respectively, >100-fold selectivity over other Bcl-2 family members.	Front Pharmacol, 2025, 16:1530270 Cell Rep, 2023, 42(10):113176 Int J Mol Sci, 2023, 24(13)11149
S1121	TW-37	TW-37 is a novel nonpeptide inhibitor to recombinant Bcl-2, Bcl-xL and Mcl-1 with K_i of 0.29 μM, 1.11 μM and 0.26 μM in cell-free assays, respectively.	Signal Transduct Target Ther, 2025, 10(1):161 bioRxiv, 2024, 10.1101/2023.01.18.524628 Cells, 2023, 12(18)2247
S7800	A-1155463 Dihydrochloride	A-1155463 Dihydrochloride, a highly potent and selective BCL-XL inhibitor, shows picomolar binding affinity to BCL-XL, and >1000-fold weaker binding to BCL-2 and related proteins BCL-W(Ki=19 nM) and MCL-1(Ki>440 nM).	Front Pharmacol, 2025, 16:1530270 iScience, 2024, 27(1):108503 World J Oncol, 2024, 15(3):472-481
S8643	AZD5991	AZD5991 is a macrocyclic MCL-1 inhibitor with sub-nanomolar affinity for MCL-1 (Ki = 0.13 nM). The binding affinity of this compound is about 25-fold lower for mouse Mcl-1 vs. human Mcl-1 but only four-fold lower for rat Mcl-1.	Theranostics, 2025, 15(7):2834-2851 Theranostics, 2025, 15(12):5705-5718 Cell Death Differ, 2025, 10.1038/s41418-025-01514-7
S7531	UMI-77	UMI-77 is a selective Mcl-1 inhibitor with Ki of 490 nM, showing selectivity over other members of Bcl-2 family.	iScience, 2024, 27(1):108503 Blood, 2022, blood.2021014304 Nat Commun, 2022, 13(1):6226
S2812	(R)-(-)-Gossypol (AT-101) acetic acid	(R)-(-)-Gossypol (AT-101) acetic acid, the R-(-) enantiomer of Gossypol acetic acid, binds with Bcl-2, Bcl-xL and Mcl-1 with K_i of 0.32 μM, 0.48 μM and 0.18 μM in cell-free assays; does not inhibit BIR3 domain and BID. AT-101 simultaneously triggers apoptosis and a cytoprotective type of autophagy. Phase 2.	Protein Cell, 2024, pwad065 Int J Mol Sci, 2023, 24(7)6662 Leiden University The Netherlands, 2023,
E2926	A-1155463	A-1155463 is a highly potent and selective BCL-XL inhibitor with EC50 of 65 nM in H146 cells.	Nat Commun, 2025, 16(1):256 Cell Rep Med, 2025, 6(6):102160 Theranostics, 2025, 15(12):5705-5718
S8061	Sabutoclax	Sabutoclax (BI-97C1) 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.	Cells, 2023, 12(18)2247 Cells, 2023, 10.3390/cells12182247 Mol Divers, 2022, 10.1007/s11030-022-10494-6
S8836	MIK665 (S64315)	MIK665 (S64315) is an inhibitor of induced myeloid leukemia cell differentiation protein Mcl-1 with Ki value of 1.2 nM and has potential pro-apoptotic and antineoplastic activities.	Biochem Biophys Res Commun, 2025, 784:152650 Nat Commun, 2024, 15(1):1581 Cancer Biol Ther, 2024, 25(1):2427374
S1071	HA14-1	HA14-1 is a non-peptidic ligand of a Bcl-2 surface pocket with IC50 of ~9 μM.	Cell Rep, 2025, 44(5):115617 Platelets, 2020, 10.1080/09537104.2020.1724276 Oncotarget, 2018, 9(24):16701-16717
S8865	BAI1	BAI1 is a direct allosteric inhibitor of BAX with a dissociation constant (Kd) of 15.0 ± 4 μM.	Biomed Pharmacother, 2025, 187:118049 Int J Hyperthermia, 2024, 41(1):2325489 Nat Commun, 2023, 14(1):865
S2448	Gambogic Acid	Gambogic Acid (Guttatic Acid, Guttic Acid, Beta-Guttiferrin) activates caspases with EC50 of 0.78-1.64 μM and competitively inhibits Bcl-X_L, 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.	Theranostics, 2025, 15(11):5420-5439 Cells, 2023, 12(18)2247 Cells, 2023, 10.3390/cells12182247
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 this compound for BCL-2 versus BCL-XL ranges from ~70 to 400 folds.	Cells, 2023, 12(18)2247 Cells, 2023, 10.3390/cells12182247 Signal Transduct Target Ther, 2022, 7(1):51
S8758	VU661013	VU661013 is a novel, potent, selective MCL1 inhibitor with Ki of 97 ± 30 pM of human MCL-1 in a TR-FRET assay. However, this compound does not significantly inhibit BCL-xL or BCL-2 with Ki > 40 μM or = 0.73 μM. It de-stabilizes BIM/MCL-1 association, leads to apoptosis in AML.	Gastric Cancer, 2025, 10.1007/s10120-025-01630-w
S9970	APG-2575 (lisaftoclax)	APG-2575 (lisaftoclax) is a dual Bcl-2 and Bcl-xl inhibitor with IC50 values of 2 nM and 5.9 nM for Bcl-2 and Bcl-xl, respectively.
E8278^New	WH244	WH244 is a second-generation PROTAC that selectively degrades the anti-apoptotic proteins BCL-xL and BCL-2 with a DC50 of 0.6 nM for BCL-xL and 7.4 nM for BCL-2.
S3243	Zeaxanthin	Zeaxanthin, the carotenoid alcohol participates in the xanthophyll cycle, activates the extrinsic apoptosis pathway which induces apoptosis on uveal melanoma cells with IC50 value 40.8 µM.
E0011	Linderalactone	Linderalactone inhibits human lung cancer growth by modulating the expression of apoptosis-related proteins (Bax and Bcl-2) with an IC50 of 15 µM in A-549 cells. This compound induces G2/M cell cycle arrest and could also suppress the JAK/STAT signalling pathway. It can be isolated from Radix linderae.
E1510	Sonrotoclax	Sonrotoclax(BGB-11417) is a highly potent, orally active and selective inhibitor of Bcl2. This compound demonstrates increased potency along with in vitro and in vivo inhibitory activity against both WT Bcl-2 and the G101V mutant. Bcl-xL It has effective cell killing effect against a variety of lymphoma and leukemia cell lines.
S5600	Flavokawain A	Flavokawain A, extracted from kava, is an apoptotic inducers and anticarcinogenic agent. This compound can down-regulation of antiapoptotic proteins, such as XIAP, survivin, and Bcl-xL, thereby changing the balance between apoptotic and antiapoptotic molecules and then induce cell death in tumor cells.
S8177	BH3I-1	BH3I-1 is a Bcl-X_L-BH3 domain interaction inhibitor with Ki of 2.4 μM (by fluorescence polarization ).This compound is a selective inhibitor of Bcl-2 family proteins.
S6004	CCI-007	CCI-007 is a novel small molecule with cytotoxic activity against infant leukemia with MLL rearrangements.
S8550	Tapotoclax (AMG-176)	Tapotoclax (AMG-176) is a potent, selective, and orally bioavailable macrocyclic inhibitor of MCL1 with a Ki of 0.13 nM. It induces a potent apoptosis in models of hematologic malignancies.
E2663	BT2	BT2 is a novel branched-chain α-ketoacid dehydrogenase complex kinase (BDK) inhibitor wieh an IC50 of 3.19 μM.
E5962^New	BRD-810	BRD-810 is a potent and highly selective inhibitor of MCL1. BRD-810 targets the BH3-binding pocket of MCL1 and blocks the capturing of pro-apoptotic proteins, thereby rapidly triggering caspase activation in MCL1-dependent cells. It demonstrates potent anti-tumor effects in both hematologic malignancies and solid tumor models.
E3020	Hedyotic Diffusa Extract	Hedyotic Diffusa Extract is extracted from Hedyotic diffusa, of which polysaccharides inhibit the growth of CNE2 cells in a dose-and-time-dependent way, the mechanism may involve induction of cell apoptosis, which is associated with the activation of Bax and caspase-3 protein and the down-regulation of Bcl-2 protein expression.
S2606	Mifepristone (RU-486)	Mifepristone is a remarkably active antagonist of progesterone receptor and glucocorticoid receptor with IC50 of 0.2 nM and 2.6 nM, respectively. Mifepristone promotes cell autophagy and apoptosis, decreases Bcl-2 level and increases Beclin1 level, accompanied by weakened interaction between Bcl-2 and Beclin1.Mifepristone (RU486) can be used to induce animal models of Spontaneous Abortion.	Pharmacol Res, 2025, 215:107696 Cell Death Dis, 2025, 16(1):237 J Virol, 2025, 99(2):e0147224
S2271	Berberine chloride	Berberine chloride is a quaternary ammonium salt from the group of isoquinoline alkaloids. This compound activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. It decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. This chemical induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. It is a dual topoisomerase I and II inhibitor. It is also a potential autophagy modulator.	J Cardiovasc Dev Dis, 2025, 12(7)278 Adv Healthc Mater, 2023, e2300591. Transl Oncol, 2023, 35:101712
S8820	Unesbulin (PTC596)	Unesbulin (PTC596) is a second-generation BMI-1 inhibitor that accelerates BMI-1 degradation. This compound downregulates MCL-1 and induces p53-independent mitochondrial apoptosis. IC50 values at 72 hours ranged from 68 to 340 nM in mantle cell lymphoma (MCL) cell lines.	Cell Rep Med, 2025, S2666-3791(25)00150-8 NPJ Precis Oncol, 2024, 8(1):68 PLoS One, 2023, 18(2):e0277313
S6852	Gossypol	Gossypol (BL 193) is an orally-active polyphenol isolated from cotton seeds and roots. This compound 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. It 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. This chemical induces apoptosis and cell growth inhibition in various cancer cells.	iScience, 2024, 27(10):110862 Cells, 2023, 12(18)2247 Cells, 2023, 10.3390/cells12182247
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 the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator.	Front Biosci (Landmark Ed), 2022, 27(8):242 Front Pharmacol, 2021, 12:632201
S9665	Motixafortide (BL-8040, BKT140)	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.	King's College London, 2023,
E0124	Chelerythrine	Chelerythrine (Toddaline, Broussonpapyrine) is a potent, selective antagonist of PKC with an IC50 of 0.66 μM. This compound also inhibits the BclXL-Bak BH3 peptide binding with an IC50 of 1.5 μM. It shows antitumor, antidiabetic and anti-inflammatory activity.	Nutr Neurosci, 2022, 1-19
S3224	Cinobufagin	Cinobufagin (Cinobufagine), an active ingredient of Venenum Bufonis, inhibits tumor development. This compound increases ATM and Chk2 and decreases CDC25C, CDK1, and cyclin B. It inhibits PI3K, AKT and Bcl-2 while increases levels of cleaved caspase-9 and caspase-3. Thus, this chemical induces cell cycle arrest at the G2/M phase and apoptosis.
S6895	TCPOBOP	TCPOBOP is a constitutive androstane receptor (CAR) agonist. This compound attenuates Fas-induced murine liver injury by altering Bcl-2 proteins.
E2354	Valepotriate	Valepotriate, an unstable iridoid isolated from Valeriana jatamansi Jones, has anti-epileptic by significantly increasing the expression of GABA_A, glutamic acid decarboxylase 65, and Bcl-2 and reduce the expression of caspase-3.