Bcl-2

シグナル伝達経路

研究分野

阻害剤の選択性比較

カタログ番号	製品カタログ	溶解度(25°C)
カタログ番号	製品カタログ	水	DMSO	アルコール
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)	<1 mg/mL	100 mg/mL	'<1 mg/mL
S3245	Nodakenetin	-1 mg/mL	100 mg/mL	-1 mg/mL
S3267	Kaempferol-3-O-rutinoside	-1 mg/mL	100 mg/mL	-1 mg/mL
S6852	Gossypol	<1 mg/mL	100 mg/mL	8 mg/mL
S8924	DT2216			' mg/mL
S8758	VU661013	<1 mg/mL	100 mg/mL	<1 mg/mL
S2812	(R)-(-)-Gossypol acetic acid	<1 mg/mL	116 mg/mL	''''89 mg/mL
S1071	HA14-1	<1 mg/mL	82 mg/mL	82 mg/mL
S2606	Mifepristone	<1 mg/mL	85 mg/mL	19 mg/mL
S8061	Sabutoclax	<1 mg/mL	100 mg/mL	54 mg/mL
S8820	PTC596	<1 mg/mL	84 mg/mL	7 mg/mL
S8643	AZD5991	<1 mg/mL	100 mg/mL	<1 mg/mL
S7790	A-1210477	<1 mg/mL	3 mg/mL	<1 mg/mL
S8759	S55746	<1 mg/mL	100 mg/mL	<1 mg/mL
S2271	Berberine chloride	<1 mg/mL	40 mg/mL	<1 mg/mL
S2448	Gambogic Acid	<1 mg/mL	100 mg/mL	100 mg/mL
S8383	S63845	<1 mg/mL	100 mg/mL	<1 mg/mL
S5600	Flavokawain A	-1 mg/mL	32 mg/mL	-1 mg/mL
S8177	BH3I-1	<1 mg/mL	64 mg/mL	13 mg/mL
S8865	BAI1	<1 mg/mL	18 mg/mL	3 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
S8836	S64315 (MIK665)	<1 mg/mL	100 mg/mL	''-1 mg/mL
S3224	Cinobufagin	-1 mg/mL	100 mg/mL	-1 mg/mL
S3238	Resibufogenin	-1 mg/mL	100 mg/mL	-1 mg/mL
S3275	Senkyunolide I	-1 mg/mL	100 mg/mL	-1 mg/mL
S7105	BAM7	<1 mg/mL	2 mg/mL	<1 mg/mL
S8650	BTSA1	<1 mg/mL	81 mg/mL	<1 mg/mL
S7747	Ro-3306	<1 mg/mL	13 mg/mL	''<1 mg/mL
S9276	Alisol B	-1 mg/mL	95 mg/mL	-1 mg/mL
S5550	Ethyl gallate	-1 mg/mL	39 mg/mL	-1 mg/mL
S1057	Obatoclax Mesylate (GX15-070)	<1 mg/mL	83 mg/mL	<1 mg/mL
S9665	Motixafortide (BL-8040)	100 mg/mL	-1 mg/mL	'-1 mg/mL
S7100	WEHI-539 HCl	-1 mg/mL	100 mg/mL	'''''-1 mg/mL
S7849	BDA-366	<1 mg/mL	84 mg/mL	5 mg/mL
S7126	Marinopyrrole A (Maritoclax)	<1 mg/mL	100 mg/mL	45 mg/mL
S8199	LTX-315 (Ruxotemitide)	100 mg/mL	-1 mg/mL	''-1 mg/mL

亜型選択性的な製品

Bcl-2製品

All (41) Bcl-2阻害剤(27) Bcl-2活性剤(8) Bcl-2拮抗剤(5) Bcl-2モジュレータ(1)

製品コード	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
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.	ACS Nano, 2020, 14(3):3378-3388 Sci Adv, 2020, 6(47)eabc3465 Nat Commun, 2020, 11(1):259	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) is 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, but binds more weakly to Mcl-1 and A1. Phase 2.	Nat Cell Biol, 2020, 4 Sci Transl Med, 2020, 15;12(539) pii: eaax3799 Cell Res, 2020, 27;1-16
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.	Platelets, 2020, 10.1080/09537104.2020.1724276 NPJ Breast Cancer, 2020, 6:30 BMC Cancer, 2019, 19(1):243	(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) 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.	Nat Genet, 2020, 52(4):408-417 Mol Cell, 2020, 7;S1097-2765(20)30269-0 Nat Commun, 2020, 11(1):752	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.
S3245^新	Nodakenetin Nodakenetin (NANI), a plant-derived coumarin isolated from Angelica decursiva, inhibits α-glucosidase, PTP1B, rat lens aldose reductase (RLAR), AChE, BChE, and β-site amyloid precursor protein cleaving enzyme 1 (BACE1). Nodakenetin alters the protein expression of Bax and Bcl-2, and prompts mitochondrial apoptosis. Nodakenetin exhibits anti-tumor activity.
S3267^新	Kaempferol-3-O-rutinoside Kaempferol-3-O-rutinoside (Nicotiflorin, Nikotoflorin, Kaempferol 3-O-β-rutinoside), a flavonoid extracted from Carthamus tinctorius, alters the shape and structure of injured neurons, decreases the number of apoptotic cells, down-regulates expression of p-JAK2, p-STAT3, caspase-3, and Bax and decreases Bax immunoredactivity, and increases Bcl-2 protein expression and immunoreactivity.
S6852^新	Gossypol Gossypol (BL 193) is an orally-active polyphenol isolated from cotton seeds and roots. Gossypol 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. Gossypol 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. Gossypol induces apoptosis and cell growth inhibition in various cancer cells.	Mol Med Rep, 2021, 23(1)40 J Biol Chem, 2015, 290(34):20841-55
S8924^新	DT2216 DT2216 is a potent and selective degrader of BCL-XL based on PROTAC technology. DT2216 inhibits various BCL-XL-dependent leukemia and cancer cells but considerably less toxic to platelets.
S8758^新	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, VU661013 does not significantly inhibit BCL-xL or BCL-2 with Ki > 40 μM or = 0.73 μM. VU661013 de-stabilizes BIM/MCL-1 association, leads to apoptosis in AML.
S2812	(R)-(-)-Gossypol 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.	Eur J Pharm Sci, 2020, 142:105105 Platelets, 2020, 10.1080/09537104.2020.1724276 Cancers (Basel), 2020, 12(8):E2298	(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 is a non-peptidic ligand of a Bcl-2 surface pocket with IC50 of ~9 μM.	Platelets, 2020, 10.1080/09537104.2020.1724276 Oncotarget, 2018, 9(24):16701-16717 Biochem Biophys Res Commun, 2015, 463(4):870-5	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.
S2606	Mifepristone Mifepristone (RU486, C-1073) 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.	Proc Natl Acad Sci U S A, 2020, 202021450 Cell Death Discov, 2020, 20;6:24 Sci Rep, 2020, 24;10(1):5363	Myogenic differentiation assay to determine the GR specificity of DEX by using RU-486 (10 uM). Immunofluorescence detection of MyHC (red) and DAPI counterstaining of nuclei (blue) was used to detect myotubes. The scale bar is 50 um.
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.	Platelets, 2020, 10.1080/09537104.2020.1724276 Am J Respir Crit Care Med, 2019, 200(1):84-97 PLoS Pathog, 2018, 14(6):e1007100	(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.
S8820	PTC596 PTC596 is a second-generation BMI-1 inhibitor that accelerates BMI-1 degradation. PTC596 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.
S8643	AZD5991 AZD5991 is a macrocyclic MCL-1 inhibitor with sub-nanomolar affinity for MCL-1 (Ki = 0.13 nM). The binding affinity of AZD5991 is about 25-fold lower for mouse Mcl-1 vs. human Mcl-1 but only four-fold lower for rat Mcl-1.	Nat Cell Biol, 2020, 4 Mol Cancer Ther, 2020, 19(10):2001-2011 Cancer Cell, 2020, 38(6):872-890.e6
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.	Cell Rep, 2020, 31(12):107800 Cell Death Dis, 2020, 5;11(5):316 Cell Death Dis, 2020, 11(11):946	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.
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 S55746 for BCL-2 versus BCL-XL ranges from ~70 to 400 folds.
S2271	Berberine chloride Berberine chloride 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.	Oncol Rep, 2018, 40(3):1525-1532 Shandong University, 2014, Haoran Cui
S2448	Gambogic Acid Gambogic Acid (Guttatic, Guttic) 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.	Clin Cancer Res, 2019, 10.1158/1078-0432.CCR-19-0775
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.	Blood, 2020, 12;blood.2020006075 Sci Adv, 2020, 6(47)eabc3465 Nat Commun, 2020, 11(1):259
S5600	Flavokawain A Flavokawain A, extracted from kava, is an apoptotic inducers and anticarcinogenic agent. Flavokawain A 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 ).It is a selective inhibitor of Bcl-2 family proteins.
S8865	BAI1 BAI1 is a direct allosteric inhibitor of BAX with a dissociation constant (Kd) of 15.0 ± 4 μM.
S7800	A-1155463 A-1155463, 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).	Oncol Rep, 2020, 44(3):927-938 Cell Rep, 2020, 32(1):107845 Cancers (Basel), 2020, 12(6):1694	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 is a potent and selectiveBCL-XL inhibitor and may be useful in the treatment of cancer, immune and autoimmune diseases.	Cancers (Basel), 2020, 12(2) Cell Death Dis, 2020, 8;11(6):443 Cell Death Dis, 2020, 11(10):875	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 is a selective Mcl-1 inhibitor with Ki of 490 nM, showing selectivity over other members of Bcl-2 family.	Mol Cancer Ther, 2020, 19(10):2001-2011 Cancers (Basel), 2020, 12(8):E2298 Int J Radiat Oncol Biol Phys, 2020, 15;106(4):867-877	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.
S8836	S64315 (MIK665) S64315 (MIK665) 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.	Cell Death Dis, 2020, 8;11(6):443 Blood Adv, 2020, 4(5):819-829 Cancers (Basel), 2020, 12(8):E2182
S3224^新	Cinobufagin Cinobufagin (Cinobufagine), an active ingredient of Venenum Bufonis, inhibits tumor development. Cinobufagin increases ATM and Chk2 and decreases CDC25C, CDK1, and cyclin B. Cinobufagin inhibits PI3K, AKT and Bcl-2 while increases levels of cleaved caspase-9 and caspase-3. Thus, Cinobufagin induces cell cycle arrest at the G2/M phase and apoptosis.
S3238^新	Resibufogenin Resibufogenin (Bufogenin, Recibufogenin), a component of huachansu with anticancer effect, triggers necroptosis through upregulating receptor-interacting protein kinase 3 (RIP3) and phosphorylating mixed lineage kinase domain-like protein at Ser358. Resibufogenin exerts cytotoxic effect by inducing reactive oxygen species (ROS) accumulation. Resibufogenin induces apoptosis and caspase-3 and caspase-8 activity. Resibufogenin increases Bax/Bcl-2 expression, and suppresses cyclin D1, cyclin E, PI3K, p-AKT, p-GSK3β and β-catenin protein expression.
S3275^新	Senkyunolide I Senkyunolide I (SEI, SENI) is an orally active compound isolated from Ligusticum chuanxiong with analgesic, anti-migraine, neuroprotective, anti-oxidation and anti-apoptosis activities. Senkyunolide I (SEI, SENI) up-regulates the phosphorylation of Erk1/2 and induces Nrf2 nuclear translocation with enhanced HO-1 and NQO1 expressions. Senkyunolide I (SEI, SENI) promotes the ratio of Bcl-2/Bax and inhibits the expressions of cleaved caspase 3 and caspase 9.
S7105	BAM7 BAM 7 is a direct and selective activator of proapoptotic Bax with EC50 of 3.3 μM.	Nat Chem Biol, 2019, 15(4):322-330 Cell Death Discov, 2018, 4:107
S8650	BTSA1 BTSA1 is a pharmacologically optimized BAX activator that binds with high affinity and specificity to the N-terminal activation site and induces conformational changes to BAX leading to BAX-mediated apoptosis. It effectively promotes apoptosis in leukemia cell lines and patient samples while sparing healthy cells.
S7747	Ro-3306 RO-3306 is an ATP-competitive, and selective CDK1 inhibitor with K_i of 20 nM, >15-fold selectivity against a diverse panel of human kinases. RO-3306 enhances p53-mediated Bax activation and mitochondrial apoptosis.	Cell Res, 2020, 10.1038/s41422-020-0357-y Mol Cell, 2020, 22 pii: S1097-2765(20)30231-8 Nat Commun, 2020, 11(1):4338	HeLa cells were untreated or treated with either colcemid (10 μg/ml for 16 h), RO-3306 (9 μM for 16 h), or both colcemid and RO-3306, as indicated. Cells were then lysed, and proteins were detected by Western analysis.
S9276	Alisol B Alisol B, a triterpene from Alismatis rhizoma, induces Bax up-regulation and nuclear translocation, the activation of initiator caspase-8 and caspase-9, and executor caspase-3, suggesting the involvement of both extrinsic and intrinsic apoptosis pathways.
S5550	Ethyl gallate Ethyl gallat (Phyllemblin, gallic acid ethyl ester), which could be found naturally in a variety of plant sources, is a food additive with antimicrobial activity
S1057	Obatoclax Mesylate (GX15-070) Obatoclax Mesylate (GX15-070) is an antagonist of Bcl-2 with K_i of 0.22 μM in a cell-free assay, can assist in overcoming MCL-1 mediated resistance to apoptosis. Phase 3.	Biomaterials, 2020, 232:119709 Int J Mol Sci, 2020, 5;21(5) pii: E1773 Invest New Drugs, 2020, 4	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.
S9665^新	Motixafortide (BL-8040) 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.
S7100^新	WEHI-539 HCl WEHI-539 HCl (WEHI-539 hydrochloride) has high affinity (IC50=1.1 nM) and selectivity for BCL-XL and potently kills cells by selectively antagonizing its prosurvival activity. It has more than a 400-fold higher affinity for BCL-XL versus other prosurvival BCL-2 family members.	Mol Pharmacol, 2019, 96(4):419-429 J Immunol, 2018, 200(5):1727-1736 Cell Death Differ, 2015, 22(12):2098-106
S7849	BDA-366 BDA-366 is a small-molecule Bcl2-BH4 domain antagonist and binds BH4 with high affinity and selectivity.
S7126	Marinopyrrole A (Maritoclax) Marinopyrrole A (Maritoclax) is a selective Mcl-1 antagonist. It binds to Mcl-1, but not Bcl-XL, and targets Mcl-1 for proteasomal degradation. Maritoclax disrupts the interaction between Bim and Mcl-1 with an IC50 of 10.1 μM.	Leukemia, 2019, 33(2):319-332 Molecules, 2018, 23(11)E3030
S8199	LTX-315 (Ruxotemitide) LTX-315 (Ruxotemitide, Oncopore) is the oncolytic peptide that kills cancer cells through Bax/Bak-regulated mitochondrial membrane permeabilization.

製品コード	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
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.	ACS Nano, 2020, 14(3):3378-3388 Sci Adv, 2020, 6(47)eabc3465 Nat Commun, 2020, 11(1):259	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) is 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, but binds more weakly to Mcl-1 and A1. Phase 2.	Nat Cell Biol, 2020, 4 Sci Transl Med, 2020, 15;12(539) pii: eaax3799 Cell Res, 2020, 27;1-16
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.	Platelets, 2020, 10.1080/09537104.2020.1724276 NPJ Breast Cancer, 2020, 6:30 BMC Cancer, 2019, 19(1):243	(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) 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.	Nat Genet, 2020, 52(4):408-417 Mol Cell, 2020, 7;S1097-2765(20)30269-0 Nat Commun, 2020, 11(1):752	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.
S3245^新	Nodakenetin Nodakenetin (NANI), a plant-derived coumarin isolated from Angelica decursiva, inhibits α-glucosidase, PTP1B, rat lens aldose reductase (RLAR), AChE, BChE, and β-site amyloid precursor protein cleaving enzyme 1 (BACE1). Nodakenetin alters the protein expression of Bax and Bcl-2, and prompts mitochondrial apoptosis. Nodakenetin exhibits anti-tumor activity.
S3267^新	Kaempferol-3-O-rutinoside Kaempferol-3-O-rutinoside (Nicotiflorin, Nikotoflorin, Kaempferol 3-O-β-rutinoside), a flavonoid extracted from Carthamus tinctorius, alters the shape and structure of injured neurons, decreases the number of apoptotic cells, down-regulates expression of p-JAK2, p-STAT3, caspase-3, and Bax and decreases Bax immunoredactivity, and increases Bcl-2 protein expression and immunoreactivity.
S6852^新	Gossypol Gossypol (BL 193) is an orally-active polyphenol isolated from cotton seeds and roots. Gossypol 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. Gossypol 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. Gossypol induces apoptosis and cell growth inhibition in various cancer cells.	Mol Med Rep, 2021, 23(1)40 J Biol Chem, 2015, 290(34):20841-55
S8924^新	DT2216 DT2216 is a potent and selective degrader of BCL-XL based on PROTAC technology. DT2216 inhibits various BCL-XL-dependent leukemia and cancer cells but considerably less toxic to platelets.
S8758^新	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, VU661013 does not significantly inhibit BCL-xL or BCL-2 with Ki > 40 μM or = 0.73 μM. VU661013 de-stabilizes BIM/MCL-1 association, leads to apoptosis in AML.
S2812	(R)-(-)-Gossypol 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.	Eur J Pharm Sci, 2020, 142:105105 Platelets, 2020, 10.1080/09537104.2020.1724276 Cancers (Basel), 2020, 12(8):E2298	(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 is a non-peptidic ligand of a Bcl-2 surface pocket with IC50 of ~9 μM.	Platelets, 2020, 10.1080/09537104.2020.1724276 Oncotarget, 2018, 9(24):16701-16717 Biochem Biophys Res Commun, 2015, 463(4):870-5	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.
S2606	Mifepristone Mifepristone (RU486, C-1073) 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.	Proc Natl Acad Sci U S A, 2020, 202021450 Cell Death Discov, 2020, 20;6:24 Sci Rep, 2020, 24;10(1):5363	Myogenic differentiation assay to determine the GR specificity of DEX by using RU-486 (10 uM). Immunofluorescence detection of MyHC (red) and DAPI counterstaining of nuclei (blue) was used to detect myotubes. The scale bar is 50 um.
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.	Platelets, 2020, 10.1080/09537104.2020.1724276 Am J Respir Crit Care Med, 2019, 200(1):84-97 PLoS Pathog, 2018, 14(6):e1007100	(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.
S8820	PTC596 PTC596 is a second-generation BMI-1 inhibitor that accelerates BMI-1 degradation. PTC596 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.
S8643	AZD5991 AZD5991 is a macrocyclic MCL-1 inhibitor with sub-nanomolar affinity for MCL-1 (Ki = 0.13 nM). The binding affinity of AZD5991 is about 25-fold lower for mouse Mcl-1 vs. human Mcl-1 but only four-fold lower for rat Mcl-1.	Nat Cell Biol, 2020, 4 Mol Cancer Ther, 2020, 19(10):2001-2011 Cancer Cell, 2020, 38(6):872-890.e6
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.	Cell Rep, 2020, 31(12):107800 Cell Death Dis, 2020, 5;11(5):316 Cell Death Dis, 2020, 11(11):946	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.
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 S55746 for BCL-2 versus BCL-XL ranges from ~70 to 400 folds.
S2271	Berberine chloride Berberine chloride 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.	Oncol Rep, 2018, 40(3):1525-1532 Shandong University, 2014, Haoran Cui
S2448	Gambogic Acid Gambogic Acid (Guttatic, Guttic) 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.	Clin Cancer Res, 2019, 10.1158/1078-0432.CCR-19-0775
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.	Blood, 2020, 12;blood.2020006075 Sci Adv, 2020, 6(47)eabc3465 Nat Commun, 2020, 11(1):259
S5600	Flavokawain A Flavokawain A, extracted from kava, is an apoptotic inducers and anticarcinogenic agent. Flavokawain A 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 ).It is a selective inhibitor of Bcl-2 family proteins.
S8865	BAI1 BAI1 is a direct allosteric inhibitor of BAX with a dissociation constant (Kd) of 15.0 ± 4 μM.
S7800	A-1155463 A-1155463, 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).	Oncol Rep, 2020, 44(3):927-938 Cell Rep, 2020, 32(1):107845 Cancers (Basel), 2020, 12(6):1694	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 is a potent and selectiveBCL-XL inhibitor and may be useful in the treatment of cancer, immune and autoimmune diseases.	Cancers (Basel), 2020, 12(2) Cell Death Dis, 2020, 8;11(6):443 Cell Death Dis, 2020, 11(10):875	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 is a selective Mcl-1 inhibitor with Ki of 490 nM, showing selectivity over other members of Bcl-2 family.	Mol Cancer Ther, 2020, 19(10):2001-2011 Cancers (Basel), 2020, 12(8):E2298 Int J Radiat Oncol Biol Phys, 2020, 15;106(4):867-877	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.
S8836	S64315 (MIK665) S64315 (MIK665) 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.	Cell Death Dis, 2020, 8;11(6):443 Blood Adv, 2020, 4(5):819-829 Cancers (Basel), 2020, 12(8):E2182

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S3224^新	Cinobufagin Cinobufagin (Cinobufagine), an active ingredient of Venenum Bufonis, inhibits tumor development. Cinobufagin increases ATM and Chk2 and decreases CDC25C, CDK1, and cyclin B. Cinobufagin inhibits PI3K, AKT and Bcl-2 while increases levels of cleaved caspase-9 and caspase-3. Thus, Cinobufagin induces cell cycle arrest at the G2/M phase and apoptosis.
S3238^新	Resibufogenin Resibufogenin (Bufogenin, Recibufogenin), a component of huachansu with anticancer effect, triggers necroptosis through upregulating receptor-interacting protein kinase 3 (RIP3) and phosphorylating mixed lineage kinase domain-like protein at Ser358. Resibufogenin exerts cytotoxic effect by inducing reactive oxygen species (ROS) accumulation. Resibufogenin induces apoptosis and caspase-3 and caspase-8 activity. Resibufogenin increases Bax/Bcl-2 expression, and suppresses cyclin D1, cyclin E, PI3K, p-AKT, p-GSK3β and β-catenin protein expression.
S3275^新	Senkyunolide I Senkyunolide I (SEI, SENI) is an orally active compound isolated from Ligusticum chuanxiong with analgesic, anti-migraine, neuroprotective, anti-oxidation and anti-apoptosis activities. Senkyunolide I (SEI, SENI) up-regulates the phosphorylation of Erk1/2 and induces Nrf2 nuclear translocation with enhanced HO-1 and NQO1 expressions. Senkyunolide I (SEI, SENI) promotes the ratio of Bcl-2/Bax and inhibits the expressions of cleaved caspase 3 and caspase 9.
S7105	BAM7 BAM 7 is a direct and selective activator of proapoptotic Bax with EC50 of 3.3 μM.	Nat Chem Biol, 2019, 15(4):322-330 Cell Death Discov, 2018, 4:107
S8650	BTSA1 BTSA1 is a pharmacologically optimized BAX activator that binds with high affinity and specificity to the N-terminal activation site and induces conformational changes to BAX leading to BAX-mediated apoptosis. It effectively promotes apoptosis in leukemia cell lines and patient samples while sparing healthy cells.
S7747	Ro-3306 RO-3306 is an ATP-competitive, and selective CDK1 inhibitor with K_i of 20 nM, >15-fold selectivity against a diverse panel of human kinases. RO-3306 enhances p53-mediated Bax activation and mitochondrial apoptosis.	Cell Res, 2020, 10.1038/s41422-020-0357-y Mol Cell, 2020, 22 pii: S1097-2765(20)30231-8 Nat Commun, 2020, 11(1):4338	HeLa cells were untreated or treated with either colcemid (10 μg/ml for 16 h), RO-3306 (9 μM for 16 h), or both colcemid and RO-3306, as indicated. Cells were then lysed, and proteins were detected by Western analysis.
S9276	Alisol B Alisol B, a triterpene from Alismatis rhizoma, induces Bax up-regulation and nuclear translocation, the activation of initiator caspase-8 and caspase-9, and executor caspase-3, suggesting the involvement of both extrinsic and intrinsic apoptosis pathways.
S5550	Ethyl gallate Ethyl gallat (Phyllemblin, gallic acid ethyl ester), which could be found naturally in a variety of plant sources, is a food additive with antimicrobial activity

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S1057	Obatoclax Mesylate (GX15-070) Obatoclax Mesylate (GX15-070) is an antagonist of Bcl-2 with K_i of 0.22 μM in a cell-free assay, can assist in overcoming MCL-1 mediated resistance to apoptosis. Phase 3.	Biomaterials, 2020, 232:119709 Int J Mol Sci, 2020, 5;21(5) pii: E1773 Invest New Drugs, 2020, 4	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.
S9665^新	Motixafortide (BL-8040) 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.
S7100^新	WEHI-539 HCl WEHI-539 HCl (WEHI-539 hydrochloride) has high affinity (IC50=1.1 nM) and selectivity for BCL-XL and potently kills cells by selectively antagonizing its prosurvival activity. It has more than a 400-fold higher affinity for BCL-XL versus other prosurvival BCL-2 family members.	Mol Pharmacol, 2019, 96(4):419-429 J Immunol, 2018, 200(5):1727-1736 Cell Death Differ, 2015, 22(12):2098-106
S7849	BDA-366 BDA-366 is a small-molecule Bcl2-BH4 domain antagonist and binds BH4 with high affinity and selectivity.
S7126	Marinopyrrole A (Maritoclax) Marinopyrrole A (Maritoclax) is a selective Mcl-1 antagonist. It binds to Mcl-1, but not Bcl-XL, and targets Mcl-1 for proteasomal degradation. Maritoclax disrupts the interaction between Bim and Mcl-1 with an IC50 of 10.1 μM.	Leukemia, 2019, 33(2):319-332 Molecules, 2018, 23(11)E3030

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S8199	LTX-315 (Ruxotemitide) LTX-315 (Ruxotemitide, Oncopore) is the oncolytic peptide that kills cancer cells through Bax/Bak-regulated mitochondrial membrane permeabilization.

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S8199

LTX-315 (Ruxotemitide)

LTX-315 (Ruxotemitide, Oncopore) is the oncolytic peptide that kills cancer cells through Bax/Bak-regulated mitochondrial membrane permeabilization.