Catalog No.
Product Name
Application
Product Information
Product Citation
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Bcl-2 inhibitor
ABT-263 also called Navitoclax is a potent and orally bioavailable Bcl-2 family inhibitor (Ki's of <1 nmol/L for Bcl-2, Bcl-xL, and Bcl-w). it maintains a high affinity for Bcl-xL, Bcl-2, and Bcl-w, (Ki ≤1 nmol/L), but binds more weakly to Mcl-1 and A1.- Abdel-Aziz S Shatat, .et al. , Purinergic Signal, 2024, May 27 PMID: 38801618
- Tristen Wright, .et al. , Mol Cell, 2024, Apr 4;84(7):1338-1353 PMID: 38503284
- Bopei Cui, .et al. , Signal Transduct Target Ther, 2023, Sep 25;8(1):366 PMID: 37743418
- Yibo Wen, .et al. , Ren Fail, 2023, Dec;45(1):2194440 PMID: 37154092
- Rindert Missiaen, .et al. , Cell Metab, 2022, Aug 2;34(8):1151-1167 PMID: 35839757
- Ashlyn Parkhurst, .et al. , Cell Death Dis, 2022, Apr 28;13(4):410 PMID: 35484114
- Suzuki, Keiji, .et al. , Mutat Res Genet Toxicol Environ Mutagen, 2022, 876-877. 503448
- Rotem Ben-Hamo, .et al. , Nat Commun, 2020, 11: 3296
- Hua Xu, .et al. , Cancers (Basel), 2020, Apr; 12(4): 831 PMID: 32235588
- Hiroki Akiyama, .et al. , Cancers, 2020, 12 (2) PMID: 32050632
- Stephanie Ketterer, .et al. , Nat Commun, 2020, Oct 12;11(1):5133 PMID: 33046706
- Makoto Koyama, .et al. , Int J Oncol, 2020, Sep 2 PMID: 32901840
- Min Li, .et al. , Nat Commun, 2020, 11: 4051 PMID: 32792548
- Hamzehlou S, .et al. , Eur J Pharmacol, 2019, Nov 15;863:172705 PMID: 31574259
- Momeny M, .et al. , Cell Oncol (Dordr), 2019, Apr 25 PMID: 31025257
- Anderson R, .et al. , EMBO J, 2019, Feb 8. pii: e100492 PMID: 30737259
- Shinya Ishida, .et al. , Oncotarget, 2018, Jun 1; 9(42): 26834-26851 PMID: 29928488
- Rhys Anderson, .et al. , bioRxiv, 2018, 2018
- Ryuta Mikawa, .et al. , Aging Cell, 2018, Oct; 17(5): e12827 PMID: 30058137
- Joo Sang Lee, .et al. , Nat Commun, 2018, 9: 2546 PMID: 29959327
- Toshiyuki Sumi, .et al. , Int J Oncol, 2018, Jul; 53(1): 33-46 PMID: 29658609
- Wei TW, .et al. , Cancer Res, 2017, Jan 15;77(2):494-508 PMID: 28069801
- Yusuke Takagi, .et al. , Cancer Sci, 2016, Sep; 107(9): 1270-1280 PMID: 27348272
- Matsumoto M, .et al. , Biochem Biophys Res Commun, 2016, Apr 29;473(2):490-6 PMID: 26996126
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Bcl-2 Inhibitor
ABT-737 is a pan-Bcl-2 inhibitor. IC50 values ranged from 192 nM (the pre-B cell line Hal-01) to <10 μM (Nalm-6, K562 and HL-60).- Jung Mo Lee, .et al. , Yonsei Med J, 2022, Jan;63(1):16-25 PMID: 34913280
- AidaVarela-Moreira, .et al. , Int J Pharm, 2022, Apr 25;618:121638 PMID: 35257802
- Daniel F R Boehmer, .et al. , Sci Immunol, 2021, Jul 16;6(61) PMID: 34272227
- Shivani Arora, .et al. , Med, 2021, 2,1-13
- Ying Ji, .et al. , Nat Commun, 2020, Aug 25;11(1):4249 PMID: 32843618
- Birgit Ritschka, .et al. , Genes Dev, 2020, Apr 1;34(7-8):489-494 PMID: 32139422
- Hiroki Akiyama, .et al. , Cancers, 2020, 12 (2) PMID: 32050632
- Hsu CC, .et al. , Arch Oral Biol, 2020, Mar;111:104653 PMID: 31935534
- Gupta VK, .et al. , Apoptosis, 2020, Feb;25(1-2):135-150 PMID: 31867678
- Meikle V, .et al. , Antimicrob Agents Chemother, 2018, Nov 12. pii: AAC.01846-18 PMID: 30420480
- Chauhan D, .et al. , Cell Rep, 2018, Nov 27;25(9):2354-2368.e5 PMID: 30485805
- Jose Mario Gonzalez-Meljem, .et al. , Nat Commun, 2017, 8: 1819 PMID: 29180744
- Zhang C, .et al. , J Biol Chem, 2017, Sep 8;292(36):15105-15120 PMID: 28673964
- Eun Young Kim, .et al. , Neoplasia, 2017, Apr; 19(4): 354-363 PMID: 28319809
- Masayoshi Toge, .et al. , Int J Oncol., 2015, Apr;46(4):1844-8 PMID: 25647738
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Bcl-2 Inhibitor
Bcl-2 homology domain-3 (BH3) mimetic,antagonize all antiapoptotic Bcl-2 family proteins (average IC50, 3 umol/L), including Mcl-1 (IC50, 2.9 umol/L) and Bfl-1 (IC50, 5 umol/L).- Ashlyn Parkhurst, .et al. , Cell Death Dis, 2022, Apr 28;13(4):410 PMID: 35484114
- Silva S, .et al. , Sci Rep, 2019, Nov 27;9(1):17703 PMID: 31776405
- Chi-Hung R. Or, .et al. , Int J Mol Sci, 2016, Jan; 18(1): 44 PMID: 28035994
- P Geserick, .et al. , Cell Death Dis., 2014, 5(9): e1412 PMID: 25210795
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Bcl-2 inhibitor
Gambogic acid is a natural product isolated from the Garcinia hanburyi tree. 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. - Jaceosidin is a pharmacologically active flavone derived from Artemisia argyi, inhibits phorbol-ester-induced upregulation of COX-2 and MMP-9 by blocking phosphorylation of ERK-1 and -2 in cultured human mammary epithelial cells.
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Bcl-2 inhibitor
ABT-199 is a so-called BH3-mimetic drug, which is designed to block the function of the protein Bcl 2.- Lindy Vernooij, .et al. , EJC Paediatric Oncology, 2024, 3: 100168
- Tristen Wright, .et al. , Mol Cell, 2024, Apr 4;84(7):1338-1353 PMID: 38503284
- Dilay Karademir, .et al. , Med Oncol, 2023, Jul 11;40(8):234 PMID: 37432531
- Ashlyn Parkhurst, .et al. , Cell Death Dis, 2022, Apr 28;13(4):410 PMID: 35484114
- Anna L Koessinger, .et al. , Cell Death Differ, 2022, Apr 26 PMID: 35473984
- Florian J Bock, .et al. , Nat Commun, 2021, Nov 12;12(1):6572 PMID: 34772930
- Chauhan D, .et al. , Cell Rep, 2018, Nov 27;25(9):2354-2368.e5 PMID: 30485805
- Martin Grundy, .et al. , PLoS One, 2018, 13(1): e0190682 PMID: 29298347
- Joanne Dai, .et al. , J Immunol, 2018, 200 (5) 1727-1736 PMID: 29358277
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Bcl-2 inhibitor
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.- Christopher D. Graham, .et al. , Oncotarget, 2017, Jan 31; 8(5): 8670-8678 PMID: 28055968
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Bax activator
BAM 7 binds the BAX trigger site with an EC50 ~ 3.3 μM as measured in a competitive FP assay using FITC-BIM SAHB and BAX.- Takino JI, .et al. , Sci Rep, 2019, Nov 13;9(1):16717 PMID: 31723205
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Bcl-xL inhibitor
WEHI-539 hydrochloride is a small-molecule inhibitor of BCL-xL with IC50 value of 1.1 nM. -
pan Bcl-2 inhibitor
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; does not inhibit BIR3 domain and BID -
Bcl-2 Inhibitor
Bcl-2 Inhibitor contains a mixture of two tautomers. A potent, cell-permeable, Bcl-2 inhibitor competes with Bak BH3 peptide for binding to Bcl-2 and Bcl-XL in vitro (IC50 =10 uM and 7 uM, respectively).- Toshiyuki Sumi, .et al. , Int J Oncol, 2018, Jul; 53(1): 33-46 PMID: 29658609
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IMPDH inhibitor
AVN-944 (also known as VX-944) serves as an effective oral inhibitor, specifically targeting and inhibiting IMPDH (inosine monophosphate dehydrogenase). This enzyme plays a crucial role as a rate-limiting factor in the synthesis of guanine nucleotides from scratch. Additionally, AVN-944 acts against the synthesis of RNA in arenaviruses, effectively preventing arenavirus infections. Demonstrating a wide spectrum of anti-cancer properties, AVN-944 is utilized in research related to multiple myeloma (MM) and acute myeloid leukemia (AML).
- Kevin Chiem, .et al. , Microbiol Spectr, 2023, Aug 17;11(4):e0474522 PMID: PMC10434227
- Desarey Morales Vasquez, .et al. , Viruses, 2020, Sep; 12(9): 1041 PMID: 32961956
- Park JG, .et al. , J Virol, 2020, Mar 17;94(7) PMID: 31941776
- Dunham EC, .et al. , Antiviral Res, 2018, Sep;157:140-150 PMID: 30031760
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Bcl-2 Inhibitor
Acetate gossypol, a polyphenolic compound isolated from cottonseeds, inhibits Bcl-2 by acting as a BH3 mimetic. -
Bcl-2 Inhibitor
AT101, the R-(-) enantiomer of Gossypol acetic acid, binds with Bcl-2, Bcl-xL and Mcl-1 with Ki of 0.32μM, 0.48μM and 0.18μM. -
Bax channel blocker
Bax channel blocker is a potent inhibitor of Bax-mediated mitochondrial cytochrome C release (IC50 = 0.52 μM).- Stella Victorelli, .et al. , Nature, 2023, Oct;622(7983):627-636 PMID: 37821702
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Bax inhibitor
Bax inhibitor peptide P5, cell-permeable synthetic peptide inhibitor of Bax translocation to mitochondria; designed from Ku70, a protein that is suggested to suppress the mitochondrial translocation of Bax. Inhibits Bax-mediated apoptosis in vitro. -
Bax inhibitor
Bax inhibitor peptide V5, cell-permeable synthetic peptide inhibitor of Bax translocation to mitochondria; designed from Ku70, a protein that is suggested to suppress the mitochondrial translocation of Bax. Inhibits Bax-mediated apoptosis in vitro. -
Bax inhibitor
Bax inhibitor peptide, negative control, negative control peptide for the Bax inhibitor peptides V5 and P5 , which inhibit Bax translocation to mitochondria and Bax-mediated apoptosis in vitro. -
EcR agonist
Muristerone A is a phytoecdysteroid analog of ecdysone which induces genes in mammalian cells and causes apoptosis in cells transfected with wild-type Bax. -
MCL-1 inhibitor
A-1210477 is a potent and selective MCL-1 inhibitor. A-1210477 induces the hallmarks of intrinsic apoptosis and demonstrates single agent killing of multiple myeloma and non-small cell lung cancer cell lines.- Vijaya Bharti, .et al. , Cell Rep, 2022, Dec 20;41(12):111826 PMID: 36543138
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BCL-XL inhibitor
A-1155463 is a highly potent and selective BCL-XL inhibitor, A-1155463 shows picomolar binding affinity to BCL-XL (Ki = <0.01 nM), and >1000-fold weaker binding to BCL-2 (Ki = 80 nM) and related proteins BCL-W (Ki = 19 nM) and MCL-1 (Ki > 440 nM)- Vijaya Bharti, .et al. , Cell Rep, 2022, Dec 20;41(12):111826 PMID: 36543138
- Daniel F R Boehmer, .et al. , Sci Immunol, 2021, Jul 16;6(61) PMID: 34272227
- Chauhan D, .et al. , Cell Rep, 2018, Nov 27;25(9):2354-2368.e5 PMID: 30485805
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Bcl-2 inhibitor
Apogossypolone is a nonpeptidic small-molecule inhibitor of Bcl-2 with -
Mcl-1 inhibitor
MIM1 is a selective small molecule inhibitor of Mcl-1(IC50= 4.8 μM) that overcomes Mcl-1-dependent leukemia cell survival. -
Bcl-2 family inhibitor
(+)-Apogossypol is a potent inhibitor of Bcl-2 family proteins; competing 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. - (S)-Gossypol acetic acid is a inhibitor of Bcl-2, potently induce cell death in Jurkat cells overexpressing Bcl-2 (IC50, 18.1μM) or Bcl-xL (IC50, 22.9μM).
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Mcl-1 inhibitor
Pyridoclax is a potent Mcl-1 inhibitor with Kd value of 25 nM. -
Bcl-2 modulator
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. -
Mcl-1 inhibitor
Marinopyrrole A, aslo known as Maritoclax, is a selective inhibitor of Mcl-1 with IC50 value of 10.1μM. -
Mcl-1 inhibitor
(R)-MIK665 is the less active enantiomer of MIK665. MIK665 is a special Mcl-1 inhibitor with an IC50 of 1.81 nM. - Thevetiaflavone could upregulate the expression of Bcl?2 and downregulate that of Bax and caspase?3.
