- 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
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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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 -
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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Bax channel blocker
Bax channel blocker is a potent inhibitor of Bax-mediated mitochondrial cytochrome C release (IC50 = 0.52 μM). -
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. -
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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Mcl-1 and Bcl-2 dual inhibitor
MCL-1/BCL-2-IN-4 (Compound 7) is a potent and selective Mcl-1 and Bcl-2 dual inhibitor. -
Mcl-1 and Bcl-2 dual inhibitor
MCL-1/BCL-2-IN-3 (Compound 2) is a potent and selective Mcl-1 and Bcl-2 dual inhibitor with IC50s of 5.95 and 4.78 μM, respectively.