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mitotic progression inhibitor
3-Hydroxycapric acid is an inhibitor for mitotic progression. -
Aurora inhibitor
Danusertib (PHA-739358) is an Aurora kinase inhibitor for Aurora A/B/C with IC50 of 13 nM/79 nM/61 nM in cell-free assays, modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc. Phase 2- Vijaya Bharti, .et al. , Cell Rep, 2022, Dec 20;41(12):111826 PMID: 36543138
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IAP inhibitor
AT-406 is an orally bioavailable inhibitor of IAP family of proteins with potential apoptotic inducing and antineoplastic activity. AT-406 selectively inhibits the biological activity of IAP proteins, including X chromosome-linked IAP (XIAP), the cellular IAPs 1 (c-IAP1) and 2 (c-IAP2) and melanoma inhibitor of apoptosis protein (ML-IAP).- Yoshikawa M, .et al. , J Med Chem, 2018, Mar 22;61(6):2384-2409 PMID: 29485864
- Tsuyoshi Ishii, .et al. , Sci Rep, 2017, 7: 13000 PMID: 29026104
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VEGFR1/2/3/PDGFRβ/Kit/RET/Raf-1 inhibitor
Regorafenib Hydrochloride is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively. -
N-SMase inhibitor
GW4869 is a cell permeable, selective inhibitor of N-SMase (neutral sphingomyelinase).
- Guohao Wang, .et al. , Nat Commun, 2021, Sep 30;12(1):5733 PMID: 34593794
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myeloperoxidase inhibitor
PF-06282999 is a potent and selective myeloperoxidase inhibitor which is potential useful for the treatment of cardiovascular diseases. -
Caspase-6 inhibitor
Z-VEID-FMK is the specific recognition sequence for caspase-6/Mch2. Z-VEID-FMK is a synthetic peptide that irreversibly inhibits activity of VEID-dependent caspases (e.g., caspase-6). The inhibitor is designed as a methyl ester to facilitate cell permeability. -
RIP1 inhibitor
GSK481 is a novel benzoxazepinone (BOAz) series of RIP1 inhibitors. Receptor Interacting Protein Kinase 1 (RIP1) has been implicated as a key contributor to inflammation through the regulation of programmed necrosis. Inhibition of this kinase has been shown to hinder cell necrotic death, thereby establishing RIP1 as a viable target for the potential treatment of multiple inflammatory diseases. -
Caspase-2 inhibitor
Z-VDVAD-FMK is a cell-permeable, irreversible inhibitor of caspase-2. Caspase inhibitors play an important role in investigating biological processes. -
caspase 8 inhibitor
Z-IETD-FMK is a specific inhibitor of caspase 8.- Jason Segura, .et al. , PLoS One, 2023, Feb 13;18(2):e0281087 PMID: 36780482
- Liqun Zhao, .et al. , Apoptosis, 2021, Apr 27 PMID: 33905036
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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 -
MDM2 inhibitor
MDM2 Inhibitor is a cell-permeable boranyl-chalcone exhibiting strong binding to MDM2 and irreversibly disrupts the MDM2/p53 protein complex. -
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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PERK inhibitor
ISRIB is a potent and selective PERK inhibitor with IC50 of 5 nM.- Zhou W, .et al. , Research Square, 2023, MAY 03
- Satoshi Watanabe, .et al. , Proc Natl Acad Sci U S A, 2021, May 18;118(20) PMID: 33972447
- Satoshi Watanabe, .et al. , bioRxiv, 2020, February 27
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Mdm2 inhibitor
MI-773 is a new small molecule inhibitor of the MDM2-p53 interaction, binds to MDM2 with high affinity (Ki=0.88 nM) and blocks the p53-MDM2 interaction. -
Caspase inhibitor
Z-WEHD-FMK is a synthetic peptide that irreversibly inhibits caspase-5 and related caspase activity. -
Caspase-3/7 Inhibitor
Caspase-3/7 Inhibitor I is a potent, cell-permeable, and specific, reversible inhibitor of caspase-3 (Ki = 60 nM) and caspase-7 (Ki = 170 nM). -
Necroptosis inhibitor
Necrostatin 2 is a potent necroptosis inhibitor with EC50 of 50 nM. -
Caspase-3 inhibitor
AZ 10417808, selective non-peptide inhibitor of caspase-3 (Ki = 247 nM); displays > 40-fold selectivity over caspases 1, 2, 6, 7 and 8 (Ki > 10 uM). -
Necroptosis inhibitor
Necrostatin 2 is a potent necroptosis inhibitor with EC50 of 50 nM. -
Necroptosis inhibitor
Necrostatin 2 is a potent necroptosis inhibitor with EC50 of 50 nM. -
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. -
MDMX inhibitor
SJ 172550 is the first MDMX inhibitor with EC50 of 0.84 uM; binds reversibly to MDMX and effectively kills retinoblastoma cells in which the expression of MDMX is amplified.- Saketh S Dinavahi, .et al. , Cancer Immunol Res, 2022, Jun 3;10(6):757-769 PMID: 35439317
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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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Caspase-1 inhibitor
Z-YVAD-FMK is a potent cell-permeable and irreversible inhibitor of caspase-1.- Yuping Fan, .et al. , Sci Transl Med, 2021, Jul 28;13(604):eabb1069 PMID: 34321317
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MDM2 inhibitor
NVP-CGM097 is a potent and selective MDM2 inhibitor; an orally bioavailable HDM2 antagonist with potential antineoplastic activity. -
TNF receptor inhibitor
AX-024 is an orally available inhibitor of the TCR-Nck interaction that selectively inhibits TCR-triggered T cell activation (IC50 value 1 nM). Inhibiting an immediate TCR signal has promise for treating a broad spectrum of human T cell-mediated autoimmune and inflammatory diseases. -
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.