- MIF antagonist is an inhibitor of the dopachrome tautomerase activity of MIF in vitro (IC50 = 7 M) and in cells (IC50 = 25 M).
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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
- 25-hydroxy Cholesterol is a side-chain substituted oxysterol derived from dietary cholesterol that inhibits the cleavage of sterol regulatory element binding proteins (SREBPs) to suppress endogenous cholesterol synthesis in various cell types
- Kevetrin (thioureidobutyronitrile), is a water-soluble, small molecule and activator of the tumor suppressor protein p53, with potential antineoplastic activity.
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PKD inhibitor
CID755673 is a potent PKD inhibitor with IC50s of 182 nM, 280 nM and 227 nM for PKD1, PKD2 and PKD3, respectively. -
PKD1 inhibitor
CID797718 is a structural analog of CID755673 (Adooq Catalog No. A13804). It was a 10-time less potent PKD1 inhibitor with an IC50 value of 7.0 +/-0.8 uM. -
PERK inhibitor
ISRIB (trans-isomer) is a potent and selective small molecule inhibitor of PERK signaling (IC50 ~5 nM) that can potently reverse the effects of eIF2α phosphorylation. - Ecabet sodium is a widely employed mucoprotective agent for the treatment of gastric ulcers.
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Caspase inhibitor
Nivocasan is a novel caspase-inhibitor has demonstrated hepatoprotective activity in fibrosis/apoptosis animal models. -
MDM2/p53 Inhibitor
Idasanutlin is a potent and selective p53-MDM2 inhibitor. -
dual cIAP and XIAP inhibitor
BV-6 is a SMAC mimetic, dual cIAP and XIAP inhibitor.- Aneri Shah, .et al. , Cancers (Basel), 2020, Aug 5;12(8):E2188 PMID: 32764479
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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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Caspase-9 Inhibitor
Z-LEHD-FMK is a synthetic peptide that irreversibly inhibits caspase-9 and related caspase activity.- Jason Segura, .et al. , PLoS One, 2023, Feb 13;18(2):e0281087 PMID: 36780482
- Wenquan Liang, .et al. , Sci Rep, 2016, 6: 38267 PMID: 27905569
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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. -
osteoblast differentiation inducer
Asperosaponin VI, A saponin component from Dipsacus asper wall, induces osteoblast differentiation through BMP?\2/p38 and ERK1/2 pathway. Asperosaponin ?? inhibits apoptosis in hypoxia-induced cardiomyocyte by increasing the Bcl-2/Bax ratio and decreasing active caspase-3 expression, as well as enhancing of p-Akt and p-CREB. -
Stat3 inhibitor & Apoptosis inducer
Homoharringtonine is a cephalotaxine alkaloid which inhibits the formation of diphenylalanine and acetylphenylalanyl-puromycin in liver ribosomes. -
Bcl-2 Inhibitor
Acetate gossypol, a polyphenolic compound isolated from cottonseeds, inhibits Bcl-2 by acting as a BH3 mimetic. -
Caspase inhibitor
Q-VD-OPH is a selective, brain and cell permeable, highly potent and irreversible inhibitor of caspase-3 ( IC50=25nm), caspase-1 (IC50=50nM), caspase-8 (IC50=100nM) and caspase-9 (IC50=430nM).- 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
- Davide Pradella, .et al. , Nat Commun, 2021, 12: 4872 PMID: 34381052
- Haschka MD, .et al. , Cell Death Differ, 2020, Feb 3 PMID: 32015503
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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). -
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. -
Apoptosis inducer
Episilvestrol is a derivative of Silvestrol, which can induce apoptosis in LNCaP cells through the mitochondrial/apoptosome pathway without activation of executioner caspase-3 or -7; 5'myc-UTR-LUC inhibtior (IC50= 0.8 nM). -
Necroptosis inhibitor
Necrostatin 2 is a potent necroptosis inhibitor with EC50 of 50 nM. -
p53-MDM2 interaction inhibitor
p53 and MDM2 proteins-interaction-inhibitor chiral is an inhibitor of the interaction between p53 and MDM2 proteins. -
p53-MDM2 interaction inhibitor
p53 and MDM2 proteins-interaction-inhibitor racemic is an inhibitor of the interaction between p53 and MDM2 proteins. -
Tyrosine kinase inhibitor
Regorafenib is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit, RET and Raf-1 with IC50 of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM, respectively. -
Survivin suppressant
YM-155 is a potent survivin suppressant by inhibiting Survivin promoter activity with IC50 of 0.54 nM. -
Fluorogenic caspase substrate
Ac-LEHD-AFC, fluorogenic caspase substrate. Analog of the caspase-9 substrate, LEHD-AFC. -
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). -
Caspase-3 inhibitor
Ivachtin is a potent, cell-permeable, reversible, non-competitive inhibitor of Caspase-3 (IC50 = 23 nM).- Yosefzon Y, .et al. , Mol Cell, 2018, May 17;70(4):573-587.e4 PMID: 29775577
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Fluorogenic caspase substrate
Ac-LEHD-AFC is a fluorogenic substrate for caspase-4, caspase-5, and caspase-9. -
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. -
Apoptosis Inducer
2,3 DCPE displays anticancer agent properties and induces ERK activation.