Caspase

Inhibitory Selectivity

Catalog No.	Inhibitor Name	Pan-Caspase	Caspase-1	Caspase-2	Caspase-3	Caspase-4	Caspase-5	Caspase-6	Caspase-7	Caspase-8	Caspase-9
A10984	VX-765 (Belnacasan)		**			***
A12373	Z-VAD-FMK	*
A13503	Z-DEVD-FMK
A14915	Q-VD-OPh hydrate		****		****					***	***
A14919	Caspase-3/7 Inhibitor I				****				***
A12611	Z-VEID-FMK
A12637	Z-VDVAD-FMK
A12697	Z-DQMD-FMK
A12800	Z-IETD-FMK
A14358	Z-LEHD-FMK
A14284	Z-FA-FMK
A15300	Ivachtin				****
A15392	Boc-D-FMK
A14916	Z-WEHD-FMK
A15816	Ac-DEVD-CHO		***	*	****	**	**	**	***	****	**

Notes:
1.Hover mouse over " * " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " * " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Catalog No.	Product Name	Application	Product Information
A15291	Ac-LEHD-AFC	Fluorogenic caspase substrate	Ac-LEHD-AFC, fluorogenic caspase substrate. Analog of the caspase-9 substrate, LEHD-AFC.
A15319	Ac-IEPD-AFC	Fluorogenic caspase substrate	Ac-LEHD-AFC is a fluorogenic substrate for caspase-4, caspase-5, and caspase-9.
A15308	PETCM	Caspase-3 activator	PETCM is an activator of caspase-3 and a stimulator of apoptosome formation in HeLa cell cytosols.
A15300	Ivachtin	Caspase-3 inhibitor	Ivachtin is a potent, cell-permeable, reversible, non-competitive inhibitor of Caspase-3 (IC50 = 23 nM). Product Citations (1) Yosefzon Y, .et al. Caspase-3 Regulates YAP-Dependent Cell Proliferation and Organ Size, Mol Cell, 2018, May 17;70(4):573-587.e4 PMID: 29775577
A15294	AZ 10417808	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).
A12611	Z-VEID-FMK	Caspase-6 inhibitor	Z-VEID-FMK is the specific recognition sequence for caspase-6/Mch2.
A14919	Caspase-3/7 Inhibitor I	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).
A14916	Z-WEHD-FMK	Caspase inhibitor	Z-WEHD-FMK is a synthetic peptide that irreversibly inhibits caspase-5 and related caspase activity.
A14915 SALE	Q-VD-OPh hydrate	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).
A12637	Z-VDVAD-FMK	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.
A14358	Z-LEHD-FMK	Caspase-9 Inhibitor	Z-LEHD-FMK is a synthetic peptide that irreversibly inhibits caspase-9 and related caspase activity. Product Citations (1) Wenquan Liang, .et al. Shikonin induces mitochondria-mediated apoptosis and enhances chemotherapeutic sensitivity of gastric cancer through reactive oxygen species, Sci Rep, 2016, 6: 38267 PMID: 27905569
A12697	Z-DQMD-FMK	Caspase-3 inhibitor	Z-DQMD-FMK is a synthetic peptide that irreversibly inhibits the activity of Caspase-3.
A13503 SALE	Z-DEVD-FMK	Caspase-3 Inhibitor	Z-DEVD-FMK is a specific, irreversible Caspase-3 inhibitor. Product Citations (3) Yosefzon Y, .et al. Caspase-3 Regulates YAP-Dependent Cell Proliferation and Organ Size, Mol Cell, 2018, May 17;70(4):573-587.e4 PMID: 29775577 Akashi E, .et al. Effects of galectin-9 on apoptosis, cell cycle and autophagy in human esophageal adenocarcinoma cells, Oncol Rep, 2017, Jul;38(1):506-514 PMID: 28586026 Wenquan Liang, .et al. Shikonin induces mitochondria-mediated apoptosis and enhances chemotherapeutic sensitivity of gastric cancer through reactive oxygen species, Sci Rep, 2016, 6: 38267 PMID: 27905569
A14100	Nivocasan (GS-9450)	Caspase inhibitor	Nivocasan is a novel caspase-inhibitor has demonstrated hepatoprotective activity in fibrosis/apoptosis animal models.
A12800	Z-IETD-FMK	caspase 8 inhibitor	Z-IETD-FMK is a specific inhibitor of caspase 8.
A12373 SALE	Z-VAD-FMK	Pan Caspase Inhibitor	Z-VAD-FMK is a cell-permeable, irreversible pan-caspase inhibitor. Inhibits caspase processing and apoptosis induction in tumor cells in vitro (IC50 = 0.0015 - 5.8 mM). Active in vivo. Product Citations (13) Fujiki K, .et al. Blockade of ALK4/5 signaling suppresses cadmium- and erastin-induced cell death in renal proximal tubular epithelial cells via distinct signaling mechanisms, Cell Death Differ, 2019, Feb 25 PMID: 30804470 T Yamamoto, .et al. Mycoplasma pneumoniae protects infected epithelial cells from hydrogen peroxide-induced cell detachment, Cell Microbiol, 2019, 2019 PMID: 30702185 D. Bosc, .et al. A new quinoline-based chemical probe inhibits the autophagy-related cysteine protease ATG4B, Sci Rep, 2018, 8: 11653 PMID: 30076329 Tsukamoto H, .et al. Lipopolysaccharide (LPS)-binding protein stimulates CD14-dependent Toll-like receptor 4 internalization and LPS-induced TBK1-IKKε-IRF3 axis activation, J Biol Chem, 2018, Jun 29;293(26):10186-10201 PMID: 29760187 Hiroshi Kuribayashi, .et al. Roles of Nmnat1 in the survival of retinal progenitors through the regulation of pro-apoptotic gene expression via histone acetylation, Cell Death Dis, 2018, Sep; 9(9): 891 PMID: 30166529 Matsuo J, .et al. Activation of caspase-3 during Chlamydia trachomatis-induced apoptosis at a late stage, Can J Microbiol, 2018, Oct 18:1-9 PMID: 30336068 Orly Ravid, .et al. Blood-Brain Barrier Cellular Responses Toward Organophosphates: Natural Compensatory Processes and Exogenous Interventions to Rescue Barrier Properties, Front Cell Neurosci, 2018, 12: 359 PMID: 30459557 Im E, .et al. Luteolin induces caspase-dependent apoptosis via inhibiting the AKT/osteopontin pathway in human hepatocellular carcinoma SK-Hep-1 cells, Life Sci, 2018, Sep 15;209:259-266 PMID: 30107166 Szalai P, .et al. Nonlinear relationship between ER Ca2+ depletion versus induction of the unfolded protein response, autophagy inhibition, and cell death, Cell Calcium, 2018, Dec;76:48-61 PMID: 30261424 Im E, .et al. Dihydroartemisinin induced caspase-dependent apoptosis through inhibiting the specificity protein 1 pathway in hepatocellular carcinoma SK-Hep-1 cells, Life Sci, 2018, Jan 1;192:286-292 PMID: 29128513 Iriyama N, .et al. The cyclin-dependent kinase 4/6 inhibitor, abemaciclib, exerts dose-dependent cytostatic and cytocidal effects and induces autophagy in multiple myeloma cells, Leuk Lymphoma, 2018, Jun;59(6):1439-1450 PMID: 28918692 Birte Plitzko, .et al. The natural product mensacarcin induces mitochondrial toxicity and apoptosis in melanoma cells, J Biol Chem, 2017, Dec 22; 292(51): 21102-21116 PMID: 29074620 Akashi E, .et al. Effects of galectin-9 on apoptosis, cell cycle and autophagy in human esophageal adenocarcinoma cells, Oncol Rep, 2017, Jul;38(1):506-514 PMID: 28586026
A15816	Ac-DEVD-CHO	Caspase Inhibitor	Ac-DEVD-CHO is an aldehyde peptide and a CPP32/Apopain Inhibitor.
A16317	Z-YVAD-FMK	Caspase-1 inhibitor	Z-YVAD-FMK is a potent cell-permeable and irreversible inhibitor of caspase-1.
A16340	Z-VAD(OH)-FMK	Caspase inhibitor	Z-VAD(OH)-FMK is an irreversible tripeptide inhibitor of all caspases.
A15392	Boc-D-FMK	Caspase inhibitor	BOC-D-FMK is a Novel inhibitor of Caspase-3.
A10984 SALE	VX-765 (Belnacasan)	Caspase-1/4 inhibitor	VX-765 is a novel Caspase-1 inhibitor,which is an enzyme that controls the generation of two cytokines, IL-1b and IL-18. Product Citations (4) Joseph Flores, .et al. Caspase-1 inhibition alleviates cognitive impairment and neuropathology in an Alzheimer-s disease mouse model, Nat Commun, 2018, 9: 3916 PMID: 30254377 Mohamed F. Ali, .et al. Canonical Stimulation of the NLRP3 Inflammasome by Fungal Antigens Links Innate and Adaptive B-Lymphocyte Responses by Modulating IL-1β and IgM Production, Front Immunol, 2017, 8: 1504 PMID: 29170665 García-Fernández A, .et al. Targeting inflammasome by the inhibition of caspase-1 activity using capped mesoporous silica nanoparticles, J Control Release, 2017, Feb 28;248:60-70 PMID: 28069553 Jiujiu Yu, .et al. Inflammasome activation leads to Caspase-1-dependent mitochondrial damage and block of mitophagy, Proc Natl Acad Sci U S A., 2014, 111(43): 15514-15519 PMID: 25313054
A13704	25-hydroxy Cholesterol	-	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
A14284	Z-FA-FMK	Irreversible Cysteine Protease inhibitor	Z-FA-FMK is an irreversible cysteine protease inhibitor.
A13070 SALE	LY573636 (Tasisulam)	Apoptosis inducer	LY573636 is a potent anti-tumor agent, which causes growth arrest and apoptosis of a variety of human solid tumors in vitro and in vivo. LY573636-induced apoptosis occurs by a mitochondrial-targeted mechanism. Product Citations (1) Ting Han, .et al. Anticancer sulfonamides target splicing by inducing RBM39 degradation via recruitment to DCAF15, Science, 2017, Apr 28;356(6336). pii: eaal3755 PMID: 28302793
A11944	Apoptosis Activator 2	Apoptosis Activator	Apoptosis Activator 2 strongly induces caspase-3 activation, PARP cleavage, and DNA fragmentation which leads to the destruction of cells (Apaf-1 dependent) with IC50 of ~4 μM, inactive to HMEC, PREC, or MCF-10A cells
A11090 SALE	PAC-1	Caspase activator	PAC-1 is first procaspase activating compound. Product Citations (1) Hirosumi Tamura, .et al. Evaluation of anticancer agents using patient-derived tumor organoids characteristically similar to source tissues, Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
A16381	Z-FA-FMK	Cysteine protease inhibitor	Z-FA-FMK is an irreversible inhibitor of cysteine protease

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A15291

A15319

A15308

A15300

A15294

A12611

A14919

A14916

A14915 SALE

A12637

A14358

A12697

A13503 SALE

A14100

A12800

A12373 SALE

A15816

A16317

A16340

A15392

A10984 SALE

A13704

A14284

A13070 SALE

A11944

A11090 SALE

A16381

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