Caspase Inhibitor

M867 is a selective and reversible inhibitor of caspase-3 with an IC₅₀ of 1.4 nM and K_i of 0.7 nM. M867 has anti apoptotic activity.

Ac-YVAD-AOM is the inhibitor of caspase-1 that shows antitumor activity.

Ac-AAVALLPAVLLALLAPVAD-CHO (TFA) is a composite of Ac-VAD-CHO. Ac-AAVALLPAVLLALLAPVAD-CHO (TFA) is a non-selective caspase inhibitor as well as a cell permeable hydrophobic sequence derived from K-FGF.

GDC-2394 (Compound 20) sodium is an orally active and selective NLRP3 inhibitor, and also inhibits IL-1β with IC₅₀s of 0.4 μM (human IL-1β) and 0.1 μM (mouse IL-1β). GDC-2394 sodium inhibits NLRP3-induced caspase-1 activity without inhibiting NLRC4-dependent inflammasome activation. GDC-2394 sodium could be used to study gouty arthritis.

CDK1/2/4-IN-1 (compound 3a) is a potent CDK inhibitor with IC₅₀ values of 1.47, 0.78 and 0.87 μM for CDK1, CDK2 and CDK4, respectively. CDK1/2/4-IN-1 arrests cell cycle at G2/M phase and induces apoptosis. CDK1/2/4-IN-1 elevates Bax, caspase-3, P53 levels and decreases Bcl-2 level. CDK1/2/4-IN-1 can be used for cancer research.

NLRP3-IN-84 (Compound 32) is a NLRP3 inflammasome inhibitor. NLRP3-IN-84 can interfere with the oligomerization process of NLRP3 by inhibiting the activity of NLRP3 ATPase (IC₅₀ = 158.4 nM). NLRP3-IN-84 inhibits Caspase-1 (IC₅₀ = 27.7 nM), IL-1β release (PBMC: IC₅₀ = 19.5 nM; mPBMC: IC₅₀ = 24.2 nM), and ASC plaque formation (IC₅₀ = 131 nM). NLRP3-IN-84 has no inhibitory activity on NLRC4 and AIM2 inflammasomes. NLRP3-IN-84 exhibits significant in vivo anti-inflammatory effects in a mouse acute peritonitis model. NLRP3-IN-84 can be used for the study of NLRP3-related inflammatory diseases.

Berberine (hemisulfate) (Standard) is the analytical standard of Berberine (hemisulfate). This product is intended for research and analytical applications. Berberine hemisulfate is the hemisulfate form of Berberine (HY-N0716). Berberine hemisulfate is an alkaloid isolated from the Chinese herbal medicine Huanglian. Berberine hemisulfate exhibits anti-inflammatory, antibiobic, antitumor, cardiovascular protective and neuroprotective activity.

Z-Asp(OMe)-Gln-Met-Asp(OMe)-FMK is an inhibitor for caspase-3, and inhibits Dihydroartemisinin (HY-N0176) and Dictamnine (HY-N0849) co-induced apoptosis.

BTX306 is a cereblon-targeting molecular glue degrader. BTX306 reduces myeloma cell viability and induces apoptosis. BTX306 overcomes myeloma cell resistance to Lenalidomide (HY-A0003) or Bortezomib (HY-10227). BTX306 is active against primary myeloma cells, and shows efficacy in vivo. BTX306 can be used for myeloma research.

9-cis-Canthaxanthin is a carotenoid with pro-apoptotic activity in THP-1 macrophage cells. 9-cis-Canthaxanthin induces cell apoptosis by increasing caspase-3 and caspase-8 activity.

Tetracaine (hydrochloride) (Standard) is the analytical standard of Tetracaine (hydrochloride). This product is intended for research and analytical applications. Tetracaine hydrochloride (Amethocaine hydrochloride) is a calcium channel protein inhibitor and blocks voltage-sensitive release of Ca2+ from sarcoplasmic reticulum. Tetracaine hydrochloride is mainly used topically in ophthalmology and as an antipruritic.

Multitarget AD-IN-8 is a blood-brain barrier-penetrant, orally active multitarget inhibitor. Multitarget AD-IN-8 inhibits abnormal Tau phosphorylation at Thr181 and Ser396 sites and attenuates NF-κB phosphorylation. Multitarget AD-IN-8 downregulates BACE1 expression to reduce Aβ production, inhibits the Bax/Bcl-2 pathway, and suppresses Caspase-1 activation. Multitarget AD-IN-8 attenuates p38, ERK1/2, and JNK phosphorylation and inhibits Aβ_25-35-induced Apoptosis. Multitarget AD-IN-8 exhibits neuroprotective effects against Aβ_25-35-induced injury, ameliorates learning and memory deficits in AD mouse models, and alleviates hippocampal neuronal pathological damage. Multitarget AD-IN-8 can be used for research on Alzheimer's disease.

NLRP3-IN-81 (N102) is a BBB-penetrable inhibitor against NLRP3 inflammasome-dependent pyroptosis with an EC₅₀ of 0.029 μM against cell pyroptosis induced by Nigericin (HY-127019). NLRP3-IN-81 potently inhibits NLRP3-dependent activation of caspase-1 and the release of IL-1β. NLRP3-IN-81 disturbs the interaction of NLRP3 with the adaptor protein ASC and inhibits ASC oligomerization. NLRP3-IN-81 can be used for pyroptosis-related diseases research, such as inflammatory bowel diseases and type 2 diabetes.

NLRP3-IN-87 is a selective and orally active NLRP3 inhibitor with a K_d of 0.23 μM. NLRP3-IN-87 binds directly to the NLRP3 NACHT domain, disrupts NLRP3-NEK7 and NLRP3-ASC interactions, inhibits ASC oligomerization, and blocks inflammasome assembly. NLRP3-IN-87 suppresses caspase-1 activation and IL-1β secretion. NLRP3-IN-87 exhibits anti-inflammatory and analgesic activity, reducing joint swelling, inflammation, and pain in an MSU (HY-B2130A)-induced acute gout mouse model. NLRP3-IN-87 can be used for the research of gout.

Z-VAD-FMK is a pan-caspase inhibitor and also an ICE-like protease inhibitor, which inhibits apoptosis by preventing the processing of CPP32 to its active form. Z-VAD-FMK sensitivity varies primarily due to differential expression of receptor-interacting protein 1 (RIP1). Z-VAD-FMK limits the cryopreservation-induced apoptosis by reducing caspase-3 activity of in vitro produced bovine embryos. Z-VAD-FMK is immunosuppressive in vitro and inhibits T cell proliferation without blocking the processing of caspase-8 and caspase-3. Z-VAD-FMK leads to a decrease in intracellular glutathione (GSH) with a concomitant increase in reactive oxygen species (ROS) levels in activated T cells. Z-VAD-FMK is due to oxidative stress via the depletion of GSH. Z-VAD-FMK can be used for the study of acute pancreatitis.

TZ3O is an anticholinergic agent with neuroprotective effects. TZ3O inhibits acetylcholinesterase (AChE) activity in human plasma with an IC₅₀ of 304.5 μM. TZ3O can improve memory impairment and cognitive decline in rats in the Scopolamine (HY-N0296)-induced Alzheimer-type model. TZ3O could be used in Alzheimer’s research.

Casp9 Rat Pre-designed siRNA Set A contains three designed siRNAs for Casp9 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

Z-VAD-CHO is a potent inhibitor of human caspase-1 with a K_i value of 0.008 μM.

Ac-ATS010-KE is a selective polypeptide inhibitor of caspase-3. Ac-ATS010-KE protects cells from FasL-induced apoptosis. The unmethylated form of Ac-ATS010-KE exhibits better cell viability than the fully methylated form. Ac-ATS010-KE can be used in research on cancers such as colorectal cancer and the development of caspase-3-targeted molecular probes.

GPR is a three amino acid peptide. GPR can rescue cultured rat hippocampal neurons from Aβ-induced neuronal death by inhibiting caspase-3/p53 dependent apoptosis. GPR can be used for the research of Alzheimer's disease (AD).