For research purposes only

Cat. No BA119944940

Availability Please, check stock availability.

Description of biological activity

Potent and reversible inhibitor of Caspase-1 and Caspase-4. In an assay [US2009/68105 A1, 2009] the compound displayed IC50 8.1 nm/l for Caspase-1. Strongly inhibits anti-Fas induced apoptosis in L929 Fas cells. In vitro reversible inhibitor of interleukin-1β-converting enzyme (ICE) from THP-1 cells. In an assay, the compound inhibited mouse fibroblast taxotere induced cell death (the cells were pretreated with 600 μmol/l of the compound for 2 h then treated with 1E-2 -1E4 ng/ml taxotere for 24 h and cell viability measured with MTT assay and Hoechst 33342 staining procedures; control cells were pretreated with DMSO then treated with taxotere).

Keywords: Anti-cancer

TECHNICAL INFORMATION

L-709049, Ac-Tyr-Val-Ala-Asp-aldehyde potent and reversible inhibitor of Caspase-1 and Caspase-4.

IUPAC Name: L-709049, Ac-Tyr-Val-Ala-Asp-aldehyde

CAS Number: 143313-51-3

Purity: > 96% chemical purity (LCMS)
> 95% de

REFERENCES

1. Bioorg. Med.Chem.Lett.1992, 2, 613-618
2. Biochemistry 1998, 37, 8508-8515
3. J. Biol. Chem.,1998, 273, 32608-32613
4. J. Biol. Chem.,1997, 272, 17907-17911
5. Biochemistry,1994, 33, 3934-3940
6. Trends Biochem. Sci.,1997, 22, 299-306 (review on caspases)

Latest added compounds

5-(4-Hydroxy-4-methyl-isoxazolidine-2-carbonyl)-1-isopropyl-3-methyl-6-(3-methyl-5-trifluoromethyl-1H-pyrazol-4-ylmethyl)-1H-thieno[2,3-d]pyrimidine-2,4-dione

Selective inhibitor of MCT1 with a binding affinity of 1.6 nM, is 6 fold selective over MCT2 and does not inhibit MCT4 at 10 μM. Both lactate transport and cell growth are potently inhibited.

Anti-cancer

Inhibitors

 
5-(4-chlorophenyl)-N-{[2-(2,2,2-trifluoroethoxy)pyridin-3-yl]methyl}pyridine-3-carboxamide

selective inhibitor of Nav1.8 sodium channel (IC50 = 3 nM); for TRPV1, P2X2/3, Cav2.2 calcium channels, KCNQ2/3 potassium channels IC50 >10 µM

Analgesic

Inhibitors

 
1-[4-chloro-3-(trifluoromethyl)benzenesulfonyl]-4-[4-(5-methyl-1H-pyrazol-1-yl)benzoyl]piperazine

inhibitor of ubiquitin ligase Smad ubiquitination regulatory factor-1 (Smuf1)

Bone disorders

Inhibitors