产品号 #100-0536_C
抑制半胱天冬酶-3和半胱天冬酶-7
总览
Ac-DEVD-CHO是一种合成肽醛，具有PARP裂解位点DEVD，可被半胱天冬酶识别（Nicholson et al.）。Ac-DEVD-CHO阻断PARP的裂解活性，并以可逆的方式抑制半胱天冬酶-3 （Ki = 0.23 nM）和半胱天冬酶-7 (Ki = 1.6 nM) (Garcia-Calvo et al.；Talanianet al.)。这种抑制作用是通过醛基团与这些半胱天冬酶的活性位点半胱氨酸的相互作用实现的（Thornberry et al.）。半胱天冬酶抑制剂用于研究半胱天冬酶的活化和凋亡。本产品作为该分子的三氟乙酸盐供应。
癌症研究
·阻断喜树碱诱导的骨肿瘤细胞凋亡（Nicholson et al.）。
别名
N‑乙酰Asp‑Glu‑Val‑Asp‑CHO
细胞类型
癌细胞及细胞系
研究领域
癌症
化学式
C20H30N4O11 • XCF3COOH
分子量
502.5 克/摩尔
纯度
≥ 95 %
Protocols and Documentation
Find supporting information and directions for use in the Product Information Sheet or explore additional protocols below.
Resources and Publications
Educational Materials (3)
Publications (3)
Inhibition of human caspases by peptide-based and macromolecular inhibitors. The Journal of biological chemistry 1998 dec
Abstract
Studies with peptide-based and macromolecular inhibitors of the caspase family of cysteine proteases have helped to define a central role for these enzymes in inflammation and mammalian apoptosis. A clear interpretation of these studies has been compromised by an incomplete understanding of the selectivity of these molecules. Here we describe the selectivity of several peptide-based inhibitors and the coxpox serpin CrmA against 10 human caspases. The peptide aldehydes that were examined (Ac-WEHD-CHO, Ac-DEVD-CHO, Ac-YVAD-CHO, t-butoxycarbonyl-IETD-CHO, and t-butoxycarbonyl-AEVD-CHO) included several that contain the optimal tetrapeptide recognition motif for various caspases. These aldehydes display a wide range of selectivities and potencies against these enzymes, with dissociation constants ranging from 75 pM to {\textgreater}10 microM. The halomethyl ketone benzyloxycarbonyl-VAD fluoromethyl ketone is a broad specificity irreversible caspase inhibitor, with second-order inactivation rates that range from 2.9 x 10(2) M-1 s-1 for caspase-2 to 2.8 x 10(5) M-1 s-1 for caspase-1. The results obtained with peptide-based inhibitors are in accord with those predicted from the substrate specificity studies described earlier. The cowpox serpin CrmA is a potent (Ki {\textless} 20 nM) and selective inhibitor of Group I caspases (caspase-1, -4, and -5) and most Group III caspases (caspase-8, -9, and -10), suggesting that this virus facilitates infection through inhibition of both apoptosis and the host inflammatory response.
Substrate specificities of caspase family proteases. The Journal of biological chemistry 1997 apr
Abstract
The caspase family represents a new class of intracellular cysteine proteases with known or suspected roles in cytokine maturation and apoptosis. These enzymes display a preference for Asp in the P1 position of substrates. To clarify differences in the biological roles of the interleukin-1beta converting enzyme (ICE) family proteases, we have examined in detail the specificities beyond the P1 position of caspase-1, -2, -3, -4, -6, and -7 toward minimal length peptide substrates in vitro. We find differences and similarities between the enzymes that suggest a functional subgrouping of the family different from that based on overall sequence alignment. The primary specificities of ICE homologs explain many observed enzyme preferences for macromolecular substrates and can be used to support predictions of their natural function(s). The results also suggest the design of optimal peptidic substrates and inhibitors.
Identification and inhibition of the ICE/CED-3 protease necessary for mammalian apoptosis. Nature 1995 jul
Abstract
The protease responsible for the cleavage of poly(ADP-ribose) polymerase and necessary for apoptosis has been purified and characterized. This enzyme, named apopain, is composed of two subunits of relative molecular mass (M(r)) 17K and 12K that are derived from a common proenzyme identified as CPP32. This proenzyme is related to interleukin-1 beta-converting enzyme (ICE) and CED-3, the product of a gene required for programmed cell death in Caenorhabditis elegans. A potent peptide aldehyde inhibitor has been developed and shown to prevent apoptotic events in vitro, suggesting that apopain/CPP32 is important for the initiation of apoptotic cell death.
更多信息
| Molecular Weight | 502.5 g/mol |
|---|---|
| Alternative Names | N-Ac-Asp-Glu-Val-Asp-CHO |
| Chemical Formula | C20H30N4O11 • XCF3COOH |
| Purity | ≥ 95% |
PRODUCTS ARE FOR RESEARCH USE ONLY AND NOT INTENDED FOR HUMAN OR ANIMAL DIAGNOSTIC OR THERAPEUTIC USES UNLESS OTHERWISE STATED. FOR ADDITIONAL INFORMATION ON QUALITY AT STEMCELL, REFER TO WWW.STEMCELL.COM/COMPLIANCE.
