CA-074 methyl ester (CA-074 Me)

半胱氨酸蛋白酶抑制剂

10mM in DMSO

CAS编号: 147859-80-1(DMSO)
分子式: C₁₉H₃₁N₃O₆
分子量: 397.47

有货

库存信息

关闭

货号 (SKU)	包装规格	是否现货	价格	数量
C408263-1ml	1ml	现货

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Compound libraries (12332)

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基本描述

英文别名	Cathepsin B Inhibitor IV \| L-Proline, N-[[(2S,3S)-3-[(propylamino)carbonyl]-2-oxiranyl]carbonyl]-L-isoleucyl-, methyl ester
规格或纯度	10mM in DMSO
英文名称	CA-074 methyl ester (CA-074 Me)
生化机理	CA-074 甲酯（CA-074 Me，Cathepsin B 抑制剂 IV）是 CA-074 的一种膜渗透性衍生物，是一种不可逆的 cathepsin B 抑制剂。
储存温度	-80℃储存
运输条件	超低温冰袋运输
产品介绍	CA-074 methyl ester 是CA-074的细胞渗透性类似物，可作为不可逆的组织蛋白酶B抑制剂。据报道，CA-074甲酯在啮齿动物模型中抑制骨再吸收，并显示出在体外抑制B16黑素瘤细胞的侵袭。介绍： CA-074 methyl ester 是一种特异性的 Cathepsin B 抑制剂，具有保护神经，抗癌、抗炎等多种生物活性。用途：使用CA-074甲酯用作心肌细胞、HeLa细胞和胰腺癌PANC-1细胞中的组织蛋白酶B抑制剂。 Information CA-074 methyl ester (CA-074 Me) CA-074 methyl ester (CA-074 Me, Cathepsin B Inhibitor IV) is a membrane-permeable derivative of CA-074 and acts as an irreversible cathepsin B inhibitor. In vitro CA-074Me is able to inhibit cathepsin L within living HL-60 cells and bloodstream forms of Trypanosoma brucei brucei, but does not inhibit cathepsin L in the absence of thiols. CA-074Me is converted into CA-074 by intracellular esterasesand is, therefore, able to inhibit cathepsin B in GSH-depleted HL-60 cell. It is suggested that CA-074 rather than CA-074Me should be used to selectively inhibit cathespsin B within living cells. Myotube size and number and induced levels of fusion-related creatine phosphokinase activity and myosin heavy-chain protein are reduced from 30 to 50% in CA074Me-treated myoblasts. These reductions are also dose related. Micromolar concentrations of CA074Me inhibit catB activity in differentiating myoblasts. In vivo Administration of CA074Me to the London APP mice results in significant improvement in memory deficit, reduces amyloid plaque load in brain, reduces levels of Aβ40 and Aβ42 in brain, and reduces C-terminal β-secretase fragment (CTFβ) derived from APP by β-secretase when compared with untreated control animals. It has no effect on any of these parameters in mice expressing the Swe mutant β-secretase site of APP (in Swedish/London APP mice). In vivo icv administration of CA074Me to normal guinea pigs results in substantial reduction of brain Aβ levels and inhibits β-secretase activity. Cell Data cell lines：Cultured human mast cells (CHMC) Concentrations：100 μM Incubation Time：2 h Powder Purity:≥99%

产品属性

ALogP	0.484
hba_count	6
HBD Count	2
Rotatable Bond	10

关联靶点（人）

CTSB Tchem 组织蛋白酶B(Cathepsin B) (1 活性数据)

点击查看靶蛋白信息： CTSB

活性类型	活性值-log(M)	作用机制	期刊	参考文献(PubMed IDs)

名称和识别符

分子类型	小分子
Canonical SMILES	CCCNC(=O)C1OC1C(=O)NC(C(C)CC)C(=O)N2CCCC2C(=O)OC
分子量	397.47
Reaxy-Rn	25187464
Reaxys-RN link address	https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=25187464&ln=

化学和物理性质

溶解性	Solubility (25°C) In vitro DMSO: 100 mg/mL (109.38 mM); Ethanol: 100 mg/mL (109.38 mM); Water: Insoluble;
DMSO(mg / mL) Max Solubility	79
DMSO(mM) Max Solubility	198.76
Water(mg / mL) Max Solubility	79
Water(mM) Max Solubility	198.76