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名称

Capzimin

分子类型

小分子

别名

卡普西明

英文名称

Capzimin

货号

C649839-5mg

包装规格

5mg

浓度

≥99%

储存温度

-20°C储存

运输条件

超低温冰袋运输

产品介绍

Capzimin is a potent and moderately specific proteasome isopeptidase Rpn11 inhibitor. In Vitro Capzimin (3027) shows 80-fold selectivity for Rpn11 over Csn5, 10-fold over AMSH and 6-fold over BRCC36 (IC 50 =30 μM, 4.5 μM and 2.3 μM respectively. Capzimin is screened against the NCI panel of 60 cancer cell lines. The median GI 50 is 3.3 μM. Capzimin exhibits promising activity in leukemia cells including the SR and K562 cell lines (GI 50 values of 0.67 μM and 1 μM respectively), as well as several solid tumor cell lines including NCI-H460 (non-small cell lung cancer; GI 50 = 0.7 μM) and MCF7 (breast cancer; GI 50 =1.0 μM). Immunoblotting for the processed form of caspase 3 and caspase-cleaved poly ADP-ribose polymerase in HCT116 cells confirm that Capzimin not only blocks cell growth, but also induces apoptosis. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:Target: Rpn11

生化机理

Capzimin 是一种强效、中等特异性的蛋白酶体异肽酶 Rpn11 抑制剂。

CAS号

2084868-04-0

分子式

C30H24N6O2S4

分子量

628.81 g/mol

PubChem编号

126599606

Isomeric SMILES

C1=CC2=CC(=CN=C2C(=C1)SSC3=CC=CC4=CC(=CN=C43)C(=O)NCCC5=NC=CS5)C(=O)NCCC6=NC=CS6

IIUPAC Name

N-[2-(1,3-thiazol-2-yl)ethyl]-8-[[3-[2-(1,3-thiazol-2-yl)ethylcarbamoyl]quinolin-8-yl]disulfanyl]quinoline-3-carboxamide

INCHI

1S/C30H24N6O2S4/c37-29(33-9-7-25-31-11-13-39-25)21-15-19-3-1-5-23(27(19)35-17-21)41-42-24-6-2-4-20-16-22(18-36-28(20)24)30(38)34-10-8-26-32-12-14-40-26/h1-6,11-18H,7-10H2,(H,33,37)(H,34,38)

InChi Key

RNEOHKZPZKEZCQ-UHFFFAOYSA-N

Smiles

C1=CC2=CC(=CN=C2C(=C1)SSC3=CC=CC4=CC(=CN=C43)C(=O)NCCC5=NC=CS5)C(=O)NCCC6=NC=CS6

PubChem CID

126599606

溶解性

DMSO : ≥ 55.67 mg/mL (88.53 mM)

氢键供体数Hydrogen Bond Donor Count

氢键受体数Hydrogen Bond Acceptor Count

可旋转键计数Rotatable Bond Count

精确质量Exact Mass

628.084 Da

单同位素质量Monoisotopic Mass

628.084 Da

拓扑极表面积Topological Polar Surface Area

217.000 Å²

重原子数Heavy Atom Count

形式电荷Formal Charge

复杂度Complexity

834.000

同位素原子数Isotope Atom Count

共价键合单元计数Covalently-Bonded Unit Count

XLogP3

5.200

RIDADR

NONHforallmodesoftransport

Safety

「No Dangerous Attributes」

「No upstream and downstream information yet」

Technical Documents

「No technical documents」

Articles

「No related articles yet」

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