Description
Capzimin is a potent and moderately specific proteasome isopeptidase Rpn11 inhibitor.
Product information
CAS Number: 2084868-04-0
Molecular Weight: 628.81
Formula: C30H24N6O2S4
Chemical Name: N-[2-(1,3-thiazol-2-yl)ethyl]-8-[(3-{[2-(1,3-thiazol-2-yl)ethyl]carbamoyl}quinolin-8-yl)disulfanyl]quinoline-3-carboxamide
Smiles: O=C(NCCC1=NC=CS1)C1=CC2=CC=CC(SSC3C=CC=C4C=C(C=NC4=3)C(=O)NCCC3=NC=CS3)=C2N=C1
InChiKey: RNEOHKZPZKEZCQ-UHFFFAOYSA-N
InChi: 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)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : ≥ 55.67 mg/mL (88.53 mM).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
Capzimin (3027) shows 80-fold selectivity for Rpn11 over Csn5, 10-fold over AMSH and 6-fold over BRCC36 (IC50=30 μM, 4.5 μM and 2.3 μM respectively. Capzimin is screened against the NCI panel of 60 cancer cell lines. The median GI50 is 3.3 μM. Capzimin exhibits promising activity in leukemia cells including the SR and K562 cell lines (GI50 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; GI50= 0.7 μM) and MCF7 (breast cancer; GI50=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.
Products are for research use only. Not for human use.
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