CRA-026440

Research use only, not for human use.

CRA-026440(PCI-34051) is a highly potent HDAC inhibitor with inhibitory effects on HDAC1, HDAC2, HDAC3, HDAC6, HDAC8 and HDAC10 with Ki values of 4,14,11,15,7 and 20 nM, respectively.

CRA-026440 is a potent, broad-spectrum HDAC inhibitor. The Ki values against recombinant HDAC isoenzymes HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, and HDAC10 are 4, 14, 11, 15, 7, and 20 nM respectively. CRA-026440 shows antitumor and antiangiogenic activities. CRA-026440 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Western Blot Analysis Cell Line:HCT116 cells Concentration:0.1 μM, 0.5 μM, 1 μM, 5 μM, 10 μM Incubation Time:18 hours Result:Resulted in the accumulation of both acetylated histones and acetylated tubulin. Induced expression of the cyclin-dependent kinase inhibitor p21Cip1/WAF1.

Animal Model:HCT-116 tumor-bearing nude mice Dosage:100 mg/kg Administration:i.v.; daily; for three consecutive daysResult:Resulted in a statistically significant reduction in tumor growth.

——

Cell Cycle/DNA Damage

HDAC

HDAC

——

——

847460-34-8

420.46

C23H24N4O4

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (237.83 mM; Ultrasonic )

O=C(NO)C1=CC=C(C#CCNC(=O)C2=CC=3C=C(OCCN(C)C)C=CC3N2)C=C1

——

(-20℃)

With Ice Pack

≥ 2 years