Ivaltinostat

Ivaltinostat (CG-200745) is an orally active, potent pan-HDAC inhibitor which has the hydroxamic acid moiety to bind zinc at the bottom of catalytic pocket. Ivaltinostat inhibits deacetylation of histone H3 and tubulin. Ivaltinostat induces the accumulation of p53, promotes p53-dependent transactivation, and enhances the expression of MDM2 and p21 (Waf1/Cip1) proteins. Ivaltinostat enhances the sensitivity of Gemcitabine-resistant cells to Gemcitabine (HY-16138) and 5-Fluorouracil (5-FU; HY-90006) . Ivaltinostat induces apoptosis and has anti-tumour effects[1][2][3][4].

Product Specifications

CAS Number

[936221-33-9]

Product Name Alternative

CG-200745

UNSPSC

12352005

Target

Apoptosis; HDAC; MDM-2/p53

Type

Reference compound

Related Pathways

Apoptosis; Cell Cycle/DNA Damage; Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/cg-200745.html

Solubility

10 mM in DMSO

Smiles

O=C(NCCCN(C)C)/C(COC1=C2C=CC=CC2=CC=C1)=C/CCCCC(NO)=O

Molecular Formula

C24H33N3O4

Molecular Weight

427.54

References & Citations

[1]Oh ET, et al. Novel histone deacetylase inhibitor CG200745 induces clonogenic cell death by modulating acetylation of p53 in cancer cells. Invest New Drugs. 2012 Apr;30 (2) :435-42.|[2]Hwang JJ, et al. A novel histone deacetylase inhibitor, CG200745, potentiates anticancer effect of docetaxel in prostate cancer via decreasing Mcl-1 and Bcl-XL. Invest New Drugs. 2012 Aug;30 (4) :1434-42.|[3]Chun SM, et al. Epigenetic modulation with HDAC inhibitor CG200745 induces anti-proliferation in non-small cell lung cancer cells. PLoS One. 2015 Mar 17;10 (3) :e0119379.|[4]Choi HS, et al. Histone deacetylase inhibitor, CG200745 attenuates renal fibrosis in obstructive kidney disease. Sci Rep. 2018 Aug 1;8 (1) :11546.|[5]Dawoon E Jung, et al. CG200745, an HDAC inhibitor, induces anti-tumour effects in cholangiocarcinoma cell lines via miRNAs targeting the Hippo pathway. Sci Rep. 2017 Sep 7;7 (1) :10921.