Domatinostat

Domatinostat (4SC-202 free base) is a selective class I HDAC inhibitor with IC50 of 1.20 μM, 1.12 μM, and 0.57 μM for HDAC1, HDAC2, and HDAC3, respectively. It also displays inhibitory activity against Lysine specific demethylase 1 (LSD1) .

Product Specifications

CAS Number

[910462-43-0]

Product Name Alternative

4SC-202 (free base)

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Apoptosis; HDAC

Type

Reference compound

Related Pathways

Apoptosis; Cell Cycle/DNA Damage; Epigenetics

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/4SC-202-free-base.html

Purity

99.34

Solubility

DMSO : ≥ 58 mg/mL

Smiles

O=C(NC1=CC=CC=C1N)/C=C/C2=CN(S(=O)(C3=CC=C(C4=CN(C)N=C4)C=C3)=O)C=C2

Molecular Formula

C23H21N5O3S

Molecular Weight

447.51

Precautions

H302, H315, H319, H335

References & Citations

[1]Pinkerneil M, et al. Evaluation of the Therapeutic Potential of the Novel Isotype Specific HDAC Inhibitor 4SC-202 in Urothelial Carcinoma Cell Lines. Target Oncol. 2016 Dec;11 (6) :783-798.|[2]Zhijun H, et al. Pre-clinical characterization of 4SC-202, a novel class I HDAC inhibitor, against colorectal cancer cells. Tumour Biol. 2016 Aug;37 (8) :10257-67.|[3]Fu M, et al. 4SC-202 activates ASK1-dependent mitochondrial apoptosis pathway to inhibit hepatocellular carcinoma cells. Biochem Biophys Res Commun. 2016 Mar 4;471 (2) :267-73|[4]S.W.Henning, et al. Preclinical characterization of 4SC-202, a noval isotype specific HDAC inhibitor.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Scientific Category

Reference compound1

Clinical Information

Phase 2

Isoform

HDAC1; HDAC10; HDAC11; HDAC2; HDAC3; HDAC5; HDAC9

Citation 01

J Mol Med (Berl) . 2019 Aug;97 (8) :1183-1193.|Proc Natl Acad Sci U S A. 2019 Feb 19;116 (8) :2961-2966. |Am J Transl Res. 2020 Jun 15;12 (6) :2968-2983.