4SC-202, HDAC/LSD1 Dual Inhibitor

Overview
Catalog #	bs-60230c-2-mg-solid
Product Name	4SC-202, HDAC/LSD1 Dual Inhibitor
Specifications
Storage Buffer	Powder
Storage Condition	Powder: 4C for 1 year.
Target
Product Information	Molecular Weight: 619.71 Formula: C30 H29 N5 O6 S2 CAS Number: 1186222-89-8 InChi Key: IAVXAZDVNICKFJ-ICSBZGNSSA-N InChi: InChI=1S/C23H21N5O3S.C7H8O3S/c1-27-16-19(14-25-27)18-7-9-20(10-8-18)32(30,31)28-13-12-17(15-28)6-11-23(29)26-22-5-3-2-4-21(22)24;1-6-2-4-7(5-3-6)11(8,9)10/h2-16H,24H2,1H3,(H,26,29);2-5H,1H3,(H,8,9,10)/b11-6+; Smiles: CN1C=C(C=N1)C1C=CC(=CC=1)S(=O)(=O)N1C=C(/C=C/C(=O)NC2C=CC=CC=2N)C=C1.CC1C=CC(=CC=1)S(O)(=O)=O Purity: 98.0 Solubility: DMSO up to 50 mM Appearance: Solid powder Shelf Life: 5.0 years
Description	4SC-202 is a potent, selective and orally bioavailable HDAC/LSD1 dual Inhibitor. It inhibits class I HDAC with IC50 of 1.20µM, 1.12 µM, and 0.57µM for HDAC1, HDAC2, and HDAC3, respectively. It also displays inhibitory activity against Lysine specific demethylase 1 (LSD1). 4SC-202 has very high selectivity over ClassIIa/IIb/III HDACs. In HeLa cells, it induces hyperacetylation of histone H3 with EC50 of 1.1 µM. It induces a G2/M cell cycle arrest by interfering with the normal development of the mitotic spindle and causing collapsed spindle apparatus and multiple nucleation centres. In addition, 4SC-202 shows a broad anti-proliferative activity towards human cancer cell lines with a mean IC50 of 0.7 µM. In vivo it shows pronounced and robust anti-tumor activity in both A549 NSCLC xenograft and RKO27 colon carcinoma model. Currently it is in phase I trials for patients with advanced haematological tumours.