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| | 4SC-202 Basic information |
| Product Name: | 4SC-202 | | Synonyms: | 4SC-202;4SC-202 2-Propenamide, N-(2-aminophenyl)-3-[1-[[4-(1-methyl-1H-pyrazol-4-yl)phenyl]sulfonyl]-1H-pyrrol-3-yl]-, (2E)-, 4-methylbenzenesul;(E)-N-(2-aminophenyl)-3-(1-((4-(1-methyl-1H-pyrazol-4-yl)phenyl)sulfonyl)-1H-pyrrol-3-yl)acrylamide 4-methylbenzenesulfonate;4SC-202 tosylate;CS-1272;Domatinostat tosylate;4SC-202;4SC202;4SC 202;Domatinostat tosylate,Domatinostat,Apoptosis,inhibit,Histone deacetylases,Inhibitor,HDAC | | CAS: | 1186222-89-8 | | MF: | C30H29N5O6S2 | | MW: | 619.71116 | | EINECS: | | | Product Categories: | | | Mol File: | 1186222-89-8.mol |  |
| | 4SC-202 Chemical Properties |
| storage temp. | Store at -20°C | | solubility | insoluble in H2O; ≥2.4 mg/mL in EtOH with gentle warming and ultrasonic; ≥62 mg/mL in DMSO | | form | Powder | | color | Light yellow to brown |
| | 4SC-202 Usage And Synthesis |
| Description | 4SC-202 is an inhibitor of the class I histone deacetylases (HDACs) HDAC1-3 and the histone demethylase KDM1A. It reduces cell viability in a panel of colorectal cancer (CRC) cell lines when used at concentrations ranging from 1 to 10 μM and in patient-derived CRC cell lines when used at a concentration of 5 μM. 4SC-202 (5 μM) induces cell cycle arrest at the G2/M phase in HT-29 cells and primary human CRC cells and increases apoptosis in HT-29 cells in a concentration-dependent manner, an effect that is enhanced by the Akt inhibitors perifosine and MK-2206 . 4SC-202 (100 mg/kg, p.o., every other day) reduces tumor growth in an HT-29 mouse xenograft model when administered alone and to an enhanced degree when co-administered with oxaliplatin (Item No. 13106). | | Uses | Domatinostat tosylate (4SC-202) 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). | | in vivo | studies, 4sc-202 has shown a good tolerability and dose-dependent effect on anti-tumour activity compared with other inhibitors in the a549nsclc xenograft model and the rko27 colon carcinoma model [1]. | | IC 50 | HDAC-3: 0.57 μM (IC50); HDAC-2: 1.12 μM (IC50); HDAC-1: 1.2 μM (IC50); HDAC-11: 9.7 μM (IC50); HDAC-5: 11.3 μM (IC50); HDAC-10: 21 μM (IC50); HDAC-9: 50 μM (IC50) | | references | [1] henning s w, doblhofer r, kohlhof h, et al. 178 preclinical characterization of 4sc-202, a novel isotype specific hdac inhibitor[j]. european journal of cancer supplements, 2010, 8(7): 61. |
| | 4SC-202 Preparation Products And Raw materials |
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