4SC-202|4SC202|cas 1186222-89-8|DC Chemicals

Cas No.:	1186222-89-8
Chemical Name:	(E)-N-(2-aminophenyl)-3-(1-((4-(1-methyl-1H-pyrazol-4-yl)phenyl)sulfonyl)-1H-pyrrol-3-yl)acrylamide
Synonyms:	4SC-202;4SC 202;Domatinostat tosylate;Domatinostat;(E)-N-(2-aminophenyl)-3-(1-((4-(1-methyl-1H-pyrazol-4-yl)phenyl)sulfonyl)-1H-pyrrol-3-yl)acrylamide;264ARM7UXX;4SC202;(E)-N-(2-aminophenyl)-3-[1-[4-(1-methylpyrazol-4-yl)phenyl]sulfonylpyrrol-3-yl]prop-2-enamide;BCP18522;BDBM50470579;s7555;DB13101;SB16852;4SC 202 free base;4SC202 free base
SMILES:	S(C1C([H])=C([H])C(C2C([H])=NN(C([H])([H])[H])C=2[H])=C([H])C=1[H])(N1C([H])=C([H])C(/C(/[H])=C(\[H])/C(N([H])C2=C([H])C([H])=C([H])C([H])=C2N([H])[H])=O)=C1[H])(=O)=O
Formula:	C₂₃H₂₁N₅O₃S
M.Wt:	447.5095
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	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:	Oral gavage of Domatinostat tosylate inhibits HT-29 xenograft growth in nude mice, and when combined with oxaliplatin, its activity is further strengthened[2].
In Vitro:	Domatinostat tosylate significantly reduces proliferation of all epithelial and mesenchymal UC cell lines (IC50 0.15-0.51 μM), inhibits clonogenic growth and induces caspase activity[1]. Domatinostat tosylate provokes apoptosis activation in CRC cells, while caspase inhibitors (z-VAD-CHO and z-DVED-CHO) significantly alleviate Domatinostat tosylate-exerted cytotoxicity in CRC cells. Meanwhile, Domatinostat tosylate induces dramatic G2-M arrest in CRC cells. Further studies show that AKT activation might be an important resistance factor of Domatinostat tosylate. Domatinostat tosylate-induced cytotoxicity is dramatically potentiated with serum starvation, AKT inhibition (by perifosine or MK-2206), or AKT1-shRNA knockdown in CRC cells. On the other hand, exogenous expression of constitutively active AKT1 (CA-AKT1) decreases the sensitivity by Domatinostat tosylate in HT-29 cells. Notably, Domatinostat tosylate, at a low concentration, enhances oxaliplatin-induced in vitro anti-CRC activity[2]. Domatinostat tosylate treatment induces potent cytotoxic and proliferation-inhibitory activities against established HCC cell lines (HepG2, HepB3, SMMC-7721) and patient-derived primary HCC cells. Domatinostat tosylate induces apoptosis signal-regulating kinase 1 (ASK1) activation, causing it translocation to mitochondria and physical association with Cyp-D[3].
References:	[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.

Cat. No.	Product name	Field of application
DC70802	SS-208	SS-208 (SS208) is a novel potent, selective inhibitor of histone deacetylase 6 (HDAC6) with IC50 of 12 nM, >100-fold selectivity over HDAC1/4/5/7/8/9/11.SS-208 has minimal effects on the viability of murine SM1 melanoma cells in vitro, significantly reduced in vivo tumor growth in a murine SM1 syngeneic melanoma mouse model.
DC3110	CUDC-907 (PI3K/HDAC InhibitorI)	CUDC-907 (PI3K/HDAC Inhibitor I) is a dual PI3K and HDAC inhibitor for PI3Kɑ, HDAC1, HDAC2, HDAC3 and HDAC10 with IC50 of 19 nM, 1.7 nM, 5 nM, 1.8 nM and 2.8 nM, respectively.
DC8252	Vorinostat (SAHA)	Vorinostat (SAHA) is an HDAC1/3 inhibitor with IC50 of ~10 nM.
DC8663	UF010	UF010 is a potent and selective HADC inhibitor with IC50 ~0.06 μM, 0.1 μM, 0.5 μM and 1.5 μM for HDACs 3, 2, 1 and 8, respectively. It has > 6-fold selectivity over other HDACs.
DC6303	Tubastatin A HCl	Tubastatin A is a potent and selective HDAC6 inhibitor with IC50 of 15 nM. It is selective against all the other isozymes (1000-fold) except HDAC8 (57-fold).
DC6304	Tubastatin A	Tubastatin A is a potent and selective HDAC6 inhibitor with IC50 of 15 nM. It is selective against all the other isozymes (1000-fold) except HDAC8 (57-fold).
DC5178	Tubacin (BML-GR362)	Tubacin is a selective inhibitor of HDAC6 via inhibition of the second deacetylase domain (DD2).
DC8134	Trichostatin A (TSA)	Trichostatin A (TSA) is a selective and potent HDAC inhibitor with IC50 of ~1.8 nM; HDAC8 is the only known member of the HDAC-family that is not affected by TSA.
DC7716	TMP269	TMP269 is a novel and selective class IIa histone deacetylase inhibitor with IC50s of 126/80/36/9 nM for HDAC 4/5/7/9, respectively; 20-400 fold selectivity over class1 HDACs.
DC10210	TMP195	TMP195 is the most potent and selective class IIa HDAC inhibitor.