4SC-202 tosylate

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

4SC-202 是 HDAC1/2/3 的 I 类 HDAC 选择性抑制剂（IC50：1.20/1.12/0.57 μM）。它还对赖氨酸特异性脱甲基酶 1 (LSD1) 具有抑制活性。

4SC-202 is a selective inhibitor of class I HDAC for HDAC1/2/3 (IC50: 1.20/1.12/0.57 μM). It also displays inhibitory activity against Lysine-specific demethylase 1 (LSD1).

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. 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. 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.

Oral gavage of Domatinostat tosylate inhibits HT-29 xenograft growth in nude mice, and when combined with oxaliplatin, its activity is further strengthened.

4SC-202

Metabolic Enzyme/Protease

Phosphatase

HDAC1|HDAC2|HDAC3|HDAC5|HDAC9|HDAC10|HDAC11|

Cancer

——

1186222-89-8

619.71

C30H29N5O6S2

>98% (HPLC)

DMSO : ≥ 51 mg/mL. 82.30 mM

CC1=CC=C(C=C1)S(=O)(=O)O.CN1C=C(C=N1)C2=CC=C(C=C2)S(=O)(=O)N3C=CC(=C3)/C=C/C(=O)NC4=CC=CC=C4N

——

(-20℃)

With Ice Pack

≥ 2 years