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Domatinostat tosylate

Catalog No. T4477   CAS 1186222-89-8
Synonyms: 4SC-202 tosylate, 4SC-202

Domatinostat tosylate (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).

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Domatinostat tosylate Chemical Structure
Domatinostat tosylate, CAS 1186222-89-8
Pack Size Availability Price/USD Quantity
1 mg In stock $ 41.00
2 mg In stock $ 59.00
5 mg In stock $ 97.00
10 mg In stock $ 147.00
25 mg In stock $ 267.00
50 mg In stock $ 443.00
100 mg In stock $ 653.00
1 mL * 10 mM (in DMSO) In stock $ 133.00
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Purity: 100%
Purity: 96.93%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Domatinostat tosylate (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).
Targets&IC50 HDAC1:1.2 μM, HDAC10:21 μM, HDAC11:9.7 μM, HDAC3:0.57 μM, HDAC5:11.3 μM, HDAC2:1.12 μM
In vitro 4SC-202 provokes apoptosis activation in CRC cells, while caspase inhibitors (z-VAD-CHO and z-DVED-CHO) significantly alleviate 4SC-202-exerted cytotoxicity in CRC cells. Meanwhile, 4SC-202 induces dramatic G2-M arrest in CRC cells. Further studies show that AKT activation might be an important resistance factor of 4SC-202. 4SC-202-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 4SC-202 in HT-29 cells. Notably, 4SC-202, at a low concentration, enhances oxaliplatin-induced in vitro anti-CRC activity[2]. 4SC-202 obviously reduces the proliferation of all epithelial and mesenchymal UC cell lines (IC50: 0.15-0.51 μM), inhibits clonogenic growth and induces caspase activity[1]. 4SC-202 treatment induces potent cytotoxic and proliferation-inhibitory activities against established HCC cell lines (HepG2, HepB3, SMMC-7721) and patient-derived primary HCC cells. 4SC-202 induces apoptosis signal-regulating kinase 1 (ASK1) activation, causing it translocation to mitochondria and physical association with Cyp-D[3].
In vivo 4SC-202 (i.g.) inhibits HT-29 xenograft growth in nude mice, and when combined with oxaliplatin, its activity is further strengthened[2].
Synonyms 4SC-202 tosylate, 4SC-202
Molecular Weight 619.71
Formula C30H29N5O6S2
CAS No. 1186222-89-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL

H2O: Insoluble

( < 1 mg/ml refers to the product slightly soluble or insoluble )

TargetMolReferences and Literature

1. Pinkerneil M, Hoffmann M J, Kohlhof H, et al. Evaluation of the Therapeutic Potential of the Novel Isotype Specific HDAC Inhibitor 4SC-202 in Urothelial Carcinoma Cell Lines[J]. Targeted Oncology, 2016, 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.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Anti-Cancer Active Compound Library Chromatin Modification Compound Library Clinical Compound Library Histone Modification Compound Library DNA Damage & Repair Compound Library Anti-Breast Cancer Compound Library Drug Repurposing Compound Library Bioactive Compounds Library Max

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Keywords

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