1. Cell Cycle/DNA Damage
    Epigenetics
  2. HDAC
  3. Domatinostat tosylate

Domatinostat tosylate (Synonyms: 4SC-202)

Cat. No.: HY-16012 Purity: 98.81%
Handling Instructions

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).

For research use only. We do not sell to patients.

Domatinostat tosylate Chemical Structure

Domatinostat tosylate Chemical Structure

CAS No. : 1186222-89-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 164 In-stock
Estimated Time of Arrival: December 31
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
10 mg USD 180 In-stock
Estimated Time of Arrival: December 31
50 mg USD 540 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1020 Get quote
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Based on 2 publication(s) in Google Scholar

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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).

IC50 & Target

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)

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].

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].

Clinical Trial
Molecular Weight

619.71

Formula

C₃₀H₂₉N₅O₆S₂

CAS No.

1186222-89-8

SMILES

O=C(NC1=CC=CC=C1N)/C=C/C2=CN(S(=O)(C3=CC=C(C4=CN(C)N=C4)C=C3)=O)C=C2.O=S(C5=CC=C(C)C=C5)(O)=O

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 51 mg/mL (82.30 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6137 mL 8.0683 mL 16.1366 mL
5 mM 0.3227 mL 1.6137 mL 3.2273 mL
10 mM 0.1614 mL 0.8068 mL 1.6137 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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Product Name:
Domatinostat tosylate
Cat. No.:
HY-16012
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