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

Domatinostat (Synonyms: 4SC-202 free base)

Cat. No.: HY-16012A Purity: 99.08%
Handling Instructions

Domatinostat (4SC-202 free base) 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 Chemical Structure

Domatinostat Chemical Structure

CAS No. : 910462-43-0

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1  mL in DMSO USD 132 In-stock
Estimated Time of Arrival: December 31
5 mg USD 120 In-stock
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10 mg USD 180 In-stock
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50 mg USD 540 In-stock
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100 mg USD 1020 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 4 publication(s) in Google Scholar

Other Forms of Domatinostat:

Top Publications Citing Use of Products

    Domatinostat purchased from MCE. Usage Cited in: Am J Transl Res. 2020 Jun 15;12(6):2968-2983.

    Western blot analyzes that the expression levels of LSD1, HDAC1/2/3, BCL-2 and CDK1 proteins are decreased and the expression levels of H3K4me2, AC-H3, cleavage caspase3/9, BAX, and p21 proteins are significantly increased by 4SC-202.
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    Description

    Domatinostat (4SC-202 free base) 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[4]

    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 (4SC-202 free base) 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 (4SC-202 free base) tosylate provokes apoptosis activation in CRC cells, while caspase inhibitors (z-VAD-CHO and z-DVED-CHO) significantly alleviate Domatinostat (4SC-202 free base) tosylate-exerted cytotoxicity in CRC cells. Meanwhile, Domatinostat (4SC-202 free base) 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 (4SC-202 free base) 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 (4SC-202 free base) tosylate, at a low concentration, enhances oxaliplatin-induced in vitro anti-CRC activity[2]. Domatinostat (4SC-202 free base) 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 (4SC-202 free base) 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 (4SC-202 free base) inhibits HT-29 xenograft growth in nude mice, and when combined with oxaliplatin, its activity is further strengthened[2].

    Clinical Trial
    Molecular Weight

    447.51

    Formula

    C₂₃H₂₁N₅O₃S

    CAS No.

    910462-43-0

    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

    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 : ≥ 58 mg/mL (129.61 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.2346 mL 11.1729 mL 22.3459 mL
    5 mM 0.4469 mL 2.2346 mL 4.4692 mL
    10 mM 0.2235 mL 1.1173 mL 2.2346 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (5.59 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (5.59 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References

    Purity: 99.08%

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    Keywords:

    Domatinostat4SC-202HDACApoptosisHistone deacetylasesInhibitorinhibitorinhibit

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