1. Epigenetics
    Apoptosis
  2. Histone Acetyltransferase
    Apoptosis
  3. DCH36_06

DCH36_06 

Cat. No.: HY-139108
Handling Instructions

DCH36_06 is a potent and selective p300/CBP inhibitor with IC50s of 0.6 μM and 3.2 μM for p300 and CBP, respectively. DCH36_06 mediated p300/CBP inhibition leading to hypoacetylation on H3K18 in leukemic cells. Anti-tumor activity.

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

DCH36_06 Chemical Structure

DCH36_06 Chemical Structure

CAS No. : 593273-05-3

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Description

DCH36_06 is a potent and selective p300/CBP inhibitor with IC50s of 0.6 μM and 3.2 μM for p300 and CBP, respectively. DCH36_06 mediated p300/CBP inhibition leading to hypoacetylation on H3K18 in leukemic cells. Anti-tumor activity[1].

In Vitro

DCH36_06 (6.7-20 μM; 24-48 hours) treatment arrests cell cycle at G1 phase and induces apotosis in a dose-dependent manner in leukemic cells[1].
DCH36_06 (5-10 μM; 24 hours) treatment significantly activates the cleavage of pro-caspase 3, pro-caspase 9 and PARP1 at dose-dependent manner[1].
DCH36_06 shows potent antiproliferative activity against tested leukemia cell lines (CEM, MOLT3, MOLT4, Jurkat, MV4-11, THP-1, RS4; 11, KOPN8, Kasumi-1 and K562 cells) in a dose-dependent manner with IC50 values at single-digit micromolar range[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis[1]

Cell Line: MV4-11 cells
Concentration: 6.7 μM, 20 μM
Incubation Time: 24 hours, 48 hours
Result: Dose-dependently arrested cell cycle at G1 phase.

Apoptosis Analysis[1]

Cell Line: MV4-11 cells
Concentration: 6.7 μM, 20 μM
Incubation Time: 24 hours, 48 hours
Result: Significantly induced apoptosis.

Western Blot Analysis[1]

Cell Line: MV4-11 cells
Concentration: 5 μM, 10 μM
Incubation Time: 24 hours
Result: Significantly activated the cleavage of pro-caspase 3, pro-caspase 9 and PARP1 at dose-dependent manner.
In Vivo

DCH36_06 (25-50 mg/kg; intraperitoneal injection; every two days; for 20 days) blocks the leukemic xenograft growth in mice[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: MV4-11 xenograft nude mice[1]
Dosage: 25 mg/kg, 50 mg/kg
Administration: Intraperitoneal injection; every two days; for 20 days
Result: The tumor growth rate showed significant reduction in dose-dependent manner.
Molecular Weight

372.83

Formula

C₁₈H₁₃ClN₂O₃S

CAS No.
SMILES

O=C(/C(C(N1C2=CC=C(C)C(Cl)=C2)=O)=C\C=C\C3=CC=CO3)NC1=S

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Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

DCH36_06Histone AcetyltransferaseApoptosisHATsHATp300CBPanti-tumorhypoacetylationantiproliferativeInhibitorinhibitorinhibit

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DCH36_06
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HY-139108
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