[CAS NO. 593273-05-3] DCH36_06
PRODUCTS SPECIFICATIONS [593273-05-3]
DESCRIPTION [593273-05-3]
Overview
| MDL | MFCD03864746 |
|---|---|
| Molecular Weight | 372.83 |
| Molecular Formula | C18H13ClN2O3S |
| SMILES | O=C(/C(C(N1C2=CC=C(C)C(Cl)=C2)=O)=C\C=C\C3=CC=CO3)NC1=S |
Summary
DCH36_06 is a potent and selective p300/CBP inhibitor with IC 50 s 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. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 125 mg/mL ( 335.27 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.6822 mL | 13.4109 mL | 26.8219 mL |
| 5 mM | 0.5364 mL | 2.6822 mL | 5.3644 mL |
| 10 mM | 0.2682 mL | 1.3411 mL | 2.6822 mL |
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1.
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2.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: 2.08 mg/mL (5.58 mM); Suspended solution; Need ultrasonic
