2. Metabolic Enzyme/Protease Apoptosis
  3. Phosphatase MDM-2/p53
  4. BRD6257

BRD6257 is an orally active inhibitor for protein phosphatase, Mg2+/Mn2+ dependent 1D PPM1D with an IC50 of 5 nM. BRD6257 activates p53 signaling pathway with an EC50 of 51 nM, increases the p21 expression, inhibits the proliferation of cancer cell MOLM13 (IC50=2.8 μM). BRD6257 exhibits good metabolic stability in human and rat liver microsomes.

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BRD6257

BRD6257 Chemical Structure

Size Price Stock Quantity
5 mg Get quote 5 - 7 weeks 4 - 6 weeks 6 - 8 weeks 4 - 6 weeks
10 mg Get quote 5 - 7 weeks 4 - 6 weeks 6 - 8 weeks 4 - 6 weeks
25 mg Get quote 5 - 7 weeks 4 - 6 weeks 6 - 8 weeks 4 - 6 weeks
50 mg Get quote 5 - 7 weeks 4 - 6 weeks 6 - 8 weeks 4 - 6 weeks
100 mg   Get quote  
200 mg   Get quote  
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Based on 1 publication(s) in Google Scholar

BRD6257 Related Antibodies

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Description

BRD6257 is an orally active inhibitor for protein phosphatase, Mg2+/Mn2+ dependent 1D PPM1D with an IC50 of 5 nM. BRD6257 activates p53 signaling pathway with an EC50 of 51 nM, increases the p21 expression, inhibits the proliferation of cancer cell MOLM13 (IC50=2.8 μM). BRD6257 exhibits good metabolic stability in human and rat liver microsomes[1].

Parmacokinetics
Species Dose Route C0 T1/2 CL Vdss AUC Cmax Tmax AUC0-inf Bioavailability
Mice[1] 1 mg/kg i.v. 4664 ng/mL 0.8 h 5.4 mL/min/kg 0.29 L/kg 3085 ng·h/mL / / / /
Mice[1] 10 mg/kg p.o. / 0.89 h / / / 145 ng/mL 1.3 h 366 ng·h/mL 12 %
Molecular Weight

550.53

Formula

C24H22F4N6O3S
SMILES

FC(F)C1=CC=C(NC([C@@H](NC2=NN3C(C=C(N=C3S2)C4=NC=C(C)O4)=O)CC5CCC(F)(C5)F)=O)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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BRD6257 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BRD6257BRD 6257BRD-6257PhosphataseMDM-2/p53MOLM13orally activeInhibitorinhibitorinhibit

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