1. Vitamin D Related/Nuclear Receptor Apoptosis
  2. Androgen Receptor Apoptosis
  3. CSRM617

CSRM617 is a selective small-molecule inhibitor of the transcription factor ONECUT2 (OC2, a master regulator of androgen receptor) with a Kd of 7.43 uM in SPR assays, binding to OC2-HOX domain directly. CSRM617 induces apoptosis by appearance of cleaved Caspase-3 and PARP. CSRM617 is well tolerated in the prostate cancer mouse model

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (CSRM617 hydrochloride) usually boasts enhanced water solubility and stability.

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

CSRM617 Chemical Structure

CSRM617 Chemical Structure

CAS No. : 787504-88-5

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Description

CSRM617 is a selective small-molecule inhibitor of the transcription factor ONECUT2 (OC2, a master regulator of androgen receptor) with a Kd of 7.43 uM in SPR assays, binding to OC2-HOX domain directly. CSRM617 induces apoptosis by appearance of cleaved Caspase-3 and PARP. CSRM617 is well tolerated in the prostate cancer mouse model[1]

In Vitro

CSRM617 (0.01-100 μM; 48 hours) inhibits cell growth in several PC cell lines: PC-3, 22RV1, LNCaP, C4-2 cells[1].
CSRM617 (10-20 μM; 48 hours) induces apoptosis in 22Rv1 cells results in cell death in a concentration-dependent fashion[1].
CSRM617 (20 μM; 72 hours) induces apoptosis in 22Rv1 cells by appearance of cleaved Caspase-3 and PARP[1].

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

Molecular Weight

255.23

Formula

C10H13N3O5

CAS No.
SMILES

O=C(C(CO)N)N/N=C/C1=CC=C(C(O)=C1O)O

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Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
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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.

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CSRM617
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HY-122611
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