1. Cell Cycle/DNA Damage
  2. CDK
  3. BSJ-5-63

BSJ-5-63 is a potent CDK12, CDK7, CDK9 degrader. BSJ-5-63 BSJ-5-63 decreases the protein expression of CDK12, CDK7, CDK9, RNAPII, Cyclin K. BSJ-5-63 decreases the mRNA expression of BRCA1, BRCA2. BSJ-5-63 shows anticancer activity and has the potential for the research of prostate cancer.

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

BSJ-5-63 Chemical Structure

BSJ-5-63 Chemical Structure

CAS No. : 2519823-37-9

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Description

BSJ-5-63 is a potent CDK12, CDK7, CDK9 degrader. BSJ-5-63 BSJ-5-63 decreases the protein expression of CDK12, CDK7, CDK9, RNAPII, Cyclin K. BSJ-5-63 decreases the mRNA expression of BRCA1, BRCA2. BSJ-5-63 shows anticancer activity and has the potential for the research of prostate cancer[1].

IC50 & Target[1]

CDK12

 

CDK7

 

CDK9

 

In Vitro

BSJ-5-63 (0-1000 nM; 8 h) decreases the protein expression of CDK12, CDK7, CDK9, RNAPII, Cyclin K in a dose-dependent manner[1].
BSJ-5-63 (0-1000 nM; 8, 16, 24 h) decreases the mRNA expression of BRCA1, BRCA2 in a dose and time dependent manner[1].

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

Western Blot Analysis[1]

Cell Line: LNCaP, C4-2B, 22Rv1 cells
Concentration: 62.5, 125, 250, 500, 1000 nM
Incubation Time: 8 h
Result: Decreased the protein expression of CDK12, CDK7, CDK9, P-RNAPII Ser2, P-RNAPII Ser5, P-RNAPII Ser7, RNAPII, Cyclin K in a dose-dependent manner.

RT-PCR[1]

Cell Line: LNCaP, C4-2B, 22Rv1 cells
Concentration: 62.5, 125, 250, 500, 1000 nM
Incubation Time: 8, 16, 24 h
Result: Decreased the mRNA expression of BRCA1, BRCA2 in a dose and time dependent manner.
In Vivo

BSJ-5-63 (50 mg/kg; i.p.; daily for 12 days) shows anticancer activity in mice[1].

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

Animal Model: 4-5 weeks, Male ICR-SCID mice (22Rv1 cells)[1]
Dosage: 50 mg/kg
Administration: I.p.; daily for 12 days
Result: Significantly inhibited the growth of 22Rv1 tumors and tumor weight was significantly reduced and increased in the number of apoptotic cells, daily administration resulted in approximately 10% weight loss in mice.
Molecular Weight

1020.78

Formula

C52H74ClN9O6S2

CAS No.
SMILES

O=S(C1=CC=CC=C1NC2=NC(N[C@H]3CN(CCCCCCCCCCC(N[C@@H](C(C)(C)C)C(N4C[C@H](O)C[C@H]4C(N[C@@H](C)C5=CC=C(C6=C(C)N=CS6)C=C5)=O)=O)=O)CCC3)=NC=C2Cl)(C(C)C)=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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Product Name:
BSJ-5-63
Cat. No.:
HY-162706
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