2. Cell Cycle/DNA Damage
  3. CDK
  4. BSJ-01-175

BSJ-01-175 

Cat. No.: HY-145072 Purity: 99.45%
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BSJ-01-175 is a potent and selective CDK12/13 covalent inhibitor. BSJ-01-175 demonstrates exquisite selectivity, potent inhibition of RNA polymerase II phosphorylation, and downregulation of CDK12-targeted genes in cancer cells.

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

BSJ-01-175 Chemical Structure

BSJ-01-175 Chemical Structure

CAS No. : 2227392-55-2

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Based on 1 publication(s) in Google Scholar

BSJ-01-175 Related Antibodies

Top Publications Citing Use of Products

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Description

BSJ-01-175 is a potent and selective CDK12/13 covalent inhibitor. BSJ-01-175 demonstrates exquisite selectivity, potent inhibition of RNA polymerase II phosphorylation, and downregulation of CDK12-targeted genes in cancer cells[1].

IC50 & Target

CDK12

 

CDK13

 

In Vitro

BSJ-01–175 (0-10 μM; 72 hours) causes a 5-fold increase in cell viability compared to the wild type (WT), indicating strong dependence on covalent bond formation with Cys1039[1].
BSJ-01–175 (0-10 μM; 72 hours) slightly decreases the activity of TC71 Ewing sarcoma cells compared to THZ531[1].
BSJ-01–175 (0-5 μM) specifically targets CDK12/13 and suppresses the transcription of BRAC1 and BRAC2[1].

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

BSJ-01-175 Related Antibodies

Cell Viability Assay[1]

Cell Line: Kelly wild type or CDK12C1039F cells
Concentration: 0-10 μM
Incubation Time: 72 hours
Result: Observed a 5-fold increase in cell viability compared to the wild type (WT), indicating strong dependence on covalent bond formation with Cys1039.

Cell Proliferation Assay[1]

Cell Line: TC71 Ewing sarcoma cells
Concentration: 0-10 μM
Incubation Time: 72 hours
Result: Slightly decreased the activity compared to THZ531.
In Vivo

BSJ-01–175 (10 mg/kg; i.p.; daily for 3 weeks) leads to a significant suppression of tumor growth throughout 3 weeks of drug treatment period[1].
Assessment of Pharmacokinetics (PK) profile of BSJ-01-175 in mouse[1].

Route Dose (mg/kg) Tmax (h) Cmax (ng/mL) AUClast (h•ng/mL) T1/2 (h) CL (mL/min/kg) VSS (L/kg) F (%)
IV 3 1511 1832 2.2 24.9 3.9
PO 10 2 272 1043 17

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

Animal Model: Female nude mice (BALB/c, 7-8 weeks) bearing TC71 Ewing sarcoma cells[1]
Dosage: 10 mg/kg
Administration: i.p.; daily for 3 weeks
Result: Led to a significant suppression of tumor growth throughout 3 weeks of drug treatment period.
Molecular Weight

545.08

Appearance

Solid

Formula

C30H33ClN6O2
CAS No.
SMILES

ClC1=CN=C(N[C@H]2C[C@@H](CCC2)OC3=CC=C(C=C3)NC(/C=C/CN(C)C)=O)N=C1C4=CNC5=CC=CC=C45
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation
References
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BSJ-01-175 Related Classifications

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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Keywords:

BSJ-01-1752227392-55-2CDKCyclin dependent kinaseCDK12/13RNA polymerase II phosphorylationanti-cancerselectivecovalentEwing sarcomaInhibitorinhibitorinhibit

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