BSJ-5-63
Based on 1 publication(s) in Google Scholar
BSJ-5-63 is a potent CDK12, CDK7, CDK9 PROTAC 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.
(Pink: CDK12 and CDK7 and CDK9 ligand (HY-150948); Blue: VHL ligand (HY-112078); Black: linker (HY-W140827)).
For research use only. We do not sell to patients.
- Purity : 99.97%
- CAS No.: 2519823-37-9
- Formula: C52H74ClN9O6S2
- Molecular Weight:1020.78
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Storage:
Store at room temperature 3 years.
In solvent -80°C, 2 years , -20°C, 1 year
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) BSJ-5-63
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Biological Activity
Description
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. Further protocols information, click here.
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Cell Line:LNCaP, C4-2B, 22Rv1 cells
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Concentration:62.5, 125, 250, 500, 1000 nM
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Incubation Time:8 h
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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.
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Cell Line:LNCaP, C4-2B, 22Rv1 cells
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Concentration:62.5, 125, 250, 500, 1000 nM
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Incubation Time:8, 16, 24 h
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Result:Decreased the mRNA expression of BRCA1, BRCA2 in a dose and time dependent manner.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:4-5 weeks, Male ICR-SCID mice (22Rv1 cells)[1]
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Dosage:50 mg/kg
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Administration:I.p.; daily for 12 days
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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.
Chemical Information
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CAS No. 2519823-37-9
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Appearance Solid
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Molecular Weight 1020.78
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Formula C52H74ClN9O6S2
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Color White to off-white
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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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Store at room temperature 3 years
In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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bioRxiv
2025 Nov 21:2025.11.20.689563. PMID: 41332615
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (97.96 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocols
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RT-PCR
Reverse transcription technology uses RNA as a template to synthesize DNA. RT-PCR is simple, specific and sensitive, and can be used to detect gene expression levels and expression differences in cells; detect RNA virus content; clone cDNA sequences of specific genes.
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RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
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Western Blot
Western blotting (WB) is a commonly used experimental method in molecular biology, biochemistry, and immunogenetics for identifying and quantifying target proteins. It combines gel electrophoresis with immunoassay, enabling researchers to analyze protein expression, post-translational modifications, and molecular weight.
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Real Time qPCR (Q-PCR)
Real-time quantitative PCR (qPCR) quantifies an amplifiable nucleic-acid target by monitoring fluorescence during PCR cycling rather than measuring product only after amplification. The increase in fluorescence tracks accumulation of PCR product, and the quantification cycle (Cq; historically also Ct/CP) is related to the initial amount of target: samples containing more starting target generally reach the defined fluorescence threshold in fewer cycles.
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Protocol For Protein Expression And Purification
Recombinant protein expression in Escherichia coli followed by purification of a His-tagged soluble protein by immobilized metal affinity chromatography (IMAC), with optional MBP fusion and TEV tag removal when the construct includes these elements. The biological readout is production of the encoded target protein, detected as an inducible band at the expected molecular mass by SDS-PAGE and quantified by total protein assay or chromatographic absorbance; the purification readout is enrichment of the target protein in elution fractions after selective binding of polyhistidine residues to immobilized Ni2+/metal-chelate resin and elution by imidazole-containing buffer. Expression is driven by an inducible bacterial expression system, commonly T7/lac-based, in which IPTG or lactose/auto-induction activates transcription and translation of the cloned gene; lower induction temperature, lower inducer concentration, induction timing, and solubility-enhancing fusion tags can influence the frac
Purity & Documentation
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Data Sheet (272 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 0.9796 mL | 4.8982 mL | 9.7964 mL | 24.4911 mL |
| 5 mM | 0.1959 mL | 0.9796 mL | 1.9593 mL | 4.8982 mL | |
| 10 mM | 0.0980 mL | 0.4898 mL | 0.9796 mL | 2.4491 mL | |
| 15 mM | 0.0653 mL | 0.3265 mL | 0.6531 mL | 1.6327 mL | |
| 20 mM | 0.0490 mL | 0.2449 mL | 0.4898 mL | 1.2246 mL | |
| 25 mM | 0.0392 mL | 0.1959 mL | 0.3919 mL | 0.9796 mL | |
| 30 mM | 0.0327 mL | 0.1633 mL | 0.3265 mL | 0.8164 mL | |
| 40 mM | 0.0245 mL | 0.1225 mL | 0.2449 mL | 0.6123 mL | |
| 50 mM | 0.0196 mL | 0.0980 mL | 0.1959 mL | 0.4898 mL | |
| 60 mM | 0.0163 mL | 0.0816 mL | 0.1633 mL | 0.4082 mL | |
| 80 mM | 0.0122 mL | 0.0612 mL | 0.1225 mL | 0.3061 mL |
BSJ-5-63 Related Classifications
HY-162706 Related Classifications
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