BS-181
Based on 7 publication(s) in Google Scholar
BS-181 is a potent and selective CDK7 inhibitor (IC50=21 nM) than Seliciclib (HY-30237). BS-181 is also against CDK2, CDK5 and CDK9 with IC50 values of 880, 3000 and 4200 nM, respectively (fails to block CDK1, 4 and 6). BS-181 inhibits a panel of cancer cells growth (IC50=11.5 μM-37.3 μM) and induces cell apoptosis. BS-181 has the potential for the research of cancer therapy.
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- Purity: 95.47%
- CAS No.: 1092443-52-1
- 화학식: C22H32N6
- 분자량:380.53
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Apoptosis Compound Library
HY-L003
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Cell Cycle/DNA Damage Compound Library
HY-L004
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Kinase Inhibitor Library
HY-L009
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Anti-Cancer Compound Library
HY-L025
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Anti-Aging Compound Library
HY-L034
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Anti-Breast Cancer Compound Library
HY-L074
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Anti-Pancreatic Cancer Compound Library
HY-L077
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Anti-Blood Cancer Compound Library
HY-L079
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Cancer Stem Cells Compound Library
HY-L135
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Heterocyclic Compound Library
HY-L138
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Highly Selective Inhibitors Library
HY-L158
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Highly Selective Activators Library
HY-L159
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Cell Death Library
HY-L162
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Serine/Threonine Kinase Inhibitor Library
HY-L164
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Anti-Hematopathy Compound Library
HY-L171
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Anti-Ovarian Cancer Compound Library
HY-L173
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Multi-Target Compound Library
HY-L176
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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Anti-Brain Cancer Compound Library
HY-L188
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Protein Kinase Compound Library
HY-L196
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Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
HY-L199
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Cell Proliferation Compound Library
HY-L201
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High-Throughput Bioactive Compound Library
HY-L205
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High-Efficiency Gene Editing Compound Library
HY-L244
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RNA Binding Bioactive Compound Library
HY-L248
Publications Citing Use of MedChemExpress (MCE) BS-181
More- Theranostics. 2017 Apr 20;7(7):1914-1927. [Abstract]
- Int J Biol Macromol. 2024 Dec 27:139117. [Abstract]
- Cell Rep. 2017 Dec 5;21(10):2796-2812. [Abstract]
- Virulence. 2026 Dec;17(1):2629100. [Abstract]
- Biochem Biophys Res Commun. 2019 Jun 11;513(4):967-973. [Abstract]
- Res Sq. 2025 Dec 18.
- Universidade de Lisboa. 2021 Dec 21.
Customer Validation & Images
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WB
Biological Activity
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CDK7/CycH/MAT1 0.021 μM (IC50) |
CDK2/Cyc E 0.88 μM (IC50) |
CDK5/p35NCK 3 μM (IC50) |
CDK9/cycT 4.2 μM (IC50) |
CDK1/cycB 8.1 μM (IC50) |
CDK4/Cyc D1 33 μM (IC50) |
CDK6/cycD1 47 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| BT-549 | IC50 |
12.82 μM
Compound: 1
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Growth inhibition of human BT-549 cells assessed as cell viability measured after 4 days by WST8 assay
Growth inhibition of human BT-549 cells assessed as cell viability measured after 4 days by WST8 assay
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[PMID: 34538051] |
| MDA-MB-231 | IC50 |
18.47 μM
Compound: 1
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Growth inhibition of human MDA-MB-231 cells assessed as cell viability measured after 4 days by WST8 assay
Growth inhibition of human MDA-MB-231 cells assessed as cell viability measured after 4 days by WST8 assay
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[PMID: 34538051] |
| MDA-MB-468 | IC50 |
16.3 μM
Compound: 1
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Growth inhibition of human MDA-MB-468 cells assessed as cell viability measured after 4 days by WST8 assay
Growth inhibition of human MDA-MB-468 cells assessed as cell viability measured after 4 days by WST8 assay
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[PMID: 34538051] |
| Sf9 | IC50 |
1.8 μM
Compound: BS-181
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Inhibition of CDK2/Cyclin E (unknown origin) expressed in sf9 cells using histone H1 as substrate in presence of [gamma33P]-ATP
Inhibition of CDK2/Cyclin E (unknown origin) expressed in sf9 cells using histone H1 as substrate in presence of [gamma33P]-ATP
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[PMID: 26851505] |
| Sf9 | IC50 |
14 μM
Compound: BS-181
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Inhibition of CDK1/Cyclin B (unknown origin) expressed in baculoviral infected insect Sf9 cells using histone H1 as substrate in presence of [gamma-33P]ATP
Inhibition of CDK1/Cyclin B (unknown origin) expressed in baculoviral infected insect Sf9 cells using histone H1 as substrate in presence of [gamma-33P]ATP
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[PMID: 26741853] |
BS-181 (0-40 μM; 72 hours) inhibits cancer cells growth, it is against Breast cancer cell lines growth with IC50 values ranging from 15.1 μM to 20 μM, it is against Colorectal cancer cell lines growth with IC50 values ranging from 11.5 μM to15.3 μM and is against lung, osteosarcoma, prostate and liver cancer cell lines with IC50 values ranging from 11.5 μM to 37.3 μM, respectively[1].BS-181 (0-50 μM; 4 hours) shows inhibition of phosphorylation of the RNA polymerase II C-terminal domain (CTD) at serine 5 (P-Ser5). It down-regulates CDK4 and cyclin D1 expression while does not effect other CDKs and cyclins[1].BS-181 (0-50 μM; 24 hours) shows an increase in cells in G1, accompanied by a reduction in cell numbers in S and G2/M at low concentrations. At higher concentrations, however, cells accumulates in the sub-G1, indicative of apoptosis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Breast cancer cell line: MCF-7, MDA-MB-231, T47D, ZR-75-1, etcColorectal cancer cell line: COLO-205, HCT-116, HCT-116 (p53-/-)Lung cancer cell line: A549, NCI-460Osteosarcoma cancer cell line: U2OS, SaOS2Prostate cancer cell line: PC3, LNCaP
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Concentration:0-50 μM
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Incubation Time:4 hours
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Result:Had anti-proliferative activities against a panel of cell lines, including breast, lung, prostate and colorectal cancer.
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Cell Line:MCF-7 cells
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Concentration:0-40 μM
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Incubation Time:72 hours
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Result:Inhibited phosphorylation of CDK7 substrates.
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Cell Line:MCF-7 cells
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Concentration:0-50 μM
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Incubation Time:24 hours
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Result:Led cells to G1 arrest and apoptosis.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:7-week old female nu/nu-BALB/c athymic nude mice with MCF-7 cells[1]
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Dosage:5 mg/kg or 10 mg/kg; 10 mg/kg or 20 mg/kg
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Administration:Intraperitoneal injection; twice daily or once total daily; 14 days
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Result:Inhibited tumor growth significantly.
Chemical Information
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CAS No. 1092443-52-1
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Appearance Solid
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분자량 380.53
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화학식 C22H32N6
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Color White to off-white
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SMILES
CC(C1=C(N=C(C=C2NCC3=CC=CC=C3)NCCCCCCN)N2N=C1)C
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (7)
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Journal Impact Factor
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Most Recent
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Theranostics
Triptolide Inhibits the AR Signaling Pathway to Suppress the Proliferation of Enzalutamide Resistant Prostate Cancer Cells. [Abstract]2017 Apr 20;7(7):1914-1927. PMID: 28638477
BS-181 purchased from MedChemExpress. Usage Cited in: Theranostics. 2017 Apr 20;7(7):1914-1927. [Abstract]
Effect of TPL on the levels of pAR S515 and related proteins in PCa cells. LNCaP and C4-2/AR-V7 cells are pretreated with TPL or BS-181 for 1 h, and then incubated with R1881 for 4 h.
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Int J Biol Macromol
CDK2-based CDK7 mimic as a tool for structural analysis: Biochemical validation and crystal structure with SY5609. [Abstract]2024 Dec 27:139117. PMID: 39733900 -
Cell Rep
Melanoma Therapeutic Strategies that Select against Resistance by Exploiting MYC-Driven Evolutionary Convergence. [Abstract]2017 Dec 5;21(10):2796-2812. PMID: 29212027 -
Virulence
The cyclin dependent kinase (CDK)7 inhibitor BS-181 inhibits pathogenic Cryptococcus species, causing G2/M arrest and a splicing defect. [Abstract]2026 Dec;17(1):2629100. PMID: 41701636 -
Biochem Biophys Res Commun
2019 Jun 11;513(4):967-973. PMID: 31005255 -
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용액&용해도
DMSO : ≥ 50 mg/mL (131.40 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 3 mg/mL (7.88 mM); Clear solution
This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 3 mg/mL (7.88 mM); Clear solution
This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
순도&문서
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Data Sheet (279 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)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Ali S et al. The development of a selective cyclin-dependent kinase inhibitor that shows antitumor activity. Cancer Res. 2009 Aug 1;69(15):6208-15. [Content Brief]
[2]. Wang BY, et al. Selective CDK7 inhibition with BS-181 suppresses cell proliferation and induces cell cycle arrest and apoptosis in gastric cancer. Drug Des Devel Ther. 2016 Mar 16;10:1181-9. [Content Brief]
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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6279 mL | 13.1396 mL | 26.2791 mL | 65.6978 mL |
| 5 mM | 0.5256 mL | 2.6279 mL | 5.2558 mL | 13.1396 mL | |
| 10 mM | 0.2628 mL | 1.3140 mL | 2.6279 mL | 6.5698 mL | |
| 15 mM | 0.1752 mL | 0.8760 mL | 1.7519 mL | 4.3799 mL | |
| 20 mM | 0.1314 mL | 0.6570 mL | 1.3140 mL | 3.2849 mL | |
| 25 mM | 0.1051 mL | 0.5256 mL | 1.0512 mL | 2.6279 mL | |
| 30 mM | 0.0876 mL | 0.4380 mL | 0.8760 mL | 2.1899 mL | |
| 40 mM | 0.0657 mL | 0.3285 mL | 0.6570 mL | 1.6424 mL | |
| 50 mM | 0.0526 mL | 0.2628 mL | 0.5256 mL | 1.3140 mL | |
| 60 mM | 0.0438 mL | 0.2190 mL | 0.4380 mL | 1.0950 mL | |
| 80 mM | 0.0328 mL | 0.1642 mL | 0.3285 mL | 0.8212 mL | |
| 100 mM | 0.0263 mL | 0.1314 mL | 0.2628 mL | 0.6570 mL |
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