BS-181 hydrochloride
Based on 7 publication(s) in Google Scholar
BS-181 hydrochloride is a highly selective CDK7 inhibitor with IC50 of 21 nM, and > 40-fold selective for CDK7 than CDK1, 2, 4, 5, 6, or 9.
For research use only. We do not sell to patients.
- Purity: 99.93%
- CAS No.: 1397219-81-6
- Formula: C22H33ClN6
- Molecular Weight:416.99
-
Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Protocol
- Purity & Documentation
- References
-
Help & FAQs
-
Cell Cycle/DNA Damage Compound Library
HY-L004
-
Kinase Inhibitor Library
HY-L009
-
Anti-Cancer Compound Library
HY-L025
-
Anti-Aging Compound Library
HY-L034
-
Anti-Breast Cancer Compound Library
HY-L074
-
Anti-Pancreatic Cancer Compound Library
HY-L077
-
Anti-Blood Cancer Compound Library
HY-L079
-
Targeted Diversity Library
HY-L099
-
Cancer Stem Cells Compound Library
HY-L135
-
Highly Selective Inhibitors Library
HY-L158
-
Serine/Threonine Kinase Inhibitor Library
HY-L164
-
Anti-Hematopathy Compound Library
HY-L171
-
Anti-Ovarian Cancer Compound Library
HY-L173
-
Multi-Target Compound Library
HY-L176
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Bioactive Compound Library
HY-L001
-
Anti-Brain Cancer Compound Library
HY-L188
-
Protein Kinase Compound Library
HY-L196
-
Cell Proliferation Compound Library
HY-L201
-
High-Throughput Bioactive Compound Library
HY-L205
-
Posttranslational Modification Library
HY-L226
-
High-Efficiency Gene Editing Compound Library
HY-L244
-
RNA Binding Bioactive Compound Library
HY-L248
Publications Citing Use of MedChemExpress (MCE) BS-181 hydrochloride
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
-
WB
Biological Activity
|
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) |
BS-181 promotes cell cycle arrest and inhibits cancer cell growth, and growth is inhibited for all cell lines tested, with IC50 values ranging from 11.5 to 37 μM. BS-181 inhibits RB phosphorylation at Ser795 and Ser821 with an apparent IC50 of 15 μM, similar to the IC50 obtained for P-Ser2 inhibition. BS-181 treatment of MCF-7 cells leads to G1 arrest at and apoptosis[1]. BS-181 inhibits GC cell and normal gastric epithelial RGM-1 cell line growth with inhibitory concentration (IC50) ranging from 17 to 22 μM and 6.5 μM, respectively. BS-181 significantly inhibits cell migration and invasion ability in a dose-dependent manner[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS No. 1397219-81-6
-
Appearance Solid
-
Molecular Weight 416.99
-
Formula C22H33ClN6
-
Color White to off-white
-
SMILES
CC(C1=C(N=C(C=C2NCC3=CC=CC=C3)NCCCCCCN)N2N=C1)C.[H]Cl
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
Publications (7)
-
Journal Impact Factor
-
Most Recent
-
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 hydrochloride 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.
-
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 -
-
Solvent & Solubility
H2O : 100 mg/mL (239.81 mM; Need ultrasonic)
DMSO : ≥ 50 mg/mL (119.91 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (7.19 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 (7.19 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 50 mg/mL (119.91 mM); Clear solution; Need ultrasonic
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Protocol
Cell viability is detected using Cell Counting Kit (CCK-8 kit) according to supplier’s introductions. Briefly, BGC823 cells are seeded at 104 cells per well for 48 hours with or without BS-181. Then, the absorbance is detected at 450 nm (reference at 650 nm) in each well.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In total, 5×106 BGC823 cells (0.1 mL) are injected subcutaneously into the flank of the mice. Tumor measurements are performed two times per week, and volumes are calculated using the formula: tumor size=(length ×width2)/2. Finally, 30 mice (tumor volume 100-200 mm3) are selected and randomLy assigned into three groups. As previously described, BS-181 is prepared in 10% dimethyl sulfoxide/50 mM HCl/5% Tween 20/85% saline. Micereceive BS-181 injection (ip) twice daily at indicated doses (BS-181 [10 mg/kg/d or 20 mg/kg/d] or Roscovitine [20 mg/kg/d]) for a total of 14 days. Control mice are injected with vehicles. Animal weights and tumor volume are measured each day throughout the 14-day treatment. In addition, all rats are kept for another 30 days for survival observation. Mice are injected intraperitoneally twice daily with BS-181 at 5 mg/kg or 10 mg/kg.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
-
Data Sheet (279 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
-
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 (sealed storage, away from moisture). 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 / H2O | 1 mM | 2.3981 mL | 11.9907 mL | 23.9814 mL | 59.9535 mL |
| 5 mM | 0.4796 mL | 2.3981 mL | 4.7963 mL | 11.9907 mL | |
| 10 mM | 0.2398 mL | 1.1991 mL | 2.3981 mL | 5.9953 mL | |
| 15 mM | 0.1599 mL | 0.7994 mL | 1.5988 mL | 3.9969 mL | |
| 20 mM | 0.1199 mL | 0.5995 mL | 1.1991 mL | 2.9977 mL | |
| 25 mM | 0.0959 mL | 0.4796 mL | 0.9593 mL | 2.3981 mL | |
| 30 mM | 0.0799 mL | 0.3997 mL | 0.7994 mL | 1.9984 mL | |
| 40 mM | 0.0600 mL | 0.2998 mL | 0.5995 mL | 1.4988 mL | |
| 50 mM | 0.0480 mL | 0.2398 mL | 0.4796 mL | 1.1991 mL | |
| 60 mM | 0.0400 mL | 0.1998 mL | 0.3997 mL | 0.9992 mL | |
| 80 mM | 0.0300 mL | 0.1499 mL | 0.2998 mL | 0.7494 mL | |
| 100 mM | 0.0240 mL | 0.1199 mL | 0.2398 mL | 0.5995 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Powered by Bioz