CDD-1653
Based on 1 Customer Validation
CDD-1653 is a potent and selective BMPR2 inhibitor with an IC50 of 2.8 nM. CDD-1653 inhibits the catalytic activity of BMPR2 by competitively binding to its ATP pocket, specifically blocking BMP-induced downstream signaling (particularly inhibiting SMAD1/5 phosphorylation), thereby suppressing the expression of related genes. CDD-1653 can be used for research on cancer, bone diseases, and vascular and endothelial dysfunction.
For research use only. We do not sell to patients.
- Purity : 99.38%
- CAS No.: 3034216-44-6
- Formula: C21H22N6O4S
- Molecular Weight:454.50
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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
Biological Activity
Description
IC50 & Target
[1]|
BMPR2 2.8 nM (IC50) |
BMP |
Smad1 |
In Vitro
CDD-1653 is a highly selective BMPR2 inhibitor with an IC50 of 2.8 nM and no activity against other related TGFβ family kinases[1].
CDD-1653 (1 μM) is a single-kinase selective inhibitor that exhibits extremely high selectivity for BMPR2 among the 403 kinases tested[1].
CDD-1653 (pre-incubated for 30 min followed by BMP2 stimulation for 6 h) inhibits BMP2 (HY-P7006)-induced BMP-mediated gene expression in 293T-BRE-Luc cells with an IC50 of 6.92 μM[1].
CDD-1653 (25 μM; preincubation for 30 min followed by costimulation with BMP2 or BMP9 for 15 min) inhibits BMP2- and BMP9 (HY-P700530)-mediated SMAD1/5 activation in HEK293T and HUVEC cells[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:HEK293T cells
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Concentration:25 μM
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Incubation Time:30 min pre-treatment, followed by stimulation with 5 ng/mL BMP2 for 15 min
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Result:Significantly decreased the phosphorylation of SMAD1/5 (pSMAD1/5).
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Cell Line:HUVECs
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Concentration:25 μM
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Incubation Time:30 min pre-treatment, followed by stimulation with 5 ng/mL BMP9 for 15 min
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Result:Significantly decreased the phosphorylation of SMAD1/5 (pSMAD1/5).
Chemical Information
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CAS No. 3034216-44-6
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Appearance Solid
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Molecular Weight 454.50
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Formula C21H22N6O4S
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Color White to yellow
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SMILES
O=C1N(CCN(C1)C2=NC(NC3=CC=CC(S(=O)(N)=O)=C3)=NC=C2OC)C4=CC=CC=C4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (220.02 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (11.00 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
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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Kinase activity and phosphorylation assays
Kinase activity assays measure the ability of kinases to transfer phosphate groups from ATP to specific substrates, while phosphorylation assays detect the presence and levels of phosphorylated proteins. Common methods include radiolabeled ATP incorporation (e. g. ,), ADP release detection via bioluminescence (e. g. ,[3]), enzyme-linked immunosorbent assays (ELISA) for phospho-specific epitopes (e. g. ,[6]), and microtiter-based formats for high-throughput screening (e. g. ,[8]). The ADP-Glo assay quantifies kinase activity by measuring ADP produced during phosphorylation using a luciferase-based system. Radiometric assays involve autoradiography or scintillation counting after incorporation of 32P-labeled ATP into substrate proteins. ELISA-based approaches rely on phospho-specific antibodies to detect activated kinases in cell lysates or purified samples.
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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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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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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Protocol for Kinase activity and phosphorylation assays
Kinase activity assays measure transfer of phosphate from ATP to a protein or peptide substrate, generating phosphorylated substrate, ADP, or incorporated radiolabeled phosphate as the readout; phosphorylation assays measure site-specific phosphorylation in cells or tissues as a proxy for kinase-pathway activation, inhibition, or substrate regulation. Phosphorylation can be detected by phospho-specific Western blot, immunoprecipitation kinase assay, phospho-immunofluorescence, phospho-flow cytometry, luminescent ADP detection, radiolabeled ATP incorporation, or reporter-based pathway assays, and these readouts can be applied to cancer cells, primary neurons, mouse tumors, organoids, inflammatory macrophages, ferroptosis studies, and mitophagy studies when the kinase target is biologically relevant.
Purity & Documentation
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Data Sheet (273 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.2002 mL | 11.0011 mL | 22.0022 mL | 55.0055 mL |
| 5 mM | 0.4400 mL | 2.2002 mL | 4.4004 mL | 11.0011 mL | |
| 10 mM | 0.2200 mL | 1.1001 mL | 2.2002 mL | 5.5006 mL | |
| 15 mM | 0.1467 mL | 0.7334 mL | 1.4668 mL | 3.6670 mL | |
| 20 mM | 0.1100 mL | 0.5501 mL | 1.1001 mL | 2.7503 mL | |
| 25 mM | 0.0880 mL | 0.4400 mL | 0.8801 mL | 2.2002 mL | |
| 30 mM | 0.0733 mL | 0.3667 mL | 0.7334 mL | 1.8335 mL | |
| 40 mM | 0.0550 mL | 0.2750 mL | 0.5501 mL | 1.3751 mL | |
| 50 mM | 0.0440 mL | 0.2200 mL | 0.4400 mL | 1.1001 mL | |
| 60 mM | 0.0367 mL | 0.1834 mL | 0.3667 mL | 0.9168 mL | |
| 80 mM | 0.0275 mL | 0.1375 mL | 0.2750 mL | 0.6876 mL | |
| 100 mM | 0.0220 mL | 0.1100 mL | 0.2200 mL | 0.5501 mL |
CDD-1653 Related Classifications
HY-164145 Related Classifications
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