CDD-1115
CDD-1115 is a BMPR2 serine/threonine kinase inhibitor with an IC50 of 1.8 nM against human BMPR2 kinase. CDD-1115 selectively inhibits the catalytic activity of BMPR2, and shows weak inhibitory effects on ALK1 and ALK2.
For research use only. We do not sell to patients.
- CAS No.: 3034215-86-3
- Formula: C32H30N6O3
- Molecular Weight:546.62
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
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BMPR2 1.8 nM (IC50) |
ALK1 |
ALK2 |
In Vitro
CDD-1115 potently inhibits recombinant BMPR2 kinase activity with an IC50 of 1.8 nM[1].
CDD-1115 (5-50 μM; thermal scanning from 20 to 95 °C) binds potently to purified recombinant human BMPR2 kinase domain, increasing its melting temperature by 15.7 °C at a concentration of 50 μM[2].
CDD-1115 (30 min) potently inhibits purified recombinant human BMPR2 kinase activity with a Kiapp of 6.2 nM[2].
CDD-1115 is a highly selective inhibitor of human BMPR2, with an IC50 of 1.8 nM and >139-fold selectivity over other tested TGFβ family kinases[2].
CDD-1115 (1 μM) exhibits high selectivity for human BMPR2 over a panel of 403 kinases, with only BMPR2 showing significant binding at a concentration of 1 μM[2].
CDD-1115 (2.0 μM; 0-60 min) is metabolically unstable in human and mouse liver microsomes, with half-lives of 7 min and 12 min, respectively[2].
CDD-1115 (30 min pretreatment, followed by 6 h incubation with 5 ng/mL BMP2) inhibits BMP2-mediated luciferase reporter activity in HEK293T-BRE-Luc cells with an IC50 of 24.1 μM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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CAS No. 3034215-86-3
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Molecular Weight 546.62
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Formula C32H30N6O3
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SMILES
NC(C1=CC=CC(CNC(C2=CC=C3N=C(C4=CC5=C(C=NC=C5)C=C4)N([C@H]6C[C@@H](CC6)C(NC)=O)C3=C2)=O)=C1)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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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.
Purity & Documentation
References
[1]. Amrhein JA, et al. Design and Synthesis of Pyrazole-Based Macrocyclic Kinase Inhibitors Targeting BMPR2. ACS medicinal chemistry letters. 2023 Jun 08;14(6):833-840. [Content Brief]
[2]. Modukuri RK, et al. Discovery of Highly Potent and BMPR2-Selective Kinase Inhibitors Using DNA-Encoded Chemical Library Screening. Journal of medicinal chemistry. 2023 Feb 09;66(3):2143-2160. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)