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
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
|
BMPR2 1.8 nM (IC50) |
ALK1 |
ALK2 |
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.
Chemical Information
-
CAS No. 3034215-86-3
-
Molecular Weight 546.62
-
Formula C32H30N6O3
-
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
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
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)