CDD-1653 is a potent and BMPR2-selective kinase inhibitor (IC50 = 2.8 nM). CDD-1653 effectively inhibited BMP-mediated gene expression. Specifically, it suppressed BRE-reporter activity in 293T-BRE-Luc cells with an IC50 of 6.92 μM. Additionally, pretreatment with 25 μM of CDD-1653 significantly decreased the phosphorylation of SMAD1/5 in human umbilical vein endothelial cells (HUVECs) stimulated with BMP9, indicating its impact on downstream signaling pathways. Selectivity profiling revealed that CDD-1653 is highly selective for BMPR2, showing over 360-fold selectivity compared to ALK1 and inactivity against other type 1 and type 2 TGFβ family kinases. Furthermore, it demonstrated complete selectivity against a panel of over 408 off-target kinases.
MedKoo Cat#: 122681
Name: CDD-1653
CAS#: 3034216-44-6
Chemical Formula: C21H22N6O4S
Exact Mass: 454.1400
Molecular Weight: 454.51
Elemental Analysis: C, 55.50; H, 4.88; N, 18.49; O, 14.08; S, 7.05
The following data is based on the product molecular weight 454.51 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
