CIB-L43 is an TRBP inhibitor with nanomolar inhibitory activity (EC50 =0.66 nM). CIB-L43 demonstrated superior TRBP binding affinity (KD = 4.78 nM) and enhanced disruption of TRBP-Dicer interactions (IC50 = 2.34 μM). Mechanistically, CIB-L43 suppressed oncogenic miR-21 biosynthesis, increasing PTEN and Smad7expression and inhibiting AKT and TGF-β signaling, thereby reducing HCC cell proliferation and migration. In vivo, CIB-L43 exhibited favorable pharmacokinetics, including 53.9% oral bioavailability, and comparable antitumor efficacy to first-line anticancer drug, sorafenib, with lower toxicity.
MedKoo Cat#: 128283
Name: CIB-L43
CAS#: N/A
Chemical Formula: C15H16N2O3S
Exact Mass: 304.0882
Molecular Weight: 304.36
Elemental Analysis: C, 59.19; H, 5.30; N, 9.20; O, 15.77; S, 10.53
The following data is based on the product molecular weight 304.36 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 |