CIB-L43 is a TRBP inhibitor. CIB-L43 exhibits a nanomolar inhibitory activity with an EC₅₀ of 0.66 nM and a dissociation constant (K_D) of 4.78 nM, indicating strong binding affinity to TRBP. CIB-L43 effectively disrupts the TRBP-Dicer interaction, with an IC₅₀ of 2.34 μM, leading to suppression of oncogenic miR-21 biosynthesis. This suppression results in increased expression of PTEN and Smad7, thereby inhibiting AKT and TGF-β signaling pathways, which are essential for hepatocellular carcinoma (HCC) cell proliferation and migration. In vivo studies demonstrate that CIB-L43 has favorable pharmacokinetics, including 53.9% oral bioavailability, and exhibits antitumor efficacy comparable to sorafenib, a first-line anticancer drug, but with lower toxicity. These findings position CIB-L43 as a promising candidate for HCC treatment, combining potent TRBP inhibition with favorable drug-like properties.
MedKoo Cat#: 556387
Name: CIB-L43
CAS#: 1082942-70-8
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 |
