New Small Molecules from MCE for December 2020

GOT1-01 is a potent aspartate aminotransferase 1 (glutamate oxaloacetate transaminase 1; GOT1) inhibitor. iGOT1-01 has IC₅₀s of 85 μM and 11.3 μM in MDH coupled GOT1 enzymatic assay and GOT1/GLOX/HRP assay, respectively. iGOT1-01 has anti-cancer activity.

Compound Screening Libraries

50 specific libraries for high throughput screening (HTS) and high content screening (HCS). Optimized for drug screening and new indication research.

Disitertide (P144) TFA is a peptidic transforming growth factor-beta 1 (TGF-β1) inhibitor specifically designed to block the interaction with its receptor. Disitertide (P144) TFA is also a PI3K inhibitor and an apoptosis inducer.

Cell Signaling Pathway

WF-47-JS03 is a potent and selective RET kinase inhibitor with IC₅₀s of 1.7 nM and 5.3 nM for KIF5B-RET transfected Ba/F3 cells and CCDC6-RET transfected LC-2/ad lung cancer cells, respectively. WF-47-JS03 demonstrates >500-fold selectivity against kinase insert domain receptor (KDR). Effective brain penetration.

NNature. 2020 Oct 21.
doi: 10.1038/s41586-020-2844-1.
Nature. 2020 Nov 18.
doi: 10.1038/s41586-020-2925-1.

COR659 is a potent and effective GABA_B positive allosteric modulator (PAM). COR659 suppresses alcohol and chocolate self-administration in rats..

BNTA, a potent extracellular matrix (ECM) modulator, facilitates cartilage structural molecule synthesis on chondrocytes by activating superoxide dismutase 3 (SOD3). BNTA shows a promising potential for osteoarthritis alleviation by modulating cartilage generation.