New Small Molecules from MCE for August 2020

JH-X-119-01 hydrochloride is a potent and selective interleukin-1 receptor-associated kinases 1 (IRAK1) inhibitor. JH-X-119-01 hydrochloride ameliorates LPS-induced sepsis in mice.

Compound Screening Libraries

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

EG01377 dihydrochloride is a potent, bioavailable and selective inhibitor of neuropilin-1 (NRP1), with a K_d of 1.32 μM, and IC₅₀s of 609 nM for both NRP1-a1 and NRP1-b1. EG01377 dihydrochloride has antiangiogenic, antimigratory, and antitumor effects.

Cell Signaling Pathway

OTS186935 hydrochloride is a potent protein methyltransferase SUV39H2 inhibitor with an IC₅₀ of 6.49 nM. OTS186935 hydrochloride shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS193320 hydrochloride regulates the production of γ-H2AX in cancer cells.

1. Nature. 2020 Jul;583(7817):620-624. doi:
10.1038/s41586-020-2502-7.

SR18662 is a potent inhibitor of Krüppel-like factor five (KLF5) with an IC₅₀ of 4.4 nM and an analogue of ML264 (HY-19994) with improved inhibitory potency against colorectal cancer cells. SR18662 can be used for the study of colorectal cancer.

TH1834 is a specific Tip60 (KAT5) histone acetyltransferase (HAT) inhibitor. TH1834 induces apoptosis and increases DNA damage in breast cancer. TH1834 does not affect the activity of related histone acetyltransferase MOF. Anticancer activity.