New Small Molecules from MCE for March 2021

Clitocine, an adenosine nucleoside analog isolated from mushroom, is a potent and efficacious readthrough agent. Clitocine acts as a suppressor of nonsense mutations and can induce the production of p53 protein in cells harboring p53 nonsense-mutated alleles. Clitocine can induce apoptosis in multidrug-resistant human cancer cells by targeting Mcl-1. Anticancer 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.

MSA-2, a potent and orally available non-nucleotide STING agonist, is bound to STING as a noncovalent dimer with nanomolar affinity. MSA-2 shows EC₅₀s of 8.3 and 24 μM for human STING isoforms WT and HAQ, respectively. MSA-2 stimulates interferon-β secretion in tumors, induces tumor regression with durable antitumor immunity, and synergizes with anti-PD-1 in syngeneic mouse tumor models.

Cell Signaling Pathway

SEC induces activation of ANXA7 GTPase via the AMPK/mTORC1/STAT3 signaling pathway. SEC selectively promotes apoptosis in cancer cells, expressing a high level of ITGB4 by inducing ITGB4 nuclear translocation.

1. Nature. 2021 Feb;590(7846):486-491.
2. Cell. 2021 Feb 18;184(4):943-956.e18.
3. Cell Metab. 2021 Feb 2;33(2):283-299.e9.
4. Cell Metab. 2021 Jan 5;33(1):174-189.e7.

Omadacycline (PTK 0796) tosylate, a first-in-class orally active aminomethylcycline antibacterial, is a member of the tetracycline class of antibiotics. Omadacycline tosylate acts through the inhibition of bacterial protein synthesis by binding to the 30S ribosomal subunit.

UTL-5g (GBL-5g), an anti-inflammatory TNF-α inhibitor, has chemoprotective and liver radioprotective effects. UTL-5g lowers hepatotoxicity, nephrotoxicity, and myelotoxicity induced by Cisplatin through TNF-α inhibition among other factors.