Blogs | MedChemExpress

SLLN-15 Activates Autophagy in Triple-Negative Breast Cancer (TNBC)

SLLN-15 is an oral activ enhancer of autophagy that activates cytostatic macroautophagy/autophagy in triple-negative breast cancer (TNBC).
TD-428 is a Highly Specific BRD4 Degrader

TD-428, a immunomodulatory drug analog, is a highly specific BRD4 degrader with a DC50 of 0.32 nM. TD-428 reduces c-Myc levels more efficiently than JQ1.
TAK-981, an Inhibitor For SUMOylation Enzymatic Cascade with Antineoplastic Activities

TAK-981 is a selective inhibitor of the SUMOylation enzymatic cascade, with potential immune-activating and antineoplastic activities
NRX-252262, an Enhancer of β-catenin:β-TrCP Interaction

NRX-252262 is a β-catenin:β-TrCP interaction enhancer, and its cognate E3 ligase, SCFβ-TrCP, induces mutant β-catenin degradation, with an EC50 of 3.8 nM
Borussertib, a Covalent-Allosteric Akt Inhibitor

Borussertib is a covalent-allosteric and first-in-class inhibitor of protein kinase Akt, with an IC50 of 0.8 nM and a Ki of 2.2 nM for Akt-wt.
Y06137 is a Selective BET Inhibitor for Treatment of CRPC

Y06137 is a potent and selective BET inhibitor, which binds to the BRD4(1) bromodomain with a Kd of 81 nM. Antitumor activity.
TAK-828F is a Potent, Selective and Orally Active RORγt Inverse Agonist

2019-04-25

TAK-828F is a potent, selective and orally active retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonist. TAK-828F inhibits IL-17A cytokine expression and reduces symptoms of autoimmune encephalomyelitis mice.
BTR-1 Induces Cell Growth Inhibition Followed by Apoptosis

BTR-1 potently inhibits cell growth. It induces S phase arrest, affects DNA replication. Dose-dependently induces cytotoxicity in leukemic cell lines.
Cevipabulin (TTI-237) is a Microtubule-Active Antitumor Compound

Cevipabulin is a microtubule-active compound and inhibits the binding of [3H] vinblastine to tubulin, with an IC50 of 18-40 nM for in human tumor cell line.
A Potent and Reversible EGFR Inhibitor (E)-AG 99

(E)-AG 99 is an EGFR inhibitor and shows a growth-inhibition on not only serum-starved cells but also normally grown cells. Treatment for Bladder cancer.

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Blogs (32)