ms4

MS4 is a novel glucocorticoid receptor (GR) agonist with anti-inflammatory activity and displaying reduced impact on islets.

BMS493 is an inverse agonist of the pan-retinoic acid receptor (RAR) that inhibits retinoic acid-induced differentiation, enhances the interaction of nuclear co-inhibitors with RARs, attenuates RA signaling, potentiates TPP-induced toxicity, and inhibits the increase in phospholipase A2 activity.

(Iso)-MS4322 ((Iso)-YS43-22) is a selective and potent protein arginine methyltransferase 5 (PRMT5) degrader with potential anticancer activity that effectively reduces PRMT5 protein levels in MCF-7 cells and inhibits the growth of a wide range of cancer cells.

MS402 is a novel BD1-selective BET BrD inhibitor.

MS436 is a selective, small-molecule inhibitor for the BRD4 bromodomains.

BMS453 (BMS-189453), a synthetic retinoid, is a potent and selective agonist of RARβ and a potent testicular toxin. BMS453 inhibits breast cell growth predominantly through the induction of active TGFβ.

MS4077 is an degrader of anaplastic lymphoma kinase (ALK) PROTAC(Kd of 37 nM for binding affinity to ALK).

MS432 is a highly selective PD0325901-based VHL-recruiting PROTAC degrader for MEK1 and MEK2.

MS4078 is an inhibitor and aplastic lymphoma kinase (ALK) PROTAC (degrader) based on Cereblon ligand, with a Kd of 19 nM for binding affinity to ALK.

MS417 (GTPL7512) is an inhibitor of BET-specific BRD4(BRD4-BD1 and BRD4-BD2 with IC50s of 30, 46 nM and Kds of 36.1, 25.4 nM, respectively), with weak selectivity at CBP BRD with IC50 of 32.7 μM.

MS41 is a selective eleven-nineteen leukemia (ENL) PROTAC degrader, with DC50s values of 3.50 nM (MV4;11), 2.84 nM (SEMK2), 3.03 nM (Jurkat), and 26.58 nM (KASUMI1). This compound effectively inhibits the growth of ENL-dependent leukemia cells, induces G1 cell cycle arrest, and increases cellular apoptosis (Apoptosis). Additionally, MS41 reduces chromatin occupancy related to ENL-mediated transcription elongation mechanisms and suppresses the expression of oncogenes and the progression of leukemia.

MS40 is a WDR5 PROTAC that selectively degrades WDR5 and serves as a novel degrader for immune-modulating compounds (IMiDs), including the new substrates CRBN and Ikaros zinc finger (IKZF) transcription factors IKZF1 and IKZF3. MS40 facilitates the degradation of WDR5, resulting in the dissociation of the MLL KMT2A complex from chromatin, thereby reducing H3K4me2 levels. In vitro, MS40 inhibits the growth of primary leukemia patient cells, and in vivo, it suppresses the expansion of patient-derived xenografts.

MS4332 is a PROTAC designed to target PRMT5.

MS437 is a potent TSH receptor agonist.

MS438 is an effective agonist of the TSH receptor.

MS453 is a potent and selective SETD8 inhibitor with an IC50 value of 804 nM.

MS47134, a selective and potent MRGPRX4 agonist, exhibits an EC50 of 149 nM and holds potential for researching pain, itch, and mast cell-mediated hypersensitivity.

Folate-MS432 is a PROTAC that degrades MEKs selectively in cancer cells via folate receptor-dependent pathways.

MS48107 is a potent, selective positive allosteric modulator of G protein-coupled receptor 68 (GPR68), demonstrating specificity for GPR68 over closely related proton GPCRs, neurotransmitter transporters, and hERG ion channels. It effectively crosses the blood-brain barrier (BBB) in mice.

G-479 is an potent MEK inhibitor. Structurally, G-479 is an analogue of GDC-0623 (or so-call Me-Too drug). G-479 with polarity distributed throughout the molecule was shown improved bioactivity over GDC-0623 in many aspects.