T1610

Metaxalone (Methaxalonum) (marketed by King Pharmaceuticals under the brand name Skelaxin ) is a muscle relaxant used to relax muscles and relieve pain caused by strains, sprains, and other musculoskeletal conditions.

EHT 1610 (EHT 5372) is a potent inhibitor of DYRK, with an IC50 of 0.36 nM and 0.59 nM for DYRK1A and DYRK1B, respectively. EHT 1610 has an inhibitory effect on leukemia, regulating cell cycle and inducing cell apoptosis.

ML402 (ZINC3671497) is an activator of TREK-1 and TREK-2 with EC50s of 13.7 μM and 5.9 μM.

Balamapimod, also known as MKI-822, is a small-molecule Ras/Raf/MEK inhibitor that directly targets deregulated MAPK signaling cascades and is being actively explored to suppress aberrant protein kinase activity implicated in oncogenic transformation, inflammatory signaling, and pathological cell proliferation, with demonstrated therapeutic relevance for stroke, osteoporosis, rheumatoid arthritis, polycystic kidney disease, colonic polyps, and other inflammation-driven disorders through pathway-level inhibition.

ML-290 is an effective relaxin/insulin-like family peptide receptor (RXFP1) agonist and activator of anti-fibrotic genes. It shows an EC50 of 94 nM.

ML-792 is a specific small ubiquitin-like modifier activating enzyme (SUMO) inhibitor. ML-792 selectively inhibits SAE/SUMO1 and SAE/SUMO2 with IC50 of 3 and 11 nM.

ML-9 (free base) suppresses MLCK, PKA, and PKC activity (Ki: 4, 32, and 54 μM, respectively). ML-9 (free base) is a selective and effective inhibitor of Akt kinase, inhibits myosin light-chain kinase (MLCK), and stromal interaction molecule 1 (STIM1) acti

ML-9 suppresses MLCK, PKA, and PKC activity with Ki values of 4, 32, and 54 μM, respectively. ML-9 is a selective and effective inhibitor of Akt kinase, inhibits myosin light-chain kinase (MLCK), and stromal interaction molecule 1 (STIM1) activity. ML-9 causes autophagy by stimulating autophagosome formation and inhibiting their degradation.

ML132 is an effective and selective inhibitor of caspase 1 (IC50: 0.316 nM).

ML224 (NCGC00242364) is a TSHR antagonist for the treatment of Graves' orbital disease and Graves' hyperthyroidism.

ML230 is a selective ATP-binding cassette (ABC) transporter ABCG2 inhibitor. It 36-fold selective for ABCG2 over ABCB1 (EC50s: 0.13 μM and 4.65 μM, respectively).

ML349 is an inhibitor of LYPLA2 (IC50: 144 nM). ML349 is an effective and specific acyl protein thioesterase 2 (APT-2) inhibitor (Ki: 120 nM).

Metaxalone-D6 is intended for use as an internal standard for the quantification of metaxalone by GC-or LC-MS. Metaxalone (T1610) is a skeletal muscle relaxant. It inhibits the proliferation of, and induces apoptosis in, RAW 264.7 cells in vitro when used at concentrations ranging from 1 to 100 µM. Metaxalone (T1610) also reduces LPS-induced increases in COX-1, COX-2, and NF-kB levels and inhibits LPS-induced production of TNF-α, IL-6, and prostaglandin E2 in RAW 264.7 cells. Formulations containing metaxalone have been used in the treatment of lower back pain.