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LM22A-4 is a potent tropomyosin-related kinase B (TrkB) agonist (IC50 = 47 nM). Induces activation of Trk, Akt and ERK in mouse hippocampus and striatum. Reverses deficits in motor task learning in mice following traumatic brain injury; restores respiratory function in a rat model of Rett syndrome. LM22A-4 significantly up-regulates OPN and ALPase mRNA expression in a dose-dependent manner and OC mRNA level is significantly increased by 5 μM of LM22A-4. LM22A-4 significantly increases OPN, ALPase and OC mRNA expression in a time-dependent manner. LM22A-4 stimulated OPN and OC mRNA expression in HCEM cells cultured with mineralizing media.
| Molecular Weight | 339.34 |
| Formula | C15H21N3O6 |
| CAS Number | 37988-18-4 |
| Solubility (25°C) | Water 50 mg/mL DMSO 29 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Trk Products |
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| GNF-5837
GNF-5837 is a potent pan-Trk inhibitor which display antiproliferative effects in cellular Ba/F3 assays (IC50 values are 7, 9 and 11 nM for cells containing the fusion proteins Tel-TrkC, Tel-TrkB and Tel-TrkA, respectively. |
| GW441756
GW441756 is a potent, selective inhibitor of TrkA with IC50 of 2 nM, with very little activity to c-Raf1 and CDK2. |
| ANA-12
ANA-12 is a potent and selective TrkB antagonist with IC50s of 45.6 nM and 41.1 μM for the high and low affinity sites, respectively. |
| 7,8-Dihydroxyflavone
7,8-Dihydroxyflavone acts as a potent and selective small-molecule agonist of the TrkB receptor (Kd ≈ 320 nM), the main signaling receptor of brain-derived neurotrophic factor (BDNF). |
| Larotrectinib (LOXO-101)
Larotrectinib (LOXO-101) is a potent, ATP competitive TRK inhibitor with IC50s in low nanomolar range for inhibition of all TRK family members in binding and cellular assays, with 100x selectivity over other kinases, with 2 to 20 nM cellular potency against the TRKA, TRKB, and TRKC kinases. |
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