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In vitro: 7,8-DHF is one of the positive compounds that specifically activate TrkB, but not TrkA or TrkC, at a concentration of 250 nM. In addition to cortical and hippocampal neurons, 7,8-DHF also protects other cell types including the RGC (retinal ganglion cells) and PC12 cells from excitotoxic and oxidative stress-induced apoptosis and cell death. Thus, it has neuroprotective properties. In vivo: 7,8-Dihydroxyflavone is a bioavailable chemical that can pass through the BBB to provoke TrkB and its downstream PI3K/Akt and MAPK activation in mouse brain upon intraperitoneal or oral administration. 7,8-DHF promotes the survival and reduces apoptosis in cortical neurons of traumatic brain injury as administration of 7,8-DHF at 3 h post-injury reduces brain tissue damage via the PI3K/Akt pathway. Its treatment does not induce any apparent toxicity in mice and is not toxic to the mice during the chronic treatment. 7,8-DHF displays robust therapeutic efficacy toward Alzheimer's disease and inhibits obesity through activating muscular TrkB.
| Molecular Weight | 254.24 |
| Formula | C15H10O4 |
| CAS Number | 38183-03-8 |
| Form | Solid |
| Solubility (25°C) | 50 mg/mL in DMSO |
| 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. |
| 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. |
| LOXO-101 sulfate
LOXO-101 sulfate is an oral potent and selective ATP-competitive inhibitor of tropomyosin receptor kinases (TRK). |
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