Neurotrophin Antagonist, Y1036 - Calbiochem (C15-1303-908)

General description

A furyl-thioxothiazolidinone compound that binds both BDNF (Cat. No. 203702) and NGF (Cat. No. 480352) (K_D = 3.5 and 3.0 µM, respectively) and prevents their interaction with cell surface receptors (IC₅₀ against BDNF/p75NTR, BDNF/trkB, NGF/p75NTR, and NGF/trkA interaction = 6.2, 3.7, 5.7, and 8.8 µM, respectively, in PC12 cultures), while exhibiting no effect against the receptor binding of the non-neurotrophin growth factors EGF and PDGF. Y1036 at 40 µM is shown to inhibit trkA and trkB phosphorylation upon 40 pM BDNF and NGF treatment, respectively, as well as downstream Erk phosphorylation. Y1036 is also demonstrated to block BDNF- and NGF-induced neurite outgrowth in rat embryonic dorsal-root ganglions in a dose-dependent manner.

A furyl-thioxothiazolidinone compound that binds both BDNF (Cat. No. 203702) and NGF (Cat. No. 480352) (K_D = 3.5 and 3.0 µM, respectively) and prevents their interaction with cell surface receptors (IC₅₀ against BDNF/p75NTR, BDNF/trkB, NGF/p75NTR, and NGF/trkA interaction = 6.2, 3.7, 5.7, and 8.8 µM, respectively, in PC12 cultures), while exhibiting no effect against the receptor binding of the non-neurotrophin growth factors EGF and PDGF. Y1036 at 40 µM is shown to inhibit trkA and trkB phosphorylation upon 40 pM BDNF and NGF treatment, respectively, as well as downstream Erk phosphorylation. Y1036 is also demonstrated to block BDNF- and NGF-induced neurite outgrowth in rat embryonic dorsal-root ganglions in a dose-dependent manner.

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Eibl, J.K., et al. 2009. J. Pharmacol. Exp. Ther.332, 446.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Molecular Weight: 438.50. Empirical Formula: C₁₇H₁₄N₂O₆S₃. Quality Level: 100. Assay: ≥. 90% (HPLC). form: solid. manufacturer/tradename: Calbiochem^®. . storage condition: OK to freeze, protect from light. color: yellow. solubility: DMSO: 50 . mg/mL. shipped in: ambient. storage temp.: 2-8°C. Storage Class Code: 11 - Combustible Solids. WGK: WGK 2. Flash Point(F): Not applicable. Flash Point(C): Not applicable.