Synonyms
SF2370; Antibiotic K 252a; Antibiotic SF 2370
Description
K-252a, a staurosporine analog, inhibits protein kinase, with IC50 values of 470 nM, 140 nM, 270 nM, and 1.7 nM for PKC, PKA, Ca2+/calmodulin-dependent kinase type II, and phosphorylase kinase, respectively. K-252a is a potent inhibitor (IC50 of 3 nM) of the tyrosine protein kinase (TRK) activity of the NGF receptor gp140trk, the product of the trk protooncogene.
Structural Formula
K-252a
Solubility
DMSO : 50 mg/mL(106.96 mM;Need ultrasonic and warming)
Shipping
Room temperature in continental US; may vary elsewhere.
SMILES
O=C(NC1)C2=C1C3=C4C5=C2C6=C(C=CC=C6)N5[C@](C[C@]7(O)C(OC)=O)([H])O[C@]7(C)N4C8=C3C=CC=C8
In Vivo
K252a (20 mg/kg/day) inhibiting TrkB pathway dampens the neuroprotective effects induced by TH.
In Vitro
K-252a (3-100 nM, 8d) inhibits NGF-promoted neurite outgrowth.