K252a

Inquiry Info. # 12754

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Product Information

Product Usage Information

K252a is supplied as a lyophilized powder. For a 1 mM stock, reconstitute the 100 μg in 213.9 µl DMSO. Working concentrations and length of treatment can vary depending on the desired effect, but it is typically used as a pretreatment at 0.1-1 µM for 0.5-1 hr prior to treating with a stimulator. Soluble in DMSO at 100 mg/ml; poorly soluble in ethanol.

Storage

Store lyophilized or in solution at -20ºC, desiccated. Protect from light. In lyophilized form, the chemical is stable for 24 months. Once in solution, use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Product Description

Molecular Weight	467.47 g/mol
Purity	>99%
Molecular Formula	C₂₇H₂₁N₃O₅
CAS	99533-80-9
Solubility	Soluble in DMSO at 100mg/ml.

Background

Originally isolated from the soil fungi Nocardiopisis sp., K252a is a staurosporine analog that inhibits various protein kinases through competition with the ATP binding site (1,2). K252a is a reversible cell-permeable, potent inhibitor of phosphorylase kinase (IC₅₀ = 1.7 nM), protein kinase A (PKA) (IC₅₀= 140 nM), and protein kinase C (PKC) (IC₅₀ = 470 nM) (3,4). K252a is also known to inhibit protein kinase G and CaM kinase II (5,6). K252a inhibits nerve growth factor induced Trk activation (IC₅₀= 3 nM), as well as downstream signaling (5,7,8). K252a is reported to induce apoptosis and cell cycle arrest through cdc25 and cdc2 inhibition (9).

Alternate Names

apoptosis; cdc25; k-252a; k252; k252a; Marcks; ngf; PKA; PKC; TPA; Trk

Limited Uses

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For Research Use Only. Not for Use in Diagnostic Procedures.

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K252a #12754