K-252a , fromNocardiopsissp. , 99533-80-9

CAS NO.：99533-80-9

Empirical Formula: C27H21N3O5

Molecular Weight: 467.47

MDL number: MFCD00161522

EINECS: 640-127-4

PRODUCT Properties

• Melting point: 262-273℃ (decomposition) (methanol )
• Boiling point: 685.3±55.0 °C(Predicted)
• Density: 1.68
• Flash point: 87℃
• storage temp.: -20°C
• solubility: DMF: 1 mg/mL
• pka: 11.95±0.40(Predicted)
• form: Lyophilized solid.
• color: White or off-white
• Stability: Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.

Description and Uses

K252a is a staurosporine analog isolated from Nocardiopsis sp. soil fungi that inhibits protein kinase (PK) C, PKA, Ca²⁺/calmodulin-dependent kinase type II, and phosphorylase kinase with IC₅₀ values of 470, 140, 270, and 1.7 nM, respectively. Because it inhibits neurotrophin receptor tyrosine kinases, K252a at 100-500 nM has been used to suppress trophoblast proliferation and increase apoptosis associated with the disruption of mitochondrial functions in cultured choriocarcinoma cells. Recently, K252a has been shown to inhibit PRK1 (IC₅₀ = 3.2 nM in vitro), a PKC-related kinase that phosphorylates histone H3 at threonine 11 and is involved in androgen-dependent gene expression.

K-252a is used to inhibit protein kinases involved in cell signaling processes, including CaM kinase; phosphorylase kinase, serine/threonine kinases, Trk. It is used to inhibit the actions of nerve growth factor (NGF) on PC1 2 cells and to inhibit smooth muscle myosin light chain kinase .

Safety

• Symbol(GHS): GHS08
• Signal word: Danger
• Hazard statements: H360D-H371
• Precautionary statements: P202-P260-P264-P270-P280-P308+P311
• Hazard Codes: Xi,T
• Risk Statements: 61-20/21/22-68/20/21/22
• Safety Statements: 22-24/25-45-36/37-53
• RIDADR: NA 1993 / PGIII
• WGK Germany: 3
• RTECS: NZ0550000
• F: 8-10
• HS Code: 29349990