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99533-80-9

99533-80-9 structure
99533-80-9 structure
  • Name: K-252a
  • Chemical Name: K-252a
  • CAS Number: 99533-80-9
  • Molecular Formula: C27H21N3O5
  • Molecular Weight: 467.473
  • Catalog: Signaling Pathways Epigenetics PKC
  • Create Date: 2017-05-31 18:40:13
  • Modify Date: 2024-01-03 11:35:11
  • K-252a, a staurosporine analog isolated from Nocardiopsis sp. soil fungi, 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[1][2].

Name K-252a
Synonyms antibiotick252a
PROTEIN KINASE INHIBITOR FROM NORCARDIOP SIS SP.
PROTEIN KINASE INHIBITOR K-252A
PROTEIN KINASE INHIBITOR
K252a
K-252A,NOCARDIOPSIS SP
K-252a
Methyl (15S,16R,18R)-16-hydroxy-15-methyl-3-oxo-28-oxa-4,14,19-triazaoctacyclo[12.11.2.1.0.0.0.0.0]octacosa-1,6,8,10,12,20,22,24,26-nonaene-16-carboxylate
6,9-Epoxy-15H-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocine-7-carboxylic acid, 6,7,8,9,16,17-hexahydro-7-hydroxy-6-methyl-15-oxo-, methyl ester, (6S,7R,9R)-
antibioticsf2370
sf2370
Description K-252a, a staurosporine analog isolated from Nocardiopsis sp. soil fungi, 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[1][2].
Related Catalog
Target

IC50: 470 nM (PKC), 140 nM (PKA), 270 nM (Ca2+/calmodulin-dependent kinase type II), 1.7 nM (phosphorylase kinase)[1][2].

References

[1]. Yasuzawa, T., et al. The structures of the novel protein kinase C inhibitors K-252a, b, c AND d Journal of Antibiotics 39(8), 1072-1078 (1986).

[2]. Davis, P.D., et al. Inhibitors of protein kinase C. 1.1 2,3-bisarylmaleimides Journal of Medicinal Chemistry 35, 177-184 (1992).

Density 1.7±0.1 g/cm3
Boiling Point 685.3±55.0 °C at 760 mmHg
Molecular Formula C27H21N3O5
Molecular Weight 467.473
Flash Point 368.2±31.5 °C
Exact Mass 467.148132
PSA 94.72000
LogP 4.23
Vapour Pressure 0.0±2.2 mmHg at 25°C
Index of Refraction 1.841

CHEMICAL IDENTIFICATION

RTECS NUMBER :
KC6500000
CAS REGISTRY NUMBER :
99533-80-9
LAST UPDATED :
199212
DATA ITEMS CITED :
1
MOLECULAR FORMULA :
C27-H21-N3-O5
MOLECULAR WEIGHT :
467.51

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD - Lethal dose
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
>300 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
JANTAJ Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo, 141, Japan) V.2-5, 1948-52; V.21- 1968- Volume(issue)/page/year: 38,1437,1985
Symbol GHS08
GHS08
Signal Word Danger
Hazard Statements H360D-H371
Precautionary Statements P201-P260-P308 + P311
Personal Protective Equipment Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter
Hazard Codes Xi: Irritant;
Safety Phrases 22-24/25
RIDADR NONH for all modes of transport
RTECS NZ0550000
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