CAS 99533-80-9|K-252a

Introduction：Basic information about CAS 99533-80-9|K-252a, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. K-252a BiologicalActivity
3. Chemical & Physical Properties
4. Toxicological Information
CHEMICAL IDENTIFICATION
HEALTH HAZARD DATA
ACUTE TOXICITY DATA
5. Safety Information
6. Articles19
7. Synonyms

Common Name	K-252a
CAS Number	99533-80-9	Molecular Weight	467.473
Density	1.7±0.1 g/cm3	Boiling Point	685.3±55.0 °C at 760 mmHg
Molecular Formula	C₂₇H₂₁N₃O₅	Melting Point	/
MSDS	ChineseUSA	Flash Point	368.2±31.5 °C
Symbol	GHS08	Signal Word	Danger

Names

Name	K-252a
Synonym	More Synonyms

K-252a BiologicalActivity

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	Signaling Pathways >>Epigenetics >>PKCSignaling Pathways >>Neuronal Signaling >>CaMKResearch Areas >>InfectionSignaling Pathways >>Protein Tyrosine Kinase/RTK >>PKASignaling Pathways >>Stem Cell/Wnt >>PKASignaling Pathways >>TGF-beta/Smad >>PKC
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).

Chemical & Physical Properties

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
InChIKey	KOZFSFOOLUUIGY-SOLYNIJKSA-N
SMILES	COC(=O)C1(O)CC2OC1(C)n1c3ccccc3c3c4c(c5c6ccccc6n2c5c31)C(=O)NC4

Toxicological Information

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

Safety Information

Symbol	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

Articles19

Rat BMSCs initiate retinal endogenous repair through NGF/TrkA signaling.

Exp. Eye Res. 132 , 34-47, (2015)

Müller cells can completely repair retinal injury by acting as endogenous stem/progenitor cells in lower-order vertebrates. However, a safe and effective approach to activate progenitor potential of r...

HBZ stimulates brain-derived neurotrophic factor/TrkB autocrine/paracrine signaling to promote survival of human T-cell leukemia virus type 1-Infected T cells.

J. Virol. 88(22) , 13482-94, (2014)

Brain-derived neurotrophic factor (BDNF) is a neurotrophin that promotes neuronal proliferation, survival, and plasticity. These effects occur through autocrine and paracrine signaling events initiate...

Dopamine-sensitive signaling mediators modulate psychostimulant-induced ultrasonic vocalization behavior in rats.

Behav. Brain Res. 296 , 1-6, (2015)

The mesolimbic dopamine system plays a major role in psychostimulant-induced ultrasonic vocalization (USV) behavior in rodents. Within this system, psychostimulants elevate synaptic concentrations of ...

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

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