[CAS NO. 99533-80-9] K-252a

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PRODUCTS SPECIFICATIONS [99533-80-9]

Catalog

HY-N6732

Brand

MCE

CAS

99533-80-9

DESCRIPTION [99533-80-9]

Overview

MDL	-
Molecular Weight	467.47
Molecular Formula	C27H21N3O5
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

For research use only. We do not sell to patients.

9 Publications Citing Use of MCE

Summary

K-252a, a staurosporine analog, inhibits protein kinase , with IC ₅₀ values of 470 nM, 140 nM, 270 nM, and 1.7 nM for PKC , PKA , Ca ²⁺ /calmodulin-dependent kinase type II, and phosphorylase kinase, respectively ^[1] ^[2] . K-252a is a potent inhibitor (IC ₅₀ of 3 nM) of the tyrosine protein kinase (TRK) activity of the NGF receptor gp140trk, the product of the trk protooncogene ^[3] .

IC50 & Target

CaMK II

In Vitro

K-252a (3-100 nM, 8d) inhibits NGF-promoted neurite outgrowth ^[5] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis ^[4] .

Cell Line:	LINC00641-overexpressed cell line.
Concentration:	1.7 nM (NGF (50 ng/mL)).
Incubation Time:	6 h.
Result:	Decreased p-Akt and p-TrkB levels.

Cell Viability Assay ^[5] .

Cell Line:	PC12 subclone h cells.
Concentration:	3 to 100 nM.
Incubation Time:	8 d.
Result:	Inhibited NGF-promoted neurite outgrowth.

In Vivo

K252a (20 mg/kg/day) inhibiting TrkB pathway dampens the neuroprotective effects induced by TH ^[6] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Mice ^[6] .
Dosage:	20 mg/kg/day.
Administration:	Intraperitoneally, daily, for consecutive 5 days.
Result:	Dampened the neuroprotective effects induced by TH.

Appearance

Solid

Source

Nocardiopsis sp.

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL ( 106.96 mM ; Need ultrasonic and warming)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1392 mL	10.6959 mL	21.3917 mL
5 mM	0.4278 mL	2.1392 mL	4.2783 mL
10 mM	0.2139 mL	1.0696 mL	2.1392 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (5.35 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.08 mg/mL (4.45 mM); Clear solution

* All of the co-solvents are available by MCE.

References

Synonyms

9,12-Epoxy-1H-diindolo[1,2,3-fg:3′,2′,1′-kl]pyrrolo[3,4-i][1,6]benzodiazocine-10-carboxylic acid, 2,3,9,10,11,12-hexahydro-10-hydroxy-9-methyl-1-oxo-, methyl ester, (9S,10R,12R)-

9,12-Epoxy-1H-diindolo[1,2,3-fg:3′,2′,1′-kl]pyrrolo[3,4-i][1,6]benzodiazocine-10-carboxylic acid, 2,3,9,10,11,12-hexahydro-10-hydroxy-9-methyl-1-oxo-, methyl ester, [9S-(9α,10β,12α)]-

Antibiotic SF 2370

Antibiotic K 252a, (+)-

K 252a

SF 2370

(+)-Antibiotic K 252a

(+)-K 252a

(+)-Antibiotic SF 2370

(+)-SF 2370

Antibiotic K 252a

Antibiotic SF 2370, (+)-

Protein kinase inhibitor K252a

K 252

K 252a Nocardiopsis sp.