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SML1728

Sigma-Aldrich

STK16-IN-1

≥98% (HPLC)

Synonym(s):

1-(4-Fluoro-3-methylphenyl)-1,7-dihydro-2H-pyrrolo[2,3-h]-1,6-naphthyridin-2-one, 1-(4-Fluoro-3-methylphenyl)-1H-pyrrolo[2,3-h][1,6]naphthyridin-2(7H)-one

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About This Item

Empirical Formula (Hill Notation):
C17H12FN3O
CAS Number:
1223001-53-3
Molecular Weight:
293.30
UNSPSC Code:
12352202
NACRES:
NA.77
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Quality Level

100

Assay

≥98% (HPLC)

form

powder

storage condition

protect from light

color

white to beige

solubility

DMSO: 10 mg/mL, clear (warmed)

storage temp.

2-8°C

SMILES string

CC1=CC(N2C(C(C=CN3)=C3N=C4)=C4C=CC2=O)=CC=C1F

InChI

1S/C17H12FN3O/c1-10-8-12(3-4-14(10)18)21-15(22)5-2-11-9-20-17-13(16(11)21)6-7-19-17/h2-9H,1H3,(H,19,20)

InChI key

WQNRDXHKVSKUPI-UHFFFAOYSA-N

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Anti-Caspase 8 antibody produced in rabbit

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antibody form

affinity isolated antibody

antibody form

affinity isolated antibody

antibody form

affinity isolated antibody

antibody form

affinity isolated antibody

conjugate

unconjugated

conjugate

unconjugated

conjugate

unconjugated

conjugate

-

Quality Level

100

Quality Level

100

Quality Level

200

Quality Level

100

biological source

rabbit

biological source

rabbit

biological source

rabbit

biological source

rabbit

species reactivity

human, mouse, rat

species reactivity

human

species reactivity

human, rat

species reactivity

human, mouse, rat

Gene Information

human ... CASP8(841)

Gene Information

human ... CASP8(841)

Gene Information

human ... CASP9(842)
rat ... Casp9(58918)

Gene Information

human ... CASP8(841)

Biochem/physiol Actions

STK16-IN-1 is a cell-permeable pyrrolonaphthyridinone compound that acts as an ATP-competitive inhibitor against NAK (Numb Associated Kinase) family serine/threonine kinase STK16 (IC50/substrate = 0.91 μM/4EBP1 and 1.2 μM/DRG1, [ATP] = 20 μM) with excellent selectivity over a panel of 378 kinases. Despite its inhibitory potency against PI 3-Ks (IC50 = 1.07, 0.856, 0.867 μM against p110α/p85α, p110σ/p85α, p110γ , respectively) in cell-free assays, STK16-IN-1 is ineffective against their cellular activity up to 10 μM concentration. STK16-IN-1 treatment (10 μM for 72 hrs) is shown to cause cell number reduction (~50% in HCT-116 and MCF-7 cultures), as well as increased populations of binucleated cells (~5-fold in MCF-7 culture) and G2/M cells (~7 and 3-fold in HCT-116 and MCF-7 cultures, respectively) in an STK16-dependent manner. A useful tool for elucidating STK16 biological functions.
STK16-IN-1 is a cell-permeable pyrrolonaphthyridinone compound that acts as an ATP-competitive inhibitor against NAK family serine/threonine kinase STK16 with excellent selectivity.

Pictograms

Exclamation mark
GHS07

Signal Word

Warning

Hazard Statements

H315,H319

Hazard Classifications

Eye Irrit. 2 - Skin Irrit. 2

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

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    106M4734V

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