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559286

RSK Inhibitor II

Name: RSK Inhibitor II
Brand: MM

The RSK Inhibitor II, also referenced under CAS 501437-28-1, controls the biological activity of RSK. This small molecule/inhibitor is primarily used for Cell Signaling applications.

Synonym(s):

RSK Inhibitor II, 2-(3,5-Difluoro-4-hydroxy-anilino)-8-isopentyl-5,7-dimethyl-7H-pteridin-6-one, racemic, p90 Ribosomal S6 Kinase Inhibitor II, BI-D1870, BID-1870, BID1870

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About This Item

Empirical Formula (Hill Notation):

C₁₉H₂₃F₂N₅O₂

CAS Number:

501437-28-1

Molecular Weight:

391.42

MDL number:

MFCD11223662

UNSPSC Code:

12352200

NACRES:

NA.77

Assay:

≥95% (HPLC)

Form:

solid

Quality level:

100

Storage condition:

OK to freeze, protect from light

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Quality Level

100

assay

≥95% (HPLC)

form

solid

manufacturer/tradename

Calbiochem^®

storage condition

OK to freeze, protect from light

color

off-white

solubility

DMSO: 50 mg/mL

shipped in

ambient

storage temp.

2-8°C

SMILES string

Fc1c(c(cc(c1)Nc2nc3c(cn2)N(C(=O)C(N3CCC(C)C)C)C)F)O

InChI

1S/C19H23F2N5O2/c1-10(2)5-6-26-11(3)18(28)25(4)15-9-22-19(24-17(15)26)23-12-7-13(20)16(27)14(21)8-12/h7-11,27H,5-6H2,1-4H3,(H,22,23,24)

InChI key

DTEKTGDVSARYDS-UHFFFAOYSA-N

Related Categories

Bioactive Small Molecule Inhibitors

General description

The racemic mixture of a cell-permeable dihydropteridinone that acts as a potent and selective RSK inhibitor (IC₅₀ = 31, 24, 18, and 15 nM against RSK1, 2, 3, and 4, respectively; [ATP] = 100 µM) by targeting RSK N-terminal kinase domain in an ATP-competitive manner, while inhibiting 11 other kinases only at higher concentrations (IC₅₀ ≥100 nM) and displaying little activity against 39 others. Shown to selectively inhibit RSK-dependent, but not RSK-independent, cellular protein phosphorylations in PMA-stimulated human HEK-293 cells and EGF-stimulated rat Rat-2 cells (IC₅₀ ~1 µM). A useful pharmacological reagent for studying RSK-mediated cellular signaling events.

Packaging

Packaged under inert gas

Other Notes

Carriere, A., et al. 2008. Curr. Biol.18, 1269
Sapkota, G.P., et al. 2007. Biochem. J.401, 29.
Zaru, R., et al. 2007. Nat. Immunol.8, 1227.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

Storage Class

11 - Combustible Solids

wgk

WGK 2

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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Characteristic ERK1/2 signaling dynamics distinguishes necroptosis from apoptosis.

François Sipieter et al.

iScience, 24(9), 103074-103074 (2021-09-28)

ERK1/2 involvement in cell death remains unclear, although many studies have demonstrated the importance of ERK1/2 dynamics in determining cellular responses. To untangle how ERK1/2 contributes to two cell death programs, we investigated ERK1/2 signaling dynamics during hFasL-induced apoptosis and

Global Trade Item Number

SKU	GTIN
559286-5MG	04055977192377

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