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Cat # PKI-SB203-010 SB 203580 Size: 10 mg M.W.=377.44 Batch No.: 1A/2004002 15875 Gaither Drive Gaithersburg, MD 20877 FAX. 301-560-4919 TEL. 301-330-5966 Toll Free. 1-866-918-6812 Email: [email protected] Web: www.signagenlabs.com Description: SB203580 is a highly selective and cell permeable i nhibitor of p38 mitogen-activated protein kinase wi th IC50 values of 50 and 500 nM for p38/SAPK2a and p38/SAPK2b respectively. Also inhibits the phosphoi nositide-dependent protein kinase 1 (PDK1) at 10-fo ld higher concentrations (IC50 ~3-5 µM). Displays 100-500-fold selectivity over Lck, GSK3b and Akt/PK B. Shown to inhibit interleukin-2-induced T-cell p roliferation, cyclooxygenase-1 and -2 and thromboxa ne synthase. PHYSICAL AND CHEMICAL PROPERTIES Batch Molecular Formula: C21H16FN3OS Batch Molecular Weight: 377.44 CAS No: [152121-47-6] Physical Appearance: White solid Melting Point (°C): 249 - 250 Solubility: DMSO to 25 mM 1eq. HCl to 100 mM ANALYTICAL DATA TLC: R f = 0.23 (Dichloromethane:Methanol [10:1]) HPLC: Shows 100% purity 1 H NMR: Consistent with authentic reference materi al Molecular Structure This product is for laboratory research ONLY and not for diagnostic use 2006 SignaGen Laboratories References: 1. Cuenda et al (1995) SB 203580 is a specific inhibitor of a MAP kinase ho mologue which is stimulated by cellul ar stresses and interleukin-1. FEBS L ett. 364 229. 2. Saklatvala et al (1996) Role for p 38 mitogen-activated protein kinase i n platelet aggregation caused by coll agen on a thromboxane analogue. J. Bi ol. Chem. 271 6586. 3. Borsch-Haubold et al (1998) Direct inhibition of cyclooxygenase-1 and -2 by the kinase inhibitors SB 203580 an d PD 98059. J. Biol. Chem. 273 28766. 4. Davies et al (2000) Specificity an d mechanism of action of some commonl y used protein kinase inhibitors. Bio chem. J. 351 95. Storage: Desiccate at +4°C . Produc t shipped at ambient temperature.

Cat # PKI-SB203-010

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SB 203580 Size: 10 mg M.W.=377.44 Batch No.: 1A/2004002. Cat # PKI-SB203-010. 15875 Gaither Drive Gaithersburg, MD 20877 FAX. 301-560-4919 TEL. 301-330-5966 Toll Free. 1-866-918-6812 Email: [email protected] Web: www.signagenlabs.com. - PowerPoint PPT Presentation

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Page 1: Cat # PKI-SB203-010

Cat

# P

KI-

SB

203-0

10

SB 203580

Size: 10 mgM.W.=377.44Batch No.: 1A/2004002

15875 Gaither DriveGaithersburg, MD 20877FAX. 301-560-4919TEL. 301-330-5966Toll Free. 1-866-918-6812Email: [email protected]

Web: www.signagenlabs.com

Description:

SB203580 is a highly selective and cell permeable inhibitor of p38 mitogen-activated protein kinase with IC50 values of 50 and 500 nM for p38/SAPK2a and p38/SAPK2b respectively. Also inhibits the phosphoinositide-dependent protein kinase 1 (PDK1) at 10-fold higher concentrations (IC50 ~3-5 µM). Displays 100-500-fold selectivity over Lck, GSK3b and Akt/PKB. Shown to inhibit interleukin-2-induced T-cell proliferation, cyclooxygenase-1 and -2 and thromboxane synthase.

PHYSICAL AND CHEMICAL PROPERTIES

Batch Molecular Formula: C21H16FN3OSBatch Molecular Weight: 377.44CAS No: [152121-47-6]Physical Appearance: White solidMelting Point (°C): 249 - 250Solubility: DMSO to 25 mM 1eq. HCl to 100 mM

ANALYTICAL DATA

TLC: R f = 0.23 (Dichloromethane:Methanol [10:1])HPLC: Shows 100% purity1 H NMR: Consistent with authentic reference material

Molecular Structure

This product is for laboratory research ONLY and not for diagnostic use

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006

Sig

na

Ge

n L

abo

rato

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s

References:1. Cuenda et al (1995) SB 203580 is a specific in

hibitor of a MAP kinase homologue which is stimu

lated by cellular stresses and interleukin-1. FEBS

Lett. 364 229.

2. Saklatvala et al (1996) Role for p38 mitogen-ac

tivated protein kinase in platelet aggregation caus

ed by collagen on a thromboxane analogue. J. Bi

ol. Chem. 271 6586.

3. Borsch-Haubold et al (1998) Direct inhibition of

cyclooxygenase-1 and -2 by the kinase inhibitors

SB 203580 and PD 98059. J. Biol. Chem. 273 28

766.

4. Davies et al (2000) Specificity and mechanism

of action of some commonly used protein kinase i

nhibitors. Biochem. J. 351 95.

Storage: Desiccate at +4°C . Product shipped a

t ambient temperature.