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401481 IKK-2 Inhibitor IV - CAS 507475-17-4 - Calbiochem

401481
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
507475-17-4C₁₂H₁₀FN₃O₂S

Products

Catalogue NumberPackaging Qty/Pack
401481-500UG Plastic ampoule 500 μg
Description
OverviewA cell-permeable ureidocarboxamido thiophene compound that acts as a potent, reversible, and ATP-competitive inhibitor of IKK-2 (IC50 = 18 nM) with selectivity over IKK-1, JNK and p38 MAPK. Inhibits TNF-α production in human monocytes (IC50 in the range of 0.15-2.5 µM) and blocks IL-8 and IL-6 production by synovial fibroblasts (IC50 = 100 nM). Further reduces paw oedema in rat arthritis model (~100% inhibition at a dose of 30 mg per kg). A 10 mM (500 µg/179 µl) solution of IKK-2 Inhibitor IV (Cat. No. 401484) in DMSO is available.
Catalogue Number401481
Brand Family Calbiochem®
Synonyms[5-(p-Fluorophenyl)-2-ureido]thiophene-3-carboxamide, TPCA-1
References
ReferencesPodolin, P.L., et al. 2005. J. Pharmacol. Exp. Ther. 312, 373.
Karin, M., et al. 2004. Nat. Rev. Drug Discov. 3, 17.
Roshak, A.K., et al. 2002. Inflamm. Res. 51, S4.
Product Information
CAS number507475-17-4
ATP CompetitiveY
FormPale yellow solid
Hill FormulaC₁₂H₁₀FN₃O₂S
Chemical formulaC₁₂H₁₀FN₃O₂S
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary TargetIKK-2
Primary Target IC<sub>50</sub>18 nM against IKK-2
Purity≥95% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications

Documentation

IKK-2 Inhibitor IV - CAS 507475-17-4 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

IKK-2 Inhibitor IV - CAS 507475-17-4 - Calbiochem Certificates of Analysis

TitleLot Number
401481

References

Reference overview
Podolin, P.L., et al. 2005. J. Pharmacol. Exp. Ther. 312, 373.
Karin, M., et al. 2004. Nat. Rev. Drug Discov. 3, 17.
Roshak, A.K., et al. 2002. Inflamm. Res. 51, S4.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision18-January-2010 RFH
Synonyms[5-(p-Fluorophenyl)-2-ureido]thiophene-3-carboxamide, TPCA-1
DescriptionA cell-permeable, reversible, ATP-competitive, and potent inhibitor of IKK-2 (IC50 = 18 nM) that exhibits selectivity over IKK-1, JNK, and p38 MAPK. Inhibits TNF-α production in human monocytes (IC50 in the range of 0.15-2.5 µM) and blocks IL-8 and IL-6 production by synovial fibroblasts (IC50 = 100 nM). Shown to reduce paw oedema in rat arthritis model (~100% inhibition at a dose of 30 mg per kg).
FormPale yellow solid
Intert gas (Yes/No) Packaged under inert gas
CAS number507475-17-4
Chemical formulaC₁₂H₁₀FN₃O₂S
Structure formulaStructure formula
Purity≥95% by HPLC
SolubilityDMSO (10 mg/ml)
Storage +2°C to +8°C
Protect from light
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity Standard Handling
ReferencesPodolin, P.L., et al. 2005. J. Pharmacol. Exp. Ther. 312, 373.
Karin, M., et al. 2004. Nat. Rev. Drug Discov. 3, 17.
Roshak, A.K., et al. 2002. Inflamm. Res. 51, S4.