401481

IKK-2 Inhibitor IV

The IKK-2 Inhibitor IV, also referenced under CAS 507475-17-4, controls the biological activity of IKK-2. This small molecule/inhibitor is primarily used for Inflammation/Immunology applications.

• 동의어(들): IKK-2 Inhibitor IV, [5-( p-Fluorophenyl)-2-ureido]thiophene-3-carboxamide, TPCA-1
• 실험식(Hill 표기법): C₁₂H₁₀FN₃O₂S
• CAS Number: 507475-17-4
• Molecular Weight: 279.29
• MDL number: MFCD09037541
• UNSPSC 코드: 12352200
• NACRES: NA.77

속성

• Quality Level: 100
• 분석: ≥95% (HPLC)
• 양식: solid
• 제조업체/상표: Calbiochem^®
• 저장 조건: OK to freeze; protect from light
• 색상: white to pale yellow
• solubility: DMSO: 10 mg/mL
• 배송 상태: ambient
• 저장 온도: 2-8°C
• SMILES string: Fc1ccc(cc1)c2[s]c(c(c2)C(=O)N)NC(=O)N
• InChI: 1S/C12H10FN3O2S/c13-7-3-1-6(2-4-7)9-5-8(10(14)17)11(19-9)16-12(15)18/h1-5H,(H2,14,17)(H3,15,16,18)
• InChI key: SAYGKHKXGCPTLX-UHFFFAOYSA-N

설명

일반 설명

A 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.

A 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).

생화학적/생리학적 작용

Cell permeable: yes

Primary Target
IKK-2

Product competes with ATP.

Reversible: yes

Target IC₅₀: 18 nM against IKK-2

포장

Packaged under inert gas

경고

Toxicity: Standard Handling (A)

재구성

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

기타 정보

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.

법적 정보

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

안전성 정보

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3