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Merck

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.

別名:

IKK-2 Inhibitor IV, [5-( p-Fluorophenyl)-2-ureido]thiophene-3-carboxamide, TPCA-1

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この商品について

実験式（ヒル表記法）:
C12H10FN3O2S
CAS番号:
507475-17-4
分子量:
279.29
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
MFCD09037541
Assay:
≥95% (HPLC)
Form:
solid
Quality level:
100
Storage condition:
OK to freeze, protect from light

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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

assay

≥95% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

color

white to pale yellow

solubility

DMSO: 10 mg/mL

shipped in

ambient

storage temp.

2-8°C

Quality Level

100

関連するカテゴリー

Biochem/physiol Actions

Cell permeable: yes
Primary Target
IKK-2
Product competes with ATP.
Reversible: yes
Target IC50: 18 nM against IKK-2

Disclaimer

Toxicity: Standard Handling (A)

General description

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).

Other Notes

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.

Packaging

Packaged under inert gas

Preparation Note

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

Legal Information

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

保管分類

11 - Combustible Solids

wgk

WGK 3

適用法令

試験研究用途を考慮した関連法令を主に挙げております。化学物質以外については、一部の情報のみ提供しています。 製品を安全かつ合法的に使用することは、使用者の義務です。最新情報により修正される場合があります。WEBの反映には時間を要することがあるため、適宜SDSをご参照ください。

401481-1.1ML: + 401481-500UG: + 401481-0MG: + 401481-UG: + 401481-10MG:

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試験成績書（COA）

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以前この製品を購入いただいたことがある場合

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文書ライブラリにアクセスする

Haibo Zhang et al.
Science signaling, 17(836), eadd5073-eadd5073 (2024-05-15)
The Ras-mitogen-activated protein kinase (MAPK) pathway is a major target for cancer treatment. To better understand the genetic pathways that modulate cancer cell sensitivity to MAPK pathway inhibitors, we performed a CRISPR knockout screen with MAPK pathway inhibitors on a
Lídia Hernandez et al.
Cancer research, 70(10), 4005-4014 (2010-04-29)
The NF-kappaB family of transcription factors has been implicated in the propagation of ovarian cancer, but the significance of constitutive NF-kappaB signaling in ovarian cancer is unknown. We hypothesized that constitutive NF-kappaB signaling defines a subset of ovarian cancer susceptible
Sang Min Jeon et al.
Virulence, 13(1), 1966-1984 (2022-10-23)
Ohmyungsamycin A (OMS) is a newly identified cyclic peptide that exerts antimicrobial effects against Mycobacterium tuberculosis. However, its role in nontuberculous mycobacteria (NTMs) infections has not been clarified. Mycobacteroides abscessus (Mabc) is a rapidly growing NTM that has emerged as
Kidong Kang et al.
FASEB journal : official publication of the Federation of American Societies for Experimental Biology, 34(3), 4369-4383 (2020-02-07)
In tumor necrosis factor (TNF) signaling, phosphorylation and activation of receptor interacting protein kinase 1 (RIPK1) by upstream kinases is an essential checkpoint in the suppression of TNF-induced cell death. Thus, discovery of pharmacological agents targeting RIPK1 may provide new
Minho Won et al.
Cell death and differentiation, 29(6), 1152-1163 (2021-11-29)
In TNF signaling, ubiquitination of RIP1 functions as an early cell-death checkpoint, which prevents the spatial transition of the signaling complex from complex-I to death-inducing complex-II. Here, we report that ankyrin repeat domain 13a (ANKRD13a) acts as a novel component

グローバルトレードアイテム番号

カタログ番号GTIN
401481-500UGCN04055977211962

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