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Merck
모든 사진(1)

주요 문서

401486

Sigma-Aldrich

IKK Inhibitor VII

The IKK Inhibitor VII, also referenced under CAS 873225-46-8, controls the biological activity of IKK. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

동의어(들):

IKK Inhibitor VII, IKK 16

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About This Item

실험식(Hill 표기법):
C28H29N5OS
CAS Number:
Molecular Weight:
483.63
MDL number:
UNSPSC 코드:
12352200
NACRES:
NA.28

Quality Level

분석

≥97% (HPLC)

양식

solid

제조업체/상표

Calbiochem®

저장 조건

OK to freeze
protect from light

색상

pale yellow

solubility

DMSO: 10 mg/mL

배송 상태

wet ice

저장 온도

−20°C

SMILES string

[s]1c2c(cc1c3nc(ncc3)Nc4ccc(cc4)C(=O)N5CCC(CC5)N6CCCC6)cccc2

InChI

1S/C28H29N5OS/c34-27(33-17-12-23(13-18-33)32-15-3-4-16-32)20-7-9-22(10-8-20)30-28-29-14-11-24(31-28)26-19-21-5-1-2-6-25(21)35-26/h1-2,5-11,14,19,23H,3-4,12-13,15-18H2,(H,29,30,31)

InChI key

BWZJBXAPRCVCKQ-UHFFFAOYSA-N

일반 설명

A cell-permeable benzamido-pyrimidine compound that acts as a potent, selective, and ATP-competitive inhibitor of IKK (IC50 = 40 nM, 70 nM, and 200 nM for IKK-2, IKK complex, and IKK-1, respectively). Inhibits cellular IκBα degradation and NF-κB-mediated gene expression in vitro in HUVEC cells and has been shown to exhibit excellent in vivo efficacy both in mice and rats.
A cell-permeable benzamido-pyrimidine compound that acts as a potent, selective, and ATP-competitive inhibitor of IKK (IC50 = 40 nM, 70 nM, and 200 nM for IKK-2, IKK complex, and IKK-1, respectively). Inhibits cellular IκBα degradation and NF-κB-mediated gene expression in vitro in HUVEC cells and has been shown to exhibit excellent in vivo efficacy both in mice and rats. Also available as a 10 mM solution in DMSO (Cat. No. 505378).

생화학적/생리학적 작용

Cell permeable: yes
Primary Target
IKK
Product competes with ATP.
Reversible: no
Target IC50: 40 nM, 70 nM, and 200 nM for IKK-2, IKK complex, and IKK-1, respectively

포장

Packaged under inert gas

경고

Toxicity: Harmful (C)

법적 정보

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

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable


시험 성적서(COA)

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문서 라이브러리 방문

Rudolf Waelchli et al.
Bioorganic & medicinal chemistry letters, 16(1), 108-112 (2005-10-21)
The design, synthesis, and the biological evaluation of 2-benzamido-pyrimidines as novel IKK inhibitors are described. By optimization of the lead compound 3, compounds 16 and 24 are identified as good inhibitors of IKK2 with IC(50) values of 40 and 25
Sabine Matou-Nasri et al.
PloS one, 17(5), e0267855-e0267855 (2022-05-06)
Most of the AML patients in remission develop multidrug resistance after the first-line therapy and relapse. AML stem cells have gained attention for their chemoresistance potentials. Chemoresistance is a multifactorial process resulting from altered survival signaling pathways and apoptosis regulators
Y Liu et al.
Journal of immunology research, 2023, 1884439-1884439 (2023-01-28)
Platelets have toll-like receptors (TLRs); however, their function in thrombosis or hemostasis under flow conditions is not fully known. Thrombin-inhibited anticoagulated whole blood was treated with various TLR agonists and then perfused over fibrillar collagen using microfluidic assay at venous
ATP Consumption Is Coupled with Endocytosis in Exudated Neutrophils.
Wang, et al.
International Journal of Molecular Sciences, 24 (2023)
A frequent SNP in TRIM5I? strongly enhances the innate immune response against LINE-1 elements.
Lagisquet, et al.
Frontiers in Immunology, 14, 1168589-1168589 (2023)

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