401480
IKK Inhibitor III, BMS-345541
IKK Inhibitor III, BMS-345541, CAS 445430-58-0, is a cell-permeable, potent, selective, and allosteric site-binding inhibitor of IKK-2 (IC50 = ~ 300 nM).
동의어(들):
IKK Inhibitor III, BMS-345541, 4-(2ʹ-Aminoethyl)amino-1,8-dimethylimidazo[1,2-a]quinoxaline
조직 및 계약 가격을 보려면 로그인를 클릭합니다.
크기 선택
제품정보 (DICE 배송 시 비용 별도)
실험식(Hill 표기법):
C14H17N5 · 2C2HF3O2
CAS 번호:
Molecular Weight:
483.36
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥96% (HPLC)
Form:
solid
Quality level:
Storage condition:
OK to freeze
desiccated (hygroscopic)
protect from light
desiccated (hygroscopic)
protect from light
제품 이름
IKK Inhibitor III, BMS-345541, IKK Inhibitor III, BMS-345541, CAS 445430-58-0, is a cell-permeable, potent, selective, and allosteric site-binding inhibitor of IKK-2 (IC50 = ~ 300 nM).
SMILES string
[n]21c(ncc2C)c(nc3c1cc(cc3)C)NCCN
InChI
1S/C14H17N5/c1-9-3-4-11-12(7-9)19-10(2)8-17-14(19)13(18-11)16-6-5-15/h3-4,7-8H,5-6,15H2,1-2H3,(H,16,18)
InChI key
PSPFQEBFYXJZEV-UHFFFAOYSA-N
assay
≥96% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
desiccated (hygroscopic)
protect from light
color
off-white
solubility
DMSO: 5 mg/mL
shipped in
ambient
storage temp.
2-8°C
Quality Level
Biochem/physiol Actions
Cell permeable: yes
Product does not compete with ATP.
Reversible: no
Target IC50: ~300 nM against IKK-2; 4 µM against cellular IκBα phosphorylation in THP-1 cells; 1-5 µM LPS-induced cytokine production in THP-1 cells
Disclaimer
Toxicity: Standard Handling (A)
General description
A cell-permeable quinoxaline compound that displays anti-inflammatory properties. Acts as a potent, selective, and allosteric site-binding inhibitor of IKK-2 (IC50 = ~ 300 nM). Exhibits ~10-fold greater selectivity over IKK-1 (IC50 = ~ 4 µM) and no activity towards IKKε and a panel of more than 15 unrelated protein kinases even at concentrations as high as 100 µM. Inhibits cellular IκBα phosphorylation (IC50 = 4 µM in THP-1 cells) and LPS-induced cytokine production both in vitro (IC50 = 1-5 µM in THP-1 cells) and in vivo (IC50 = 10 mg/kg in mice). Effectively blocks inflammation and joint destruction in a murine arthritis model.
A cell-permeable, potent, selective, and allosteric site-binding inhibitor of IKK-2 (IC50 ~300 nM) that displays anti-inflammatory properties. Exhibits ~10-fold greater selectivity for IKK-2 over IKK-1 (IC50 ~4.0 µM) and does not inhibit IKKε and a panel of more than 15 unrelated protein kinases even at concentrations as high as 100 µM. Inhibits cellular IκBα phosphorylation (IC50 = 4 µM in THP-1 cells) and LPS-induced cytokine production both in vitro (IC50 = 1-5 µM in THP-1 cells) and in vivo (IC50 = 10 mg/kg in mice). Effectively blocks inflammation and joint destruction in a murine arthritis model.
Other Notes
Townsend, R.M., et al. 2004. Transplantation77, 1090.
MacMaster, J.F., et al. 2003. Inflamm. Res.52, 508.
McIntyre, K.W., et al. 2003. Arthritis Rheum.48, 2652.
Burke, J. R., et al. 2003. J. Biol. Chem.278, 1450.
MacMaster, J.F., et al. 2003. Inflamm. Res.52, 508.
McIntyre, K.W., et al. 2003. Arthritis Rheum.48, 2652.
Burke, J. R., et al. 2003. J. Biol. Chem.278, 1450.
Packaging
Packaged under inert gas
Physical form
Supplied as bis-TFA salt.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
저장 등급
11 - Combustible Solids
wgk
WGK 1
flash_point_f
Not applicable
flash_point_c
Not applicable
시험 성적서(COA)
제품의 로트/배치 번호를 입력하여 시험 성적서(COA)을 검색하십시오. 로트 및 배치 번호는 제품 라벨에 있는 ‘로트’ 또는 ‘배치’라는 용어 뒤에서 찾을 수 있습니다.
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국제 무역 품목 번호
| SKU | GTIN |
|---|---|
| 401480-1MGCN | 04055977211955 |
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