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Submit ReviewML 120B dihydrochloride is a novel, ATP-competitive IKK2-selective inhibitor (IC50 = 60 nM at 50 μM ATP). Exhibits no inhibition at IKK1 (EC50 >100 μM), IKKε (EC50 >100 μM) or a panel of 28 other kinases (EC50 >50 μM). Exhibits antitumor activity in lymphoma-bearing SCID mice. Demonstrates synergistic cytotoxic effects with vincristine (Cat. No. 1257).
ML 120B dihydrochloride is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Antiviral Library. 了解 Tocris 化合物库的更多信息。
分子量 | 439.72 |
公式 | C19H15ClN4O2.2HCl |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 1782573-78-7 |
PubChem ID | 90488985 |
InChI Key | AWKOVWFBTRXQLW-UHFFFAOYSA-N |
Smiles | ClC1=C(OC)C(NC(C4=CC=CN=C4C)=O)=C2C(C(C=CN=C3)=C3N2)=C1.Cl.Cl |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 8.79 | 20 | |
water | 2.2 | 5 温和加热 |
以下数据基于产品分子量 439.72。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
0.2 mM | 11.37 mL | 56.85 mL | 113.71 mL |
1 mM | 2.27 mL | 11.37 mL | 22.74 mL |
2 mM | 1.14 mL | 5.69 mL | 11.37 mL |
10 mM | 0.23 mL | 1.14 mL | 2.27 mL |
参考文献是支持产品生物活性的出版物。
Catley et al (2006) Validation of the anti-inflammatory properties of small-molecule IkappaB Kinase (IKK)-2 inhibitors by comparison with adenoviral-mediated delivery of dominant-negative IKK1 and IKK2 in human airways smooth muscle. Mol.Pharmacol. 70 697 PMID: 16687566
Nagashima et al (2006) Rapid TNFR1-dependent lymphocyte depletion in vivo with a selective chemical inhibitor of IKKbeta. Blood 107 4266 PMID: 16439676
Al-Katib et al (2010) I-kappa-kinase-2 (IKK-2) inhibition potentiates vincri. cytotoxicity in non-Hodgkin's lymphoma. Mol.Cancer 9 1476 PMID: 20809973
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RAW macrophages were incubated with 1 μM ML 120B for 30 min prior to addition of 200 ng/ml LPS for 8 h to follow TNFa mRNA expression. LPS elevated TNFa mRNA levels that was significantly inhibited by pretreatment of cells with ML 120B.