GlpBio

ERK5-IN-1

目录号: GC32796纯度: >99.50%同义词: ERK5-IN-1
An ERK5 inhibitor
ERK5-IN-1
Cas No.: 1234479-76-5
规格价格库存数量操作
1mg¥540.00现货
1
5mg¥1,350.00现货
1
10mg¥1,890.00现货
1
25mg¥3,578.00现货
1
50mg¥4,725.00现货
1
10mM (in 1mL DMSO)¥1,364.00现货
1
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文献被引

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产品描述 Description

XMD8-85 is an ERK5 inhibitor (IC50 = 87 nM in an enzyme assay).1 It is selective for ERK5 over tyrosine non-receptor kinase 2 (TNK2; IC50 = 959 nM), but does inhibit the leucine-rich repeat kinase 2 (LRRK2) mutant LRRK2G2019S (IC50 = 26 nM), which has been found in patients with Parkinson’s disease.2,1 XMD8-85 inhibits EGF-induced ERK5 autophosphorylation in HeLa cells (EC50 = 0.19 μM).1

1.Deng, X., Elkins, J.M., Zhang, J., et al.Structural determinants for ERK5 (MAPK7) and leucine rich repeat kinase 2 activities of benzo[e]pyrimido-[5,4-b]diazepine-6(11H)-onesEur. J. Med. Chem.70758-767(2013) 2.Groendyke, B.J., Powell, C.E., Feru, F., et al.Benzopyrimidodiazepinone inhibitors of TNK2Bioorg. Med. Chem. Lett.30(4)126948(2020)

实验参考方法 Experimental Reference Method

Kinase experiment:

Kinase activity is determined in an assay volume of 40 μL in kinase buffer (50 mM Tris-HCl, pH 7.5, 0.1 mM EGTA, 1 mM 2-mercaptoethanol) containing 200 ng of pure active ERK5 and the indicated amount of inhibitor. Reaction started by adding 10 mM magnesium acetate, and 50 μM [γ-32P]-ATP (500 cpm/pmol) and 250 μM PIMtide (ARKKRRHPSGPPTA) as substrates. Assays are carried out for 20 min at 30°C, terminated by applying the reaction mixture onto p81 paper and the incorporated radioactivity measured[1].

References:

[1]. Deng X, et al. Structural determinants for ERK5 (MAPK7) and leucine rich repeat kinase 2 activities of benzo[e]pyrimido-[5,4-b]diazepine-6(11H)-ones. Eur J Med Chem. 2013;70:758-767.

产品文档 Product Documents

Purity:>99.50%

化学性质Chemical Properties

CAS 号
1234479-76-5
同义词
ERK5-IN-1
SMILES
O=C1C2=C(C=CC=C2)N(C)C3=NC(NC4=C(OC)C=C(N5CCN(C)CC5)C=C4)=NC=C3N1C
分子式
C25H29N7O2
分子量
459.54 g/mol
溶解性
DMSO : ≥ 100 mg/mL (217.61 mM)
保存条件
Store at -20°C
General tips
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol