URMC-099
Cat. No.:YN350115
CAS No. :1229582-33-5
产品名称: | URMC-099 |
CAS No.: | 1229582-33-5 |
Chemical Name: | 3-(1H-indol-5-yl)-5-[4-[(4-methyl-1-piperazinyl)methyl]phenyl]-1H-pyrrolo[2,3-b]pyridine |
Synonyms: | URMC-099,URMC 099 |
分子量: | 421.54 |
分子式: | C₂₇H₂₇N₅ |
SMILES: | CN(CC1)CCN1CC(C=C2)=CC=C2C3=CN=C4C(C(C5=CC=C(NC=C6)C6=C5)=CN4)=C3 |
存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
运输: | Room temperature in continental US; may vary elsewhere. |
产品描述: | URMC-099 是一种口服生物有效的混合谱系激酶 3 (MLK3) (IC50=14 nM) 抑制剂,具有优异的血脑屏障穿透性。 |
IC50和靶点: | [{name:"LRRK2:11 nM (IC50)"},{name: "FLT3:4 nM (IC50)"},{name: "FLT1:39 nM (IC50)"},{name: "ABL1 (T315I):3 nM (IC50)"},{name: "ABL1:6.8 nM (IC50)"},{name: "SGK:67 nM (IC50)"},{name: "SGK1:201 nM (IC50)"},{name: "AurA:108 nM (IC50)"},{name: "AurB:123 nM (IC50)"},{name: "AurC:290 nM (IC50)"},{name: "IKKβ:257 nM (IC50)"},{name: "IKKα:591 nM (IC50)"},{name: "TNFα:460 nM (IC50)"},{name: "ROCK1:1030 nM (IC50)"},{name: "ROCK2:111 nM (IC50)"},{name: "CDK1:1125 nM (IC50)"},{name: "CDK2:1180 nM (IC50)"},{name: "TRKA:85 nM (IC50)"},{name: "c-MET:177 nM (IC50)"},{name: "TRKB:217 nM (IC50)"},{name: "IGF1R:307 nM (IC50)"},{name: "LCK:333 nM (IC50)"},{name: "MEKK2:661 nM (IC50)"},{name: "SYK:731 nM (IC50)"},{name: "AMPK:1512 nM (IC50)"},{name: "JNK1:3280 nM (IC50)"},{name: "SRC:4330 nM (IC50)"},{name: "ZAP70:5050 nM (IC50)"},{name: "ERK2:6290 nM (IC50)"},{name: "P38α:12050 nM (IC50)"},{name: "CYP3A4:16.2 μM (IC50)"}] |
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Quadro, L., Blaner, W.S., Salchow, D.J., et al.Impaired retinal function and vitamin A availability in mice lacking retinol-binding proteinEMBO J.18(17),4633-4644(1999)
Marker, D.F., Tremblay, M.É., Puccini, J.M., et al.The new small-molecule mixed-lineage kinase 3 inhibitor URMC-099 is neuroprotective and anti-inflammatory in models of human immunodeficiency virus-associated neurocognitive disordersJ. Neurosci.33(24),9998-10010(2013)