URMC-099

For research use only. Not for therapeutic Use.

  • CAT Number: I000904
  • CAS Number: 1229582-33-5
  • Molecular Formula: C₂₇H₂₇N₅
  • Molecular Weight: 421.55
  • Purity: 97%
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URMC-099(Cat No.:I000904)is a potent, brain-penetrant inhibitor of mixed-lineage kinases (MLKs), which are involved in the regulation of neuroinflammation and neuronal survival. By inhibiting MLKs, URMC-099 effectively blocks downstream activation of JNK and p38 MAPK, reducing inflammation and protecting against neurotoxic effects. It has been studied for its potential to treat neurodegenerative diseases such as Alzheimer’s and Parkinson’s, as well as HIV-associated neurocognitive disorders. URMC-099 is a valuable tool in researching the role of MLKs in neuroinflammation, providing insights into therapeutic strategies for neuroprotective and anti-inflammatory treatments.


Catalog Number I000904
CAS Number 1229582-33-5
Synonyms

3-(1H-indol-5-yl)-5-[4-[(4-methyl-1-piperazinyl)methyl]phenyl]-1H-pyrrolo[2,3-b]pyridine; URMC099

Molecular Formula C₂₇H₂₇N₅
Purity 97%
Target Autophagy
Solubility DMSO: ≥ 33 mg/mL
Appearance Solid powder
Storage -20°C
IC50 14 nM
IUPAC Name 3-(1H-indol-5-yl)-5-[4-[(4-methylpiperazin-1-yl)methyl]phenyl]-1H-pyrrolo[2,3-b]pyridine
InChI InChI=1S/C27H27N5/c1-31-10-12-32(13-11-31)18-19-2-4-20(5-3-19)23-15-24-25(17-30-27(24)29-16-23)21-6-7-26-22(14-21)8-9-28-26/h2-9,14-17,28H,10-13,18H2,1H3,(H,29,30)
InChIKey QKKIWEILHCXECO-UHFFFAOYSA-N
SMILES CN1CCN(CC1)CC2=CC=C(C=C2)C3=CC4=C(NC=C4C5=CC6=C(C=C5)NC=C6)N=C3
Reference

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1:The mixed-lineage kinase 3 inhibitor URMC-099 facilitates microglial amyloid-&beta; degradation. Dong W, Embury CM, Lu Y, Whitmire SM, Dyavarshetty B, Gelbard HA, Gendelman HE, Kiyota T.J Neuroinflammation. 2016 Jul 11;13(1):184. doi: 10.1186/s12974-016-0646-z. PMID: 27401058 Free PMC Article<br />
2:The mixed lineage kinase-3 inhibitor URMC-099 improves therapeutic outcomes for long-acting antiretroviral therapy. Zhang G, Guo D, Dash PK, Ara&iacute;nga M, Wiederin JL, Haverland NA, Knibbe-Hollinger J, Martinez-Skinner A, Ciborowski P, Goodfellow VS, Wysocki TA, Wysocki BJ, Poluektova LY, Liu XM, McMillan JM, Gorantla S, Gelbard HA, Gendelman HE.Nanomedicine. 2016 Jan;12(1):109-22. doi: 10.1016/j.nano.2015.09.009. Epub 2015 Oct 22. PMID: 26472049 Free PMC Article<br />
3:The new small-molecule mixed-lineage kinase 3 inhibitor URMC-099 is neuroprotective and anti-inflammatory in models of human immunodeficiency virus-associated neurocognitive disorders. Marker DF, Tremblay M&Egrave;, Puccini JM, Barbieri J, Gantz Marker MA, Loweth CJ, Muly EC, Lu SM, Goodfellow VS, Dewhurst S, Gelbard HA.J Neurosci. 2013 Jun 12;33(24):9998-10010. doi: 10.1523/JNEUROSCI.0598-13.2013. PMID: 23761895 Free PMC Article

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