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URMC-099

Chemical Structure : URMC-099

CAS No.: 1229582-33-5

URMC-099 (URMC099)

Catalog No.: PC-43118Not For Human Use, Lab Use Only.

URMC-099 is a potent, orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3 (MLK3) with IC50 of 14 nM.

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25 mg $198 In stock
50 mg $368 In stock
100 mg $588 In stock
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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

URMC-099 is a potent, orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3 (MLK3) with IC50 of 14 nM.
URMC-099 shows >90% inhibition against 111 kinases in a panel of 442 kinases at 1 uM.
URMC-099 likely functions in HIV-1 associated neurocognitive disorders (HAND) preclinical models by inhibiting multiple kinase pathways, including MLK3 and LRRK2 (IC50=11 nM).
URMC-099 inhibits LPS-induced TNFα release in microglial cells, HIV-1 Tat-induced release of cytokines in human monocytes and up-regulation of phospho-JNK in Tat-injected brains of mice.

Physicochemical Properties

M.Wt 421.5368
Formula C27H27N5
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 33 mg/mL

Chemical Name/SMILES

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

References

1. Marker DF, et al. J Neurosci. 2013 Jun 12;33(24):9998-10010.

2. Goodfellow VS, et al. J Med Chem. 2013 Oct 24;56(20):8032-48.

3. Zhang G, et al. Nanomedicine. 2016 Jan;12(1):109-22.

4. Polesskaya O, et al. Mol Immunol. 2014 Apr;58(2):214-22.

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