AdipoGen Life Sciences

URMC-099

Product Code:
 
SYN-1211
Product Group:
 
Inhibitors and Activators
Regulatory Status:
 
RUO
Shipping:
 
Ambient
Storage:
 
Short term: +4°C. Long term +4°C
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Chemical Structure
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Chemical Structure

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SYN-1211-M100100 mgEnquire
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SYN-1211-M0011 mg£128.00
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Further Information

Alternate Names/Synonyms:
3-(1H-Indol-5-yl)-5-(4-(4-methylpiperazin-1-yl)methyl)phenyl)-1H-pyrrolo[2,3- b]pyridine
Appearance:
Solid.
CAS:
1229582-33-5
EClass:
32160000
Form (Short):
liquid
Handling Advice:
Keep cool and dry.
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
Long Description:
Chemical. CAS: 1229582-33-5. Formula: C27H27N5. MW: 421.5. Inhibition of mixed lineage kinase 3 (MLK-3) is a potential strategy for the treatment of Parkinson's disease and HIV-1 associated neuro-cognitive disorders (HAND), requiring an inhibitor that can achieve significant brain concentration levels. URMC-099 is an orally bioavailable MLK-3 inhibitor with excellent brain exposure in mouse PK models and minimal interference with key human CYP450 enzymes or hERG channels. URMC-099 inhibits multiple kinase pathways, including MLK-3 (14nM) and leucine-rich repeat serine/threonine-protein kinase 2 (LRRK2) (11nM).
Molecular Formula:
C27H27N5
Molecular Weight:
421.5
Package Type:
Plastic Vial
Product Description:
Inhibition of mixed lineage kinase 3 (MLK-3) is a potential strategy for the treatment of Parkinson's disease and HIV-1 associated neuro-cognitive disorders (HAND), requiring an inhibitor that can achieve significant brain concentration levels. URMC-099 is an orally bioavailable MLK-3 inhibitor with excellent brain exposure in mouse PK models and minimal interference with key human CYP450 enzymes or hERG channels. URMC-099 inhibits multiple kinase pathways, including MLK-3 (14nM) and leucine-rich repeat serine/threonine-protein kinase 2 (LRRK2) (11nM).
Purity:
>95% (HPLC)
Solubility Chemicals:
Soluble in DMSO or water.
Transportation:
Non-hazardous
UNSPSC Category:
Protein Kinase Modulators
UNSPSC Number:
12352200
Use & Stability:
Stable for at least 3 years after receipt when stored at -20°C.

References

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: D.F. Marker, et al.; J. Neurosci. 33, 9998 (2013) | Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3: V.S. Goodfellow, et al.; J. Med. Chem. 56, 8032 (2013) | MLK3 regulates fMLP-stimulated neutrophil motility: O. Polesskaya, et al.; Mol. Immunol. 58, 214 (2014)