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SynKinase
URMC-099
CHF 0.00
In stock
SYN-1211-M0011 mgCHF 142.00
SYN-1211-M0055 mgCHF 255.00
SYN-1211-M01010 mgCHF 397.00
SYN-1211-M05050 mgCHF 1'348.00
SYN-1211-M100100 mgINQ
| Product Details | |
|---|---|
| Synonyms | 3-(1H-Indol-5-yl)-5-(4-(4-methylpiperazin-1-yl)methyl)phenyl)-1H-pyrrolo[2,3- b]pyridine |
| Product Type | Chemical |
| Properties | |
| Formula | C27H27N5 |
| MW | 421.5 |
| CAS | 1229582-33-5 |
| Purity Chemicals | ≥95% (HPLC) |
| Appearance | Solid. |
| Solubility | Soluble in DMSO or water. |
| Declaration | Manufactured by SYNkinase. |
| Other Product Data |
Target: MLK-3 | Kinase Group: TKL Click here for Original Manufacturer Product Datasheet Our product description may differ slightly from the original manufacturers product datasheet. |
| InChi Key | QKKIWEILHCXECO-UHFFFAOYSA-N |
| Shipping and Handling | |
| Shipping | AMBIENT |
| Short Term Storage | +4°C |
| Long Term Storage | -20°C |
| Handling Advice | Keep cool and dry. |
| Use/Stability | Stable for at least 3 years after receipt when stored at -20°C. |
| Documents | |
| MSDS |
 Download PDF |
| Product Specification Sheet | |
| Datasheet |
Download PDF |
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).
Product 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)