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- Elad Prinz, .et al. WDR62 mediates TNFα-dependent JNK activation via TRAF2-MLK3 axis, Mol Biol Cell, 2018, Oct 1; 29(20): 2470-2480 PMID: 30091641
Biological Activity
URMC-099 is an orally bioavailable, brain penetrant mixed lineage kinase (MLK) inhibitor with IC50 of 19 nM, 42 nM, 14 nM, and 150 nM, for MLK1, MLK2, MLK3, and DLK, respectively.
Targets
| Target | Value |
|---|---|
| Abl1 | IC50: 6.5nM |
| LRRK2 | IC50: 11nM |
| MLK3 | IC50: 14nM |
| MLK1 | IC50: 19nM |
| VEGFR1/FLT1 | IC50: 39nM |
| MLK2 | IC50: 42nM |
| SGK | IC50: 67nM |
| TrkA | IC50: 85nM |
| AuroraA | IC50: 108nM |
| ROCK2 | IC50: 111nM |
| AuroraB | IC50: 123nM |
| DLK | IC50: 150nM |
| c-Met | IC50: 177nM |
| IR | IC50: 200nM |
| SGK1 | IC50: 201nM |
| TrkB | IC50: 217nM |
| AuroraC | IC50: 290nM |
| IGF-1R | IC50: 307nM |
| LCK | IC50: 333nM |
| MEKK2 | IC50: 661nM |
| Syk | IC50: 731nM |
| ROCK1 | IC50: 1030nM |
| CDK1 | IC50: 1125nM |
| CDK2 | IC50: 1180nM |
| AMPK | IC50: 1512nM |
| JNK1 | IC50: 3280nM |
| Src | IC50: 4330nM |
| ZAP70 | IC50: 5050nM |
| ERK2 | IC50: 6290nM |
| GSK-3β | IC50: >10000nM |
| p38α | IC50: 12050nM |
| In vitro | DMSO | 76 mg/mL (180.28 mM) | |
| Water | Insoluble | ||
| Ethanol | 5 mg/mL (11.86 mM) | ||
|
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
|||
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 23.72 mL | 118.61 mL | 237.23 mL |
| 0.5 mM | 4.74 mL | 23.72 mL | 47.45 mL |
| 1 mM | 2.37 mL | 11.86 mL | 23.72 mL |
| 5 mM | 0.47 mL | 2.37 mL | 4.74 mL |
*The above data is based on the productmolecular weight 421.54. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Catalog Num | A14219 |
|---|---|
| Actions | Inhibitor |
| CAS No. | 1229582-33-5 |
| Formula | C27H27N5 |
| M. Wt | 421.54 |
| Purity | >98% |
| Synonyms | URMC 099,URMC099 |
| SMILES | CN1CCN(CC1)CC2=CC=C(C=C2)C3=CN=C4C(=C3)C(=CN4)C5=CC6=C(C=C5)NC=C6 |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
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