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Biochem/physiol Actions
ATP site-targeting, dual salt-inducible kinase (SIK1/2/3) & p21-activated kinase (PAK2/3) inhibitor with excellent selectivity over other kinases.
MRIA9 is an ATP site-targeting, dual salt-inducible kinase (SIK1/2/3 IC50 = 55/48/22 nM; SIK2/3 IC50 = 180/127 nM by cell-based NanoBRET) & p21-activated kinase (PAK2/3 IC50 = 41/140 nM; PAK1 IC50 = 580 nM) inhibitor with excellent selectivity over other kinases. MRIA9 sensitizes ovarian cancer cells to mitotic agent paclitaxel (Pac) treatment in SKOV3 cultures (1 nM Pac plus 0.5-5 µM MRIA9) and HeLa spheroids (2 nM Pac plus 5 µM MRIA9).
Disclaimer
Hygroscopic
| Quality Segment | 100 |
| assay | ≥96% (HPLC) |
| form | powder |
| storage condition | desiccated |
| color | white to beige |
| solubility | DMSO: 2 mg/mL, clear |
| storage temp. | -10 to -25°C |
| SMILES string | Fc1c(nccc1)c2cc(c(cc2)C3=Cc4c(nc(nc4)NC)N(C3=O)C[C@@H]5OC[C@H](CO5)N)Cl |
| InChI key | QKNBRNSGPNCARD-SGNKCFNYSA-N |
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