MRT199665 is a potent and ATP-competitive, selective MARK/SIK/AMPK inhibitor with IC50s of 2/2/3/2 nM, 10/10 nM, and 110/12/43 nM for MARK1/MARK2/MARK3/MARK14, AMPKα1/AMPKα2, and SIK1/SIK2/SIK3, respectively. MRT199665 causes apoptosis in MEF2C-activated human acute myeloid leukemias (AML) cells. MRT199665 inhibits the phosphorylation of SIK substrate CRTC3 at S370.
| Molecular Weight | 469.58 |
| Formula | C28H31N5O2 |
| CAS Number | 1456858-57-3 |
| Form | Solid |
| Solubility (25°C) | DMSO 125 mg/mL (ultrasonic) |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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SIKs-IN-1 inhibitor. |
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MR22 is a potent pan-SIK (salt-inducible kinase) inhibitor. |
| SIK2-IN-1
SIK2-IN-1 is a potent SIK2 inhibitor over other AMPK kinases. |
| GLPG3970
GLPG3970 is a first-in-class salt-inducible kinase SIK2/SIK3 inhibitor for studies related to inflammatory and autoimmune diseases such as psoriasis. |
| YKL-06-062
YKL-06-062 is a second-generation salt-inducible kinase (SIK) inhibitor with an IC50 of 2.12 nM/1.40 nM/2.86 nM for SIK1, SIK2 and SIK3, respectively. |
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