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MRT199665 is a novel and potent salt-inducible kinases (SIKs) inhibitor. MRT199665 increases IL-10 production while suppressing IL-6, IL-12, and TNF secretion.
| ln Vitro |
MRT199665 (1 μM; 1 hour post-death) enhances the synthesis of IL-10 and Nurr77 mRNA in response to LPS (100 ng/mL; stimulation lasting up to 24 hours) [1]. Treatment with MRT199665 inhibits the phosphorylation of MEF2C S222 in acute myeloid leukemia (AML) cells. MRT199665 inhibits the growth of leukemia by causing total MEF2C at 10 nM-1000 nM for 12 hours and -100 μM for 48 hours [2]. Additionally, MRT199665 lowers the amount of MEF2C protein overall [2].
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| Cell Assay |
Western Blot Analysis[2]
Cell Types: OCI-AML2 and MOLM-13 Cell Tested Concentrations: 10, 100, 500, and 1000 nM Incubation Duration: 12 Experimental Results: Compared to untreated cells, 10 nM resulted in total MEF2C and pS222 dose-dependently diminished MEF2C, resulting in a >40% reduction in MEF2C phosphorylation. Cell proliferation assay [2] Cell Types: human AML cell lines OCI-AML2, MV4-11, MOLM-13 and Kasumi-1 with endogenous MEF2C phosphorylation; human AML cell lines NB-4, HEL, HL lacking MEF2C -60 and U937 Tested Concentrations: 1 nM, 10 nM, 100n M, 1 μM, 10 μM, 100μM Incubation Duration: 48 hrs (hours) Experimental Results: Human AML cell lines with endogenous MEF2C phosphorylation vs. cell lines lacking MEF2C (NB- 4. Compared with HEL, HL-60 and U937), (OCI-AML2, MV4-11, MOLM-13 and Kasumi-1) are more sensitive, with an average IC50 of 26±13 and an average IC50 of 990 and ±29 nM respectively. . |
| References |
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| Molecular Formula |
C18H19N3O4S
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|---|---|
| Molecular Weight |
373.426162958145
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| Exact Mass |
469.247
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| CAS # |
1456858-57-3
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| PubChem CID |
71725150
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
4.3
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
35
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| Complexity |
770
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| Defined Atom Stereocenter Count |
1
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| SMILES |
S(C)(C1=NC=C2C(=N1)N(C(C2(C)C)=O)[C@@H]1C2C=CC=C(C=2CC1)O)(=O)=O
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| InChi Key |
LZUYOYKXEXENTQ-ZDUSSCGKSA-N
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| InChi Code |
InChI=1S/C18H19N3O4S/c1-18(2)12-9-19-17(26(3,24)25)20-15(12)21(16(18)23)13-8-7-11-10(13)5-4-6-14(11)22/h4-6,9,13,22H,7-8H2,1-3H3/t13-/m0/s1
|
| Chemical Name |
7-[(1S)-4-Hydroxy-2,3-dihydro-1H-inden-1-yl]-5,5-dimethyl-2-(methylsulfonyl)-5,7-dihydro-6H-pyrrolo[2,3-d]pyrimidin-6-one
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| Synonyms |
MRT199665 MRT-199665 MRT 199665
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~266.20 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.43 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.43 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.43 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6779 mL | 13.3894 mL | 26.7788 mL | |
| 5 mM | 0.5356 mL | 2.6779 mL | 5.3558 mL | |
| 10 mM | 0.2678 mL | 1.3389 mL | 2.6779 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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