YKL-05-099 manufacturers
- YKL-05-099
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- $68.00
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2026-07-14
- CAS:1936529-65-5
- Purity: 99.89%
- Supply Ability: 10g
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| | YKL-05-099 Basic information |
| Product Name: | YKL-05-099 | | Synonyms: | YKL-05-099;Pyrimido[4,5-d]pyrimidin-2(1H)-one, 3-(2-chloro-6-methylphenyl)-3,4-dihydro-7-[[2-methoxy-4-(1-methyl-4-piperidinyl)phenyl]amino]-1-(5-methoxy-2-pyridinyl)-;3-(2-Chloro-6-methylphenyl)-7-((2-methoxy-4-(1-methylpiperidin-4-yl)phenyl)amino)-1-(5-methoxypyridin-2-yl)-3,4-dihydropyrimido[4,5-d]pyrimidin-2(1H)-one;YKL05099,YKL 05 099,inhibit,Salt-inducible Kinase (SIK),Inhibitor;YKL-05-099, 10 mM in DMSO | | CAS: | 1936529-65-5 | | MF: | C32H34ClN7O3 | | MW: | 600.11 | | EINECS: | | | Product Categories: | | | Mol File: | 1936529-65-5.mol |  |
| | YKL-05-099 Chemical Properties |
| Boiling point | 761.0±70.0 °C(Predicted) | | density | 1.311±0.06 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | Soluble in DMSO:103.33(Max Conc. mg/mL);172.18(Max Conc. mM) | | form | A solid | | pka | 8.63±0.20(Predicted) | | color | White to light yellow | | InChIKey | VQINULODWGEVBB-UHFFFAOYSA-N | | SMILES | CC1=CC=CC(Cl)=C1N2C(N(C3=CC=C(OC)C=N3)C4=NC(NC5=C(OC)C=C(C6CCN(C)CC6)C=C5)=NC=C4C2)=O |
| WGK Germany | WGK 3 | | Storage Class | 11 - Combustible Solids |
| | YKL-05-099 Usage And Synthesis |
| Uses | YKL-05-099 is a salt-inducible kinase (SIK) inhibitor. YKL-05-099 binds to SIK1 and SIK3 with IC50s of ~10 and ~30 nM, respectively. YKL-05-099 has slightly less potent SIK2-inhibitory (IC50=40 nM)[1]. | | Biological Activity | Potent and selective salt-inducible kinases (SIK1, SIK2, SIK3) inhibitor in vitro and in vivo.
YKL-05-099 is a potent and selective salt-inducible kinases inhibitor (SIK1/2/3 IC50 = 10/40/30 nM) with superior pharmacokinetic properties than HG-9-91-01. YKL-05-099 pre-treatment of murine BDMCs up-regulates Zymosan A-stimulated IL-10 (EC50 = 460 nM with 24h ), while suppresses inflammatory cytokines production (TNFα, IL-6 and IL-12p40). Likewise, YKL-05-099 intraperitoneal administration in mice (20 mg/kg i.p.) 15 min prior to LPS (0.5 mg/kg i.p.) enhances serum IL-10, while reduces HDAC5 pSer259 levels in total splenic leukocytes and serum TNFα level in vivo. | | in vivo | YKL-05-099 is non-toxic at concentrations less than 10 μM and stable in mouse liver microsomes for more than 2 hours. YKL-05-099 is highly soluble (PBS solubility=428 μM) and present in an unbound state at appreciable levels in mouse plasma. YKL-05-099 dose dependently decreases phosphorylation of HDAC5 at the SIK-regulated site Ser259; reduced phosphorylation is observed at the lowest dose (5 mg/Kg) and is below the limit of detection by immunoblotting beginning at the 20 mg/Kg dose. YKL-05-099 dose-dependently reduces abundance of TNFα in serum beginning at 5 mg/Kg, and increases IL-10 levels at the 20 mg/Kg dose by more than 2-fold[1]. | | IC 50 | SIK1; SIK3 | | References | [1] Sundberg TB, et al. Development of Chemical Probes for Investigation of Salt-Inducible Kinase Function in Vivo. ACS Chem Biol. 2016 Aug 19;11(8):2105-11. DOI:10.1021/acschembio.6b00217 |
| | YKL-05-099 Preparation Products And Raw materials |
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