Name: HG-9-91-01
Price: 303.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    HG-9-91-01 is a pan-SIK (salt-inducible kinases) inhibitor with IC50 values of 0.92nM, 6.6nM and 9.6nM for SIK1, SIK2, SIK3, respectively [1].
    SIKs restrict the formation of regulatory macrophages. The inhibition of these enzymes is thought to have potential for treating inflammatory and autoimmune diseases. HG-9-91-01 potently inhibits SIKs through targeting both the ATP-binding site and the small hydrophobic pocket. It is reported that, besides SIKs, HG-9-91-01 also inhibits various protein tyrosine kinases such as Src, BTK, FGF and Ephrin receptors. But other AMPK-related kinase subfamily members are not sensitive to HG-9-91-01. HG-9-91-01 can promote LPS-stimulated IL-10 production, CREB-dependent gene transcription, inhibit proinflammatory cytokine secretion and induce the expression of regulatory macrophage markers [1].
    
    [1] Clark K, MacKenzie K F, Petkevicius K, et al. Phosphorylation of CRTC3 by the salt-inducible kinases controls the interconversion of classically activated and regulatory macrophages. Proceedings of the National Academy of Sciences, 2012, 109(42): 16986-16991.
- Properties
  - Alternative Name
    
    (Z)-N-(2,4-dimethoxyphenyl)-N'-(2,6-dimethylphenyl)-N-(6-((4-(4-methylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)carbamimidic acid
    
    CAS Number
    
    1456858-58-4
    
    Molecular Formula
    
    C32H37N7O3
    
    Molecular Weight
    
    567.68
    
    Purity
    
    98.00%
    
    Solubility
    
    ≥56.8 mg/mL in DMSO; ≥27.3 mg/mL in EtOH; ≥6.35 mg/mL in H2O with ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Caterina Iorio, Jillian L. Rourke, Met al. "Silencing the G-protein coupled receptor 3-salt inducible kinase 2 pathway promotes human β cell proliferation." Commun Biol. 2021 Jul 23;4(1):907. PMID:34302056
    2. Wang Z, Ma J, Met al. "Quantitative phosphoproteomic analysis of the molecular substrates of sleep need." Nature. 2018 Jun;558(7710):435-439. PMID:29899451
    3. Abend A, Shkedi O, et al. "Salt-inducible kinase induces cytoplasmic histone deacetylase 4 to promote vascular calcification." EMBO Rep.2017 Jul;18(7):1166-1185. PMID:28588072

HG-9-91-01

HG-9-91-01

Background

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