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HG-9-91-01

In stock
Catalog No.
B1052
Pan-SIK (salt-inducible kinases) inhibitor
Grouped product items
SizePriceStock Qty
2mg
$162.00
In stock
5mg
$243.00
In stock
10mg
$369.00
In stock
50mg
$875.00
In stock
100mg
$1,361.00
In stock

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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].

References:
[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.

Product Citation

Chemical Properties

StorageStore at -20°C
M.Wt567.68
Cas No.1456858-58-4
FormulaC32H37N7O3
Solubility≥56.8mg/mL in DMSO
Chemical Name(Z)-N-(2,4-dimethoxyphenyl)-N'-(2,6-dimethylphenyl)-N-(6-((4-(4-methylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)carbamimidic acid
SDFDownload SDF
Canonical SMILESCC1=C(/N=C(O)/N(C2=NC=NC(NC3=CC=C(N4CCN(CC4)C)C=C3)=C2)C5=C(OC)C=C(OC)C=C5)C(C)=CC=C1
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Protocol

Cell experiment [1]:

Cell lines

Macrophages

Preparation method

Limited solubility. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reaction Conditions

1 h

Applications

HG-9-91-01increases LPS-stimulated IL-10 production and markedly inhibits proinflammatory cytokine secretion even when WT SIK2 is expressed to the same level. In addition, CRTC3 is required for HG-9-91-01 to enhance IL-10 production in LPS-stimulated primary mouse macrophages.

References:

1. Clark K, MacKenzie KF, Petkevicius K et al. Phosphorylation of CRTC3 by the salt-inducible kinases controls the interconversion of classically activated and regulatory macrophages. Proc Natl Acad Sci U S A. 2012 Oct 16;109(42):16986-91.

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