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HG-9-91-01

Catalog No. T4599 CAS 1456858-58-4

Synonyms: SIK inhibitor 1

HG-9-91-01 is a potent and highly selective salt-inducible kinase (SIKs) inhibitor with IC50s of 0.92 nM, 6.6 nM and 9.6 nM for SIK1, SIK2 and SIK3respectively.

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HG-9-91-01, CAS 1456858-58-4

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Purity: 98%

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Description	HG-9-91-01 is a potent and highly selective salt-inducible kinase (SIKs) inhibitor with IC50s of 0.92 nM, 6.6 nM and 9.6 nM for SIK1, SIK2 and SIK3respectively.
Targets&IC50	SIK1:0.92 nM, SIK3:9.6 nM, SIK2:6.6 nM
In vitro	HG-9-91-01 inhibits a number of protein tyrosine kinases that possess a threonine residue at the gatekeeper site, such as Src family members (Src, Lck, and Yes), BTK, and the FGF and Ephrin receptors[1]. HG-9-91-01 demonstrates a strong correlation between the potency of SIK2 inhibition and enhanced IL-10 production. In agreement with these reports, pretreating BMDCs with HG-9-91-01, a recently described inhibitor of SIK1-3, along with several other kinases, results in concentration-dependent potentiation of zymosan-induced IL-10 production with an EC50 ~200 nM and a maximum effect similar to that observed with PGE2[2]. HG-9-91-01 has more than a 100-fold greater potency against SIKs than AMPK (IC50=4.5 μM) in a cell-free assay. HG-9-91-01 treatment dose dependently increased mRNA expression of Pck1 and G6pc and that effect is similar in cells treated with 4 μM HG-9-91-01 or 0.1 μM glucagon. Consistent with this observation, there is also a dose-dependent increase in glucose production following HG-9-91-01 treatment[3].
Cell Research	Bone marrow is harvested from femurs and tibias of C57BL/6 mice. Bone-marrow-derived dendritic cells (BMDCs) are differentiated DMEM supplemented with 2 mM GlutaMAX, 10% (vol/vol) FBS, Penicillin, Streptomycin, and 2% mouse granulocyte-macrophage colony-stimulating factor (GM-CSF)-conditioned media derived from murine L cells. Cultures are differentiated for 7 d and routinely analyzed for >90% CD11c (allophycocyanin (APC) anti-CD11c clone HL3) positivity by flow cytometry before use in experiments. Lentiviral transduction of bone marrow cultures is conducted by addition of 293T culture supernatants containing lentiviral particles encoding the CREB-dependent luciferase reporter construct or CRTC3 targeting or control shRNAs 1 d postisolation. Stable integration of lentiviral shRNA constructs is selected by addition of puromycin (3 μg/mL) on day 4 posttransduction. After 2 d, stably transduced BMDCs are released from selection and used in subsequent assays. Unless otherwise indicated, cells are treated for 2 d with PGE2 (5 μM) or HG-9-91-01 (0.5 μM) or an equivalent concentration of DMSO (≤0.5%) and then stimulated for 18 h with LPS (100 ng/mL), R848 (10 μg/mL), or Zymosan (4 μg/mL)[2].

Synonyms	SIK inhibitor 1
Molecular Weight	567.694
Formula	C32H37N7O3
CAS No.	1456858-58-4

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

30% propylene glycol plus 70% ethanol: Soluble

DMSO: 150 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Clark K, et al. Phosphorylation of CRTC3 by the salt-inducible kinases controls the interconversion of classically activated andregulatory macrophages. Proc Natl Acad Sci U S A. 2012 Oct 16;109(42):16986-91. 2. Sundberg TB, et al. Small-molecule screening identifies inhibition of salt-inducible kinases as a therapeutic strategy to enhance immunoregulatory functions of dendritic cells. Proc Natl Acad Sci U S A. 2014 Aug 26;111(34):12468-73. 3. Patel K, et al.The LKB1-salt-inducible kinase pathway functions as a key gluconeogenic suppressor in the liver. Nat Commun. 2014 Aug 4;5:4535. 4. Mujahid N, et al. A UV-Independent Topical Small-Molecule Approach for Melanin Production in Human Skin. Cell Rep. 2017 Jun 13;19(11):2177-2184.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Compound Library Autophagy Compound Library Anti-Lung Cancer Compound Library AMPK-Targeted Compound Library HIF-1 Signaling Pathway Compound Library Glycometabolism Compound Library Anti-Cancer Metabolism Compound Library Lipid Metabolism Compound Library Anti-Pancreatic Cancer Compound Library Inhibitor Library

Related Products

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WH-4-025 ARN-3236 YKL-06-061 HG-9-91-01 MRT 67307 dihydrochloride YKL-05-099

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Keywords

HG-9-91-01 1456858-58-4 PI3K/Akt/mTOR信号通路 SIK Salt-inducible Kinase (SIK) HG99101 SIK inhibitor-1 SIK inhibitor1 inhibit HG 9 91 01 SIK inhibitor 1 Inhibitor inhibitor

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