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HG-9-91-01

Catalog No. T4599   CAS 1456858-58-4
Synonyms: SIK inhibitor 1

HG-9-91-01 (SIK inhibitor 1) 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 Chemical Structure
HG-9-91-01, CAS 1456858-58-4
Pack Size Availability Price/USD Quantity
1 mg In stock $ 76.00
2 mg In stock $ 97.00
5 mg In stock $ 163.00
10 mg In stock $ 289.00
25 mg In stock $ 483.00
50 mg In stock $ 693.00
100 mg In stock $ 988.00
1 mL * 10 mM (in DMSO) In stock $ 197.00
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Purity: 99.64%
Purity: 96.86%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description HG-9-91-01 (SIK inhibitor 1) 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, SIK2:6.6 nM, SIK3:9.6 nM
In vitro HG-9-91-01, a recently identified inhibitor of SIK1-3 and various other kinases, targets numerous protein tyrosine kinases with a threonine residue at their gatekeeper site, including members of the Src family (Src, Lck, and Yes), BTK, and the FGF and Ephrin receptors. This compound has been shown to significantly inhibit SIK2, thereby enhancing IL-10 production, with effects akin to those observed with PGE2 treatment—demonstrating potentiation of zymosan-induced IL-10 production in a concentration-dependent manner with an EC50 of approximately 200 nM. Moreover, HG-9-91-01 exhibits over 100-fold greater potency against SIKs compared to AMPK in cell-free assays (IC50=4.5 μM). Additionally, treatment with HG-9-91-01 leads to a dose-dependent increase in mRNA expression of Pck1 and G6pc, paralleling the effects of 0.1 μM glucagon, and consequently results in elevated glucose production.
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 567.68
Formula C32H37N7O3
CAS No. 1456858-58-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

30% propylene glycol plus 70% ethanol: Soluble

DMSO: 50 mg/mL (88.08 mM)

TargetMolReferences 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.

TargetMolCitations

1. Huang J, Fan H, Chen Y M, et al.The salt-inducible kinases inhibitor HG-9-91-01 exhibits antidepressant-like actions in mice exposed to chronic unpredictable mild stress.Neuropharmacology.2023: 109437. 2. Li X W, Yuan S C, Wang M, et al.Rosmarinic acid ameliorates autoimmune responses through suppression of intracellular nucleic acid-mediated type I interferon expression.Biochemical and Biophysical Research Communications.2023

Related compound libraries

This product is contained In the following compound libraries:
Highly Selective Inhibitor Library Kinase Inhibitor Library Inhibitor Library Anti-Colorectal Cancer Compound Library Anti-Aging Compound Library Covalent Inhibitor Library Anti-Ovarian Cancer Compound Library Anti-Cancer Metabolism Compound Library Nonsteroidal Anti-Inflammatory Compound Library Neuronal Differentiation Compound Library

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Keywords

HG-9-91-01 1456858-58-4 PI3K/Akt/mTOR signaling 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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