HG-9-91-01

SKU: orb1222685

Description

HG-9-91-01 is a potent and highly selective salt-inducible kinase (SIKs) inhibitor for SIK1, SIK2 and SIK3. Inhibition of SIK kinase activity induces an anti-inflammatory phenotype in macrophages.

Key Properties

• CAS Number: 1456858-58-4
• MW: 567.68
• Purity: >98% (HPLC)
• Formula: C₃₂H₃₇N₇O₃
• SMILES: CC1=C(C(=CC=C1)C)NC(=O)N(C2=C(C=C(C=C2)OC)OC)C3=NC=NC(=C3)NC4=CC=C(C=C4)N5CCN(CC5)C
• Target: PKC
• Solubility: DMSO : ≥ 150 mg/mL; 264.23 mM

Bioactivity

• 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. 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. 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. Consistent with this observation, there is also a dose-dependent increase in glucose production following HG-9-91-01 treatment.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

HG-9-91-01 | HG-9-91-01 | HG 9-91-01

Quick Database Links

Gene Symbol

PKC