Product Details
| Product Name:
HG-9-91-01 |
CAS No.:
1456858-58-4 |
| Purity:
99.64% |
Supply Ability:
10g |
| Release date:
2024/11/16 |
Product Introduction
Bioactivity
| 名称 | HG-9-91-01 |
| 描述 | 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. |
| 细胞实验 | 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]. |
| 体外活性 | 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. |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | 30% propylene glycol plus 70% ethanol : Soluble
DMSO : 50 mg/mL (88.08 mM)
|
| 关键字 | Salt-inducible Kinase (SIK) | HG99101 | SIK inhibitor-1 | SIK inhibitor1 | inhibit | HG 9 91 01 | HG-9-91-01 | Inhibitor |
| 相关产品 | YKL-06-061 | MRT 67307 dihydrochloride | Pterosin B | GLPG3970 | ARN-3236 | WH-4-025 | YKL-05-099 | YKL-06-062 |
| 相关库 | 高选择性抑制剂库 | 经典已知活性库 | 抗糖尿病库 | 激酶抑制剂库 | 抗乳腺癌化合物库 | 抑制剂库 | 干细胞分化化合物库 | 抗前列腺癌化合物库 | 抗衰老化合物库 | 已知活性化合物库 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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