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- 详细信息
- 文献和实验
- 技术资料
- 保存条件:
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 英文名:
SIK inhibitor 1
- 库存:
货期:1-2天
- 供应商:
MedChemExpress LLC
- CAS号:
1456858-58-4
- 规格:
10 mM * 1 mL/1 mg/2 mg/5 mg/10 mg/25 mg
| 规格: | 10 mM * 1 mL | 产品价格: | ¥2435.0 |
|---|---|---|---|
| 规格: | 1 mg | 产品价格: | ¥761.0 |
| 规格: | 2 mg | 产品价格: | ¥1475.0 |
| 规格: | 5 mg | 产品价格: | ¥1950.0 |
| 规格: | 10 mg | 产品价格: | ¥3150.0 |
| 规格: | 25 mg | 产品价格: | ¥5230.0 |
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HG-9-91-01
CAS No. : 1456858-58-4
MCE 国际站:HG-9-91-01
产品活性:HG-9-91-01 是一种有效,选择性的盐诱导型激酶 (SIK) 抑制剂,作用于 SIK1,SIK2 和 SIK3 的 IC50 分别为 0.92 nM,6.6 nM 和 9.6 nM。
作用靶点:Salt-inducible Kinase (SIK)
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.
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文献和实验3.58 3.41 3.29 3.20 3.12 3.06 2.96 2.86 2.76 2.64 2.52 2.39 15 16 4.69 4.08 3.73 3.50 3.34 3.22 3.12 3.05 2.99 2.89 2.79 2.68 2.57 2.45 2.32 16 17 4.62 4.01 3.66 3.44 3.28 3.16 3.06 2.98 2.92 2.82 2.72 2.62 2.50 2.38 2.25 17 18 4.56 3.95
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8.79 8.74 8.71 8.69 8.67 8.66 3 4 7.71 6.94 6.59 6.39 6.26 6.16 6.09 6.04 6.00 5.96 5.91 5.87 5.84 5.82 5.80 4 5 6.61 5.79 5.41 5.19 5.05 4.95 4.88 4.82 4.77 4.74 4.68 4.64 4.60 4.58 4.56 5 6 5.99 5.14 4.76 4.53 4.39 4.28 4.21 4.15 4.10 4.06 4.00
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