Reagenti e strumenti per immunologia, biologia cellulare e biologia molecolare

HG-9-91-01 [1456858-58-4]

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Cat# NB-64-28859-10mg

Size : 10mg

Marca : Neo Biotech

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HG-9-91-01

(Synonyms: SIK inhibitor 1) Copy Product Info

Synonyms: SIK inhibitor 1

Catalog No. T4599 Copy Product Info

Purity: 99.71%

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.

Cas No. 1456858-58-4

With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.

For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.71%

Color:White

Product Information

Bioactivity

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.
Synonyms	SIK inhibitor 1
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].

Chemical Properties

Molecular Weight	567.68
Formula	C₃₂H₃₇N₇O₃
Cas No.	1456858-58-4
Smiles	COc1ccc(N(C(=O)Nc2c(C)cccc2C)c2cc(Nc3ccc(cc3)N3CCN(C)CC3)ncn2)c(OC)c1
Relative Density.	1.257 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Store at low temperature Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

30% propylene glycol plus 70% ethanol: Soluble

DMSO: 250 mg/mL (440.39 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+90% Saline: < 10 mg/mL (17.62 mM), Lower concentrations may be soluble, but exact solubility limit is unknown.

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 10 mg/mL (17.62 mM), Solution.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.7616 mL	8.8078 mL	17.6156 mL	88.0778 mL
5 mM	0.3523 mL	1.7616 mL	3.5231 mL	17.6156 mL
10 mM	0.1762 mL	0.8808 mL	1.7616 mL	8.8078 mL
20 mM	0.0881 mL	0.4404 mL	0.8808 mL	4.4039 mL
50 mM	0.0352 mL	0.1762 mL	0.3523 mL	1.7616 mL
100 mM	0.0176 mL	0.0881 mL	0.1762 mL	0.8808 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 µL Tween 80 and mix well until fully clarified.

3) Add 450 µL Saline,PBS or ddH₂O and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

Keywords

SIK3SIK2SIK1SIK inhibitor-1SIK inhibitor1Salt-inducible Kinase (SIK)InhibitorinhibitHG-9-91-01HG99101HG 9 91 01

Related Tags: HG-9-91-01 chemical structure | HG-9-91-01 in vitro | HG-9-91-01 formula | HG-9-91-01 molecular weight