2. Immunology/Inflammation Apoptosis
  3. Salt-inducible Kinase (SIK) Interleukin Related TNF Receptor
  4. SIK2-IN-4

SIK2-IN-4 (Compound 4) is a highly selective SIK1/2 inhibitor (IC50s 0.143 and 0.076 μM, respectively). SIK2-IN-4 reduces the phosphorylation of transcription coactivator 3 (CRTC3) by targeting SIK1/2, thereby regulating cAMP response element binding protein (CREB)-dependent transcriptional activity. SIK2-IN-4 inhibits the production of pro-inflammatory cytokines such as TNF (IC50: 0.11 µM), IL-12/23 p40 (IC50: 0.25 µM), and IL-23 (IC50: 0.47 µM), while inducing the expression of the anti-inflammatory cytokine IL-10. SIK2-IN-4 can be used to study intestinal inflammation and other chronic inflammatory diseases.

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SIK2-IN-4

SIK2-IN-4 Chemical Structure

CAS No. : 2810810-00-3

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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SIK2-IN-4 Related Antibodies

Top Publications Citing Use of Products

View All Salt-inducible Kinase (SIK) Isoform Specific Products:

View All Isoforms
SIK1 SIK2 SIK3

View All Interleukin Related Isoform Specific Products:

View All Isoforms
IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

View All TNF Receptor Isoform Specific Products:

View All Isoforms
TNFRSF1A/CD120a TNFRSF3/CD18 TNFRSF4 TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF10B/DR5/CD262 TNFRSF12A/TWEAK TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

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Description

SIK2-IN-4 (Compound 4) is a highly selective SIK1/2 inhibitor (IC50s 0.143 and 0.076 μM, respectively). SIK2-IN-4 reduces the phosphorylation of transcription coactivator 3 (CRTC3) by targeting SIK1/2, thereby regulating cAMP response element binding protein (CREB)-dependent transcriptional activity. SIK2-IN-4 inhibits the production of pro-inflammatory cytokines such as TNF (IC50: 0.11 µM), IL-12/23 p40 (IC50: 0.25 µM), and IL-23 (IC50: 0.47 µM), while inducing the expression of the anti-inflammatory cytokine IL-10. SIK2-IN-4 can be used to study intestinal inflammation and other chronic inflammatory diseases[1].

IC50 & Target[1]

SIK1

0.143 μM (IC50)

SIK2

0.076 μM (IC50)

IL-23

0.47 μM (IC50)

Molecular Weight

388.42

Formula

C21H20N6O2
CAS No.
Appearance

Solid

Color

Yellow to green

SMILES

N#CC1=CC(C2=CC3=CC(NC(C4CC4)=O)=NN3C=C2)=C(OC5CN(C5)C)C=N1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (64.36 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5745 mL 12.8727 mL 25.7453 mL
5 mM 0.5149 mL 2.5745 mL 5.1491 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5745 mL 12.8727 mL 25.7453 mL 64.3633 mL
5 mM 0.5149 mL 2.5745 mL 5.1491 mL 12.8727 mL
10 mM 0.2575 mL 1.2873 mL 2.5745 mL 6.4363 mL
15 mM 0.1716 mL 0.8582 mL 1.7164 mL 4.2909 mL
20 mM 0.1287 mL 0.6436 mL 1.2873 mL 3.2182 mL
25 mM 0.1030 mL 0.5149 mL 1.0298 mL 2.5745 mL
30 mM 0.0858 mL 0.4291 mL 0.8582 mL 2.1454 mL
40 mM 0.0644 mL 0.3218 mL 0.6436 mL 1.6091 mL
50 mM 0.0515 mL 0.2575 mL 0.5149 mL 1.2873 mL
60 mM 0.0429 mL 0.2145 mL 0.4291 mL 1.0727 mL
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SIK2-IN-4 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SIK2-IN-42810810-00-3Salt-inducible Kinase (SIK)Interleukin RelatedTNF ReceptorILTumor Necrosis Factor ReceptorTNFRSIKAMPKIBDCDIL-10TNFimmunological disordersInhibitorinhibitorinhibit

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