2. Epigenetics Stem Cell/Wnt Protein Tyrosine Kinase/RTK JAK/STAT Signaling Metabolic Enzyme/Protease
  3. JAK Phosphodiesterase (PDE)
  4. TyK2-IN-2

TyK2-IN-2 (Compoud 18) est un inhibiteur de TYK2 qui est puissant et sélectif avec des IC50s de 7 nM, 0,1 μM et 0,05 μM pour TYK2 JH2, IL-23 et IFNα, respectivement. TyK2-IN-2 inhibe également la phosphodiestérase 4 (PDE4) avec un IC50 de 62 nM. TyK2-IN-2 peut être utilisé pour la recherche des maladies inflammatoires et auto-immunes.

TyK2-IN-2 (Compoud 18) is a potent and selective TYK2 inhibitor with IC50s of 7 nM, 0.1 μM and 0.05 μM for TYK2 JH2, IL-23 and IFNα, respectively. TyK2-IN-2 also inhibits phosphodiesterase 4 (PDE4) with an IC50 of 62 nM. TyK2-IN-2 can be used for the research of inflammatory and autoimmune diseases.

For research use only. We do not sell to patients.

TyK2-IN-2 Chemical Structure

TyK2-IN-2 Chemical Structure

CAS No. : 2098466-94-3

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 369 In-stock
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10 mM * 1 mL in DMSO USD 369 In-stock
Solid
1 mg USD 180 In-stock
5 mg USD 540 In-stock
10 mg USD 780 In-stock
50 mg USD 2340 In-stock
100 mg USD 3360 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

TyK2-IN-2 Related Antibodies

Top Publications Citing Use of Products

View All JAK Isoform Specific Products:

View All Isoforms
JAK1 JAK2 JAK3 Tyk2 JAK

View All Phosphodiesterase (PDE) Isoform Specific Products:

View All Isoforms
PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

  • Biological Activity

  • Purity & Documentation

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  • Customer Review

Description

TyK2-IN-2 (Compoud 18) is a potent and selective TYK2 inhibitor with IC50s of 7 nM, 0.1 μM and 0.05 μM for TYK2 JH2, IL-23 and IFNα, respectively. TyK2-IN-2 also inhibits phosphodiesterase 4 (PDE4) with an IC50 of 62 nM. TyK2-IN-2 can be used for the research of inflammatory and autoimmune diseases[1].

IC50 & Target

Tyk2 JH2

7 nM (IC50)

PDE4

62 nM (IC50)

In Vitro

A co-crystal structure of TyK2-IN-2 (Compoud 18) bound to the TYK2 JH2 is solved. First, limited room between C8 and the hinge is seen, consistent with the loss in affinity seen with groups larger than methylamino at this position. There are also hydrogen bonds revealed between the NH of the C8 methylamine and from N1 of the IZP core to the ‘hinge’ (Val690). Additional hydrogen bonds are observed from the oxygen of the C3 amide to Lys642 and to the hinge carbonyl of Glu688 through a bridging water molecule. The pocket proximal to the C3 amide of the TYK2 JH2 domain contains a combination of residues which are largely unique relative to the kinome such as a small residue (Ala671) under the “gatekeeper” (Thr687) and the replacement of the highly kinase-conserved DFG motif by DPG which alters the positioning of the conserved catalytic Lys642 and Asp759. The ability of the C3 amide to fit and bind to this pocket is believed to be a key source of kinome selectivity for TyK2-IN-2 (Compoud 18)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

TyK2-IN-2 Related Antibodies
Molecular Weight

310.35

Formula

C16H18N6O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CNC1=CC(NC2=CC(C)=CC(C)=C2)=NN3C1=NC=C3C(N)=O
Shipping

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

DMSO : ≥ 25 mg/mL (80.55 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.2222 mL 16.1108 mL 32.2217 mL
5 mM 0.6444 mL 3.2222 mL 6.4443 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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

Purity: 98.64%

COA (251 KB) LCMS (270 KB)

Handling Instructions (2659 KB)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.2222 mL 16.1108 mL 32.2217 mL 80.5542 mL
5 mM 0.6444 mL 3.2222 mL 6.4443 mL 16.1108 mL
10 mM 0.3222 mL 1.6111 mL 3.2222 mL 8.0554 mL
15 mM 0.2148 mL 1.0741 mL 2.1481 mL 5.3703 mL
20 mM 0.1611 mL 0.8055 mL 1.6111 mL 4.0277 mL
25 mM 0.1289 mL 0.6444 mL 1.2889 mL 3.2222 mL
30 mM 0.1074 mL 0.5370 mL 1.0741 mL 2.6851 mL
40 mM 0.0806 mL 0.4028 mL 0.8055 mL 2.0139 mL
50 mM 0.0644 mL 0.3222 mL 0.6444 mL 1.6111 mL
60 mM 0.0537 mL 0.2685 mL 0.5370 mL 1.3426 mL
80 mM 0.0403 mL 0.2014 mL 0.4028 mL 1.0069 mL
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TyK2-IN-2 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:

TyK2-IN-22098466-94-3JAKPhosphodiesterase (PDE)Janus kinaseInhibitorinhibitorinhibit

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