1. Epigenetics
    Stem Cell/Wnt
    JAK/STAT Signaling
    Metabolic Enzyme/Protease
  2. JAK
    Phosphodiesterase (PDE)
  3. TyK2-IN-2

TyK2-IN-2 

Cat. No.: HY-101762 Purity: 99.71%
Handling Instructions

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

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10 mM * 1  mL in DMSO USD 369 In-stock
Estimated Time of Arrival: December 31
1 mg USD 180 In-stock
Estimated Time of Arrival: December 31
5 mg USD 540 In-stock
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10 mg USD 780 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2340 In-stock
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100 mg USD 3360 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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].

Molecular Weight

310.35

Formula

C₁₆H₁₈N₆O

CAS No.

2098466-94-3

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 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 25 mg/mL (80.55 mM)

*"≥" 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
10 mM 0.3222 mL 1.6111 mL 3.2222 mL
*Please refer to the solubility information to select the appropriate solvent.
References

Purity: 99.71%

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Keywords:

TyK2-IN-2JAKPhosphodiesterase (PDE)Janus kinaseInhibitorinhibitorinhibit

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