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

TyK2-IN-2 

目录号: HY-101762 纯度: 99.71%
产品使用指南

TyK2-IN-2 (Compoud 18) 是一种有效的选择性 TYK2 抑制剂,对 TYK2 JH2IL-23IFNαIC50 值分别为 7 nM,0.1 μM 和 0.05 μM。TyK2-IN-2 还抑制磷酸二酯酶 4 (PDE4),其 IC50 为 62 nM。TyK2-IN-2 可用于炎症及自身免疫病的研究。

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TyK2-IN-2 Chemical Structure

TyK2-IN-2 Chemical Structure

CAS No. : 2098466-94-3

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥2724
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1 mg ¥1330
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5 mg ¥3990
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10 mg ¥5800
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50 mg ¥17350
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100 mg ¥24880
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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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)

体外研究
(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].

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

分子量

310.35

Formula

C16H18N6O

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 25 mg/mL (80.55 mM)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 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
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

参考文献

纯度: 99.71%

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质量   浓度   体积   分子量 *
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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2

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产品名称:
TyK2-IN-2
目录号:
HY-101762
需求量: