您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > TYK2-IN-2
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
TYK2-IN-2
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
TYK2-IN-2图片
CAS NO:2098466-94-3
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
1mg电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品介绍
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。
生物活性

TyK2-IN-2 (Compoud 18) is a potent and selectiveTYK2inhibitor withIC50s of 7 nM, 0.1 μM and 0.05 μM forTYK2JH2,IL-23andIFNα, respectively. TyK2-IN-2 also inhibitsphosphodiesterase4 (PDE4)with anIC50of 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].

分子量

310.35

性状

Solid

Formula

C16H18N6O

CAS 号

2098466-94-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 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 mg5 mg10 mg
1 mM3.2222 mL16.1108 mL32.2217 mL
5 mM0.6444 mL3.2222 mL6.4443 mL
10 mM0.3222 mL1.6111 mL3.2222 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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。