CAS NO: | 2098466-94-3 |
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 |
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 |
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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 |
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溶解性数据 | In Vitro: DMSO : ≥ 25 mg/mL(80.55 mM) *"≥" means soluble, but saturation unknown. 配制储备液
* 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。 |