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抑制剂/激活剂

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凋亡与自噬

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IWP-2

IWP-2 是 Wnt 加工和分泌的抑制剂，其 IC50 为 27 nM。IWP-2 靶向膜结合的 O-酰基转移酶 porcupine (Porcn)，从而阻止关键的 Wnt 配体棕榈糖基化。IWP-2 还是一种具有 ATP 竞争能力的 CK1δ 抑制剂，对于 M82FCK1δ 的 IC50 为 40 nM。

货号：
TK0278
规格：

1mg

5mg

10mg
价格：
￥0.00

产品参数

CAS No.	686770-61-6
生物活性	IWP-2 is an inhibitor of Wnt processing and secretion with an IC50 of 27 nM. IWP-2 targets the membrane-bound O-acyltransferase porcupine (Porcn) and thus preventing a crucial Wnt ligand palmitoylation. IWP-2 is also an ATP-competitive CK1δ inhibitor with an IC50 of 40 nM for the gatekeeper mutant CK1δ.
分子式	C22H18N4O2S3
分子量	466.6
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	Powder -20°C 3 years
溶解性数据	DMSO : 2 mg/mL (4.29 mM; Need ultrasonic)
体内研究	To evaluate the efficacy of IWP-2 in vivo, 200 μL each of IWP-2-liposome or free liposome i separately injected into C57BL/6 mice intraperitoneally about 2 h before injection of a similar volume of either blue-dye-filled latex beads or E. coli DH5α. IWP-2 causes significant reduction in the uptake of blue beads as well as E. coli as assessed by CFUs in peritoneal lavage cells within 2 h. In addition, the levels of TNF-α and IL-6 in the lavage fluid of the corresponding mice are reduced by 2-4-fold compared with control values. Interestingly, IWP-2 even induces a considerable increase in secretion of the anti-inflammatory cytokine IL-10.
体外研究	IWP-2 inhibits the proliferation of the investigated cell lines within the single digit μM range. IWP-2 inhibits cell proliferation in A818-6, MiaPaCa2, Panc-1, Panc-89, HT29, HEK293, SW620 and Capan cell with EC50s of 8.96 μM, 1.90 μM, 2.33 μM, 3.86 μM, 4.67 μM, 2.76 μM, 1.90 μM and 2.05 μM, respectively. Panc-1 cells are either untreated or treated with 2.33 μM IWP-2 for 48 h. In IWP-2 treated cells, the CK1δ kinase peak activity is reduced to approximately 66% residual activity compared to the activity in untreated cells, respectively. IWP-2 reduces the activity of CK1δ in Panc1 cells.
文献	•Adv Mater. 2021 Oct 10;e2104829. •Dev Cell. 2020 Dec 21;55(6):679-694.e11. •Stem Cells Transl Med. 2021 May;10(5):743-755. •J Cell Physiol. 2020 Jul;235(7-8):5811-5822. •Biochem Pharmacol. 2019 Nov;169:113608. •ACS Comb Sci. 2019 Dec 9;21(12):805-816. •Exp Ther Med. 2020 Mar;19(3):1701-1710. •Patent. US20180263995A1.
纯度及产品资料	98%

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