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IWP-2
IWP-2 是 Wnt 加工和分泌的抑制劑，其 IC50 為 27 nM。IWP-2 靶向膜結(jié)合的 O-?；D(zhuǎn)移酶 porcupine (Porcn)，從而阻止關(guān)鍵的 Wnt 配體棕櫚糖基化。IWP-2 還是一種具有 ATP 競爭能力的 CK1δ 抑制劑，對于 M82FCK1δ 的 IC50 為 40 nM。
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 M82FCK1δ[1][2].
IC50 & Target
CK1δ
40 nM (IC50)
體外研究(In Vitro)
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[2].
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[2].
體內(nèi)研究(In Vivo)
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[2].
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[2].
體內(nèi)研究(In Vivo)
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[3].
分子量：466.60
性狀：Solid
Formula：C22H18N4O2S3
CAS 號：686770-61-6
運輸條件：Room temperature in continental US; may vary elsewhere.
儲存方式
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
溶解性數(shù)據(jù)
In Vitro:
DMF : 12.5 mg/mL (26.79 mM; ultrasonic and warming and heat to 60°C)
DMSO : 2 mg/mL (4.29 mM; Need ultrasonic)
| 濃度溶劑體積質(zhì)量 | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.1432 mL | 10.7158 mL | 21.4316 mL |
| 5 mM | 0.4286 mL | 2.1432 mL | 4.2863 mL |
| 10 mM | 0.2143 mL | 1.0716 mL | 2.1432 mL |
請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 儲存時，請在 6 個月內(nèi)使用，-20°C 儲存時，請在 1 個月內(nèi)使用。
參考文獻
[1]. Chen B, et al. Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. Nat Chem Biol. 2009 Feb;5(2):100-7. [Content Brief]
[2]. García-Reyes B, et al. Discovery of Inhibitor of Wnt Production 2 (IWP-2) and Related Compounds As Selective ATP-Competitive Inhibitors of Casein Kinase 1 (CK1) δ/ε. J Med Chem. 2018 May 10;61(9):4087-4102. [Content Brief]
[3]. Maiti G, et al. The Wingless homolog Wnt5a stimulates phagocytosis but not bacterial killing. Proc Natl Acad Sci U S A. 2012 Oct 9;109(41):16600-5. [Content Brief]
IWP-2
IWP-2 是 Wnt 加工和分泌的抑制劑，其 IC50 為 27 nM。IWP-2 靶向膜結(jié)合的 O-酰基轉(zhuǎn)移酶 porcupine (Porcn)，從而阻止關(guān)鍵的 Wnt 配體棕櫚糖基化。IWP-2 還是一種具有 ATP 競爭能力的 CK1δ 抑制劑，對于 M82FCK1δ 的 IC50 為 40 nM。
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 M82FCK1δ[1][2].
IC50 & Target
CK1δ
40 nM (IC50)
體外研究(In Vitro)
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[2].
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[2].
體內(nèi)研究(In Vivo)
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[2].
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[2].
體內(nèi)研究(In Vivo)
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[3].
分子量：466.60
性狀：Solid
Formula：C22H18N4O2S3
CAS 號：686770-61-6
運輸條件：Room temperature in continental US; may vary elsewhere.
儲存方式
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
溶解性數(shù)據(jù)
In Vitro:
DMF : 12.5 mg/mL (26.79 mM; ultrasonic and warming and heat to 60°C)
DMSO : 2 mg/mL (4.29 mM; Need ultrasonic)
| 濃度溶劑體積質(zhì)量 | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.1432 mL | 10.7158 mL | 21.4316 mL |
| 5 mM | 0.4286 mL | 2.1432 mL | 4.2863 mL |
| 10 mM | 0.2143 mL | 1.0716 mL | 2.1432 mL |
請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 儲存時，請在 6 個月內(nèi)使用，-20°C 儲存時，請在 1 個月內(nèi)使用。
參考文獻
[1]. Chen B, et al. Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. Nat Chem Biol. 2009 Feb;5(2):100-7. [Content Brief]
[2]. García-Reyes B, et al. Discovery of Inhibitor of Wnt Production 2 (IWP-2) and Related Compounds As Selective ATP-Competitive Inhibitors of Casein Kinase 1 (CK1) δ/ε. J Med Chem. 2018 May 10;61(9):4087-4102. [Content Brief]
[3]. Maiti G, et al. The Wingless homolog Wnt5a stimulates phagocytosis but not bacterial killing. Proc Natl Acad Sci U S A. 2012 Oct 9;109(41):16600-5. [Content Brief]
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