WS6

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Chemical Structure| 1421227-53-3 同义名 : -
CAS号 : 1421227-53-3
货号 : A129008
分子式 : C29H31F3N6O3
纯度 : 99%+
分子量 : 568.59
MDL号 : MFCD26793882
存储条件：

Pure form Sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(184.67 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
描述 WS6 is a novel small molecule that promotes β cell proliferation in rodent and human primary islets with EC50 of 0.28 uM(R7T1 cell viability). EC50 value: 0.28 uM. RIP-DTA mice were fed Dox in the drinking water until the onset of overt diabetes (blood glucose reading >300 mg/dL, typically 4-10 days), at which point Dox treatment was discontinued and treatment with WS6 was initiated (5 mg/kg every other day via intraperitoneal injection). Pharmacokinetic studies with WS6 at 50 mg/kg revealed a CMAX of ～5 μM and T1/2 of ～2 h. Treatment with WS6 caused a progressive reduction of blood glucose over time, starting around 2 weeks[3]. Enhancement of human β-cell proliferation is one potential approach to restore β-cell mass to prevent and/or cure type 1 and type 2 diabetes. WS6, an IkB kinase and EBP1 inhibitor, can promote effective human β-cell proliferation[4]. WS6 did not change the proportion of insulin-positive beta cells or the expression of beta cell-specific transcription factors, suggesting that WS6 does not alter beta cell differentiation, and WS6 had no effect on human islet cell apoptosis or viability[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.76mL

0.35mL

0.18mL

8.79mL

1.76mL

0.88mL

17.59mL

3.52mL

1.76mL
参考文献

[1]Boerner BP, George NM, et al. WS6 induces both alpha and beta cell proliferation without affecting differentiation or viability. Endocr J. 2015;62(4):379-86.

[2]Shen W, Tremblay MS, et al. Small-molecule inducer of βcell proliferation identified by high-throughput screening. J Am Chem Soc. 2013 Feb 6;135(5):1669-72.

[3]Shen W, Tremblay MS, Deshmukh VA, Wang W, Filippi CM, Harb G, Zhang YQ, Kamireddy A, Baaten JE, Jin Q, Wu T, Swoboda JG, Cho CY, Li J, Laffitte BA, McNamara P, Glynne R, Wu X, Herman AE, Schultz PG. Small-molecule inducer of β cell proliferation identified by high-throughput screening. J Am Chem Soc. 2013 Feb 6;135(5):1669-72

[4]Shirakawa J, Kulkarni RN. Novel factors modulating human β-cell proliferation. Diabetes Obes Metab. 2016 Sep;18 Suppl 1(Suppl 1):71-7

[5]Boerner BP, George NM, Mir SU, Sarvetnick NE. WS6 induces both alpha and beta cell proliferation without affecting differentiation or viability. Endocr J. 2015;62(4):379-86