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Y-320 {[allProObj[0].p_purity_real_show]}

货号:A657468 Ambeed 开学季,买赠积分,赢豪礼

Y-320 is a phenylpyrazoleanilide immuno modulator and inhibits IL-17 production by CD4 T cells stimulated with IL-15 with IC50 values of 20 to 60 nM.

Y-320 化学结构 CAS号:288250-47-5
Y-320 化学结构
CAS号:288250-47-5
Y-320 3D分子结构
CAS号:288250-47-5
Y-320 化学结构 CAS号:288250-47-5
Y-320 3D分子结构 CAS号:288250-47-5
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Y-320 纯度/质量文件 产品仅供科研

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Y-320 生物活性

描述 Y-320, a potent phenylpyrazoleanilide immunomodulator, is recognized for its oral activity. It suppresses IL-17 production by CD4 T cells stimulated with IL-15, presenting IC50 values ranging from 20 to 60 nM. This compound also bolsters TP53, DMD, and COL17A1 PTC readthrough alongside G418, elevating both cellular protein levels and protein synthesis. When used with a low dosage of Paclitaxel, Y-320 notably increases the sensitivity of multidrug resistance (MDR) tumors to the drug, triggering G2/M phase arrest and apoptosis. Y-320's applications extend to rheumatoid arthritis (RA) and cancer research[1].[2].
体内研究

In vivo, Y-320 at doses up to 3 mg/kg administered orally daily for 42 days ameliorates collagen-induced arthritis (CIA) in DBA/1J mice, reducing IL-17 mRNA expression in arthritic joints[1].

Furthermore, at a dosage of 5 mg/kg intravenously every three days for 18 days, Y-320 sensitizes MDR xenograft tumors to Paclitaxel in homogenous nude athymic mice bearing Bats-72 xenografts[3].

体外研究

In both murine and human CD4 T cells stimulated with IL-15, Y-320 demonstrates inhibitory effects on IL-17 production, with IC50 values identified as 25.7, 52.4, and 57.4 nM for murine CD4 T cells, murine Th17 cells, and human CD4 T cells, respectively, over a 48-hour period at concentrations up to 100 nM[1]. Otherwise, Y-320 also inhibits phosphorylation of JAK1/JAK3 in murine CD4 T cells stimulated with IL-15/CXCL12/anti-CD3 mAb[1].

At concentrations ranging from 0.25 to 2 μM over 48 hours, Y-320 enhances PTC readthrough in various cell lines and increases cellular protein levels and ribosome biogenesis in a concentration-dependent manner[2].

Y-320 (0-2 μM; 48 h; Tsc2-/- cells) causes a small decrease in phospho-S6K combination with G418 (100 μM)[2].

Additionally, at 1 μM over 48 hours, Y-320 up-regulates the expression of several CXC chemokines, including CXCL10, CXCL8, and CXCL2, in HDQ-P1 cells[2].

Y-320, at a dose of 500 nM for 72 hours, reverses paclitaxel resistance in MDR cancer cells, with reversal indices (RI) when combined with Paclitaxel ranging from 1.7 to 9.4 in different cell lines. It enhances paclitaxel-induced G2/M arrest and apoptosis in Bads-200 cells[3].

Additionally, Y-320 serves as a substrate of P-gp and reverses MDR by inhibiting P-gp function[3].

Y-320 参考文献

[1]Ushio H, et, al. A new phenylpyrazoleanilide, y-320, inhibits interleukin 17 production and ameliorates collagen-induced arthritis in mice and cynomolgus monkeys. Pharmaceuticals (Basel). 2013 Dec 23;7(1):1-17.

[2]Hosseini-Farahabadi S, et, al. Small molecule Y-320 stimulates ribosome biogenesis, protein synthesis, and aminoglycoside-induced premature termination codon readthrough. PLoS Biol. 2021 May 3;19(5):e3001221.

[3]Hong J, et, al. Y-320, a novel immune-modulator, sensitizes multidrug-resistant tumors to chemotherapy. Am J Transl Res. 2020 Feb 15;12(2):551-562.

Y-320 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.98mL

0.40mL

0.20mL

9.90mL

1.98mL

0.99mL

19.80mL

3.96mL

1.98mL

Y-320 技术信息

CAS号288250-47-5
分子式C27H29ClN6O2
分子量 505.011
别名
运输蓝冰
存储条件

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 4 mg/mL(7.92 mM),配合低频超声助溶,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

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