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Y-320

MCE China：Y-320

Brand：MedChemExpress (MCE)

Cat. No.HY-15898

CAS：288250-47-5

Purity：99.74%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Y-320 is a potent, orally active phenylpyrazoleanilide immunomodulator. Y-320 inhibits IL-17 production by CD4 T cells stimulated with IL-15 with IC50 values of 20 to 60 nM. Y-320 enhances TP53, DMD, and COL17A1 PTC readthrough by G418 and increases cellular protein levels and protein synthesis. Y-320 concomitants use of with a low dose of Paclitaxel (HY-B0015) significantly sensitized multidrug resistance (MDR) tumors by inducing G2/M phase arrest and apoptosis. Y-320 can be used for research of rheumatoid arthritis (RA) and cancer.

In Vitro：Y-320 (0-100 nM; 48 h) inhibits IL-17 production by murine and human CD4 T Cells stimulated with IL-15 with IC50 values of 25.7, 52.4 and 57.4 nM for murine CD4 T cells, murine Th17 cells and human CD4 T cells, respectively[1]. Y-320 (0-100 nM; 48 h) inhibits phosphorylation of JAK1/JAK3 in murine CD4 T cells stimulated with IL-15/CXCL12/anti-CD3 mAb[1]. Y-320 (0.25-2 μM; 48 h) enhances PTC readthrough by G418 in different cell lines[2]. Y-320 (0-2 μM; 48 h; HDQ-P1 cells) 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]. Y-320 (1 μM; 48 h; HDQ-P1 cells) up-regulates CXC chemokine expression including CXCL10, CXCL8, and CXCL2[2]. Y-320 (500 nM; 72 h) reverses the resistance to paclitaxel in MDR cancer cells. Y-320 has the reversal index (RI) combined with Paclitaxel (0-1000 nM) are 5.5 (Bads-200), 9.4 (Bats-72) and 1.7 (Huh7-TS-48)[3]. Y-320 (500 nM; 72 h; Bads-200 cells) enhances Paclitaxel-induced G2/M arrest and enhances Paclitaxel-induced (500 nM) tumor cell apoptosis[3]. Y-320 (0-20 μM; 72 h; Bads-200 cells) is a substrate of P-gp reverses MDR by inhibiting P-gp function[3].

In Vivo：Y-320 (0-3 mg/kg; p.o.; daily, for 42 d) ameliorates collagen-induced arthritis (CIA) in DBA/1J mice with a reduction of IL-17 mRNA in arthritic joints[1]. Y-320 (5 mg/kg; i.v.; every three days, for 18 d; Homozygous nude athymic mice with Bats-72 xenograft) sensitizes MDR xenograft tumor to Paclitaxel in vivo[3].

IC50 & Target：IL-15 IL-17

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References：

[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.  [Content Brief]

[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.  [Content Brief]

[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.  [Content Brief]