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WJ460 Sale

目录号 : GC38203

WJ460是一种有效的myoferlin(MYOF)抑制剂,可直接与MYOF相互作用。

WJ460 Chemical Structure

Cas No.:1415251-36-3

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥1,135.00
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1mg
¥350.00
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5mg
¥1,120.00
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10mg
¥1,890.00
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25mg
¥3,150.00
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50mg
¥5,390.00
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100mg
¥9,100.00
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Sample solution is provided at 25 µL, 10mM.

Description

WJ460 is a potent myoferlin (MYOF) inhibitor, which interacts directly with MYOF[2]. WJ460 blocks breast cancer cell invasion with IC50 values of 43.37±3.42nM in MDA-MB-231[2]. However , WJ460 was inadequate in terms of metabolic stability and water solubility as well as binding activity with MYOF[3].

WJ460 (1μM, 24h) reduced Human T-cell leukemia virus type 1 (HTLV-1 infection) , which was correlated with a reduction in the intracellular level of mature Env[4]. WJ460 (50nM, 15h, 2Gy x-rays) treated HCT116 (cancer cell lines) spheroids were significantly radiosensitized as observed by a reduction in growth at day 15 post-seeding , compared with vehicle cells[5].

WJ460 (10mg/kg; 28 days; intraperitoneal injection) inhibits breast tumor growth, angiogenesis, and spontaneous metastasis in a mouse model[2]. WJ460(10mg/kg; 4weeks; intraperitoneal injection) caused a reduction of the abundance of ferroptosis core regulators solute carrier family 7 member 11 (SLC7A11) and glutathione peroxidase 4 (GPX-4)[1].

THPTA ligand

WJ460 , a myoferlin inhibitor , exerts anti-metastatic activity in breast cancer[2].

References:

[1] RADEMAKER G, BOUMAHD Y, PEIFFER R, et al. Myoferlin targeting triggers mitophagy and primes ferroptosis in pancreatic cancer cells [J]. Redox Biol, 2022, 53(102324.

[2] ZHANG T, LI J, HE Y, et al. A small molecule targeting myoferlin exerts promising anti-tumor effects on breast cancer [J]. Nat Commun, 2018, 9(1): 3726.

[3] GU H, ZHANG T, LI Y, et al. Discovery of 1,5-diaryl-1,2,4-triazole derivatives as myoferlin inhibitors and their antitumor effects in pancreatic cancer [J]. Future Med Chem, 2022, 14(20): 1425-40.

[4] POLAKOWSKI N, SARKER M A K, HOANG K, et al. HBZ upregulates myoferlin expression to facilitate HTLV-1 infection [J]. PLoS Pathog, 2023, 19(2): e1011202.

[5] FOWLER H, CLIFFORD R E, BOWDEN D, et al. Myoferlin: A Potential Marker of Response to Radiation Therapy and Survival in Locally Advanced Rectal Cancer [J]. Int J Radiat Oncol Biol Phys, 2024, 120(4): 1111-23.

WJ460是一种有效的myoferlin(MYOF)抑制剂,可直接与MYOF相互作用[1]。WJ460阻断乳腺癌细胞侵袭,MDA-MB-231的IC50值为43.37±3.42nM[1]。然而,WJ460在代谢稳定性、水溶性以及与MYOF的结合活性方面存在不足[2]

WJ460(1μM,24小时)下调了人类T细胞白血病病毒1型(HTLV-1)的感染,这与细胞内成熟Env水平的降低有关[3]。与对照组相比,用WJ460(50nM,15小时,2居里X射线)处理的HCT116(癌细胞系)球体在接种后第15天的生长明显减少,表明其对放射治疗的敏感性增加[4]

WJ460 (10mg/kg;28天;腹腔注射) 抑制小鼠模型中乳腺肿瘤的生长、血管生成和自发转移[1]。WJ460(10mg/kg ; 4周;腹腔注射)导致铁死亡下调的核心调节因子溶质载体家族7成员11(SLC7A11)和谷胱甘肽过氧化物酶4(GPX-4)丰度降低[5]

WJ460,作为myoferlin抑制剂,在乳腺癌中有抗转移活性[1]

实验参考方法

Cell experiment[1]:

Cell lines

Pancreatic Cancer Cell Line 1 (PANC-1)

Preparation method

PANC-1 cells were maintained in Dulbecco's modified Eagle's medium (DMEM) supplemented with 10% fetal bovine serum (FBS). Cells were cultured in a 37℃, 5% CO2 incubator. Cells were checked monthly for mycoplasma and used between passage 1 and 10. The cells culture were submitted to 50nM WJ460 during 24h.

Reaction Conditions

50nM ; 24h

Applications

WJ460 triggers a cell cycle arrest in G2/M phase and mitophagy

Animal experiment[2]:

Animal models

Female nude mice BALB/c athymic nude mice

Preparation method

For the spontaneous metastasis model , MDA-MB-231- Luciferase cells (1×106) were injected in the #4 mammary fat pad of the mice. Lung metastasis was monitored weekly by an in vivo image system and histological examination.  

Dosage form

10mg/kg ; 28 days ; intraperitoneal injection.

Applications

WJ460 caused significant inhibition of breast cancer pulmonary metastasis.

References:

[1] RADEMAKER G, BOUMAHD Y, PEIFFER R, et al. Myoferlin targeting triggers mitophagy and primes ferroptosis in pancreatic cancer cells [J]. Redox Biol, 2022, 53(102324.

[2] ZHANG T, LI J, HE Y, et al. A small molecule targeting myoferlin exerts promising anti-tumor effects on breast cancer [J]. Nat Commun, 2018, 9(1): 3726.

化学性质

Cas No. 1415251-36-3 SDF
Canonical SMILES O=C(NCCCCC1=CC=CC=C1)C2=CC=CC(C(N3C4=CC=CC=C4OC)SCC3=O)=C2
分子式 C27H28N2O3S 分子量 460.59
溶解度 DMSO: 250 mg/mL (542.78 mM) 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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1 mg 5 mg 10 mg
1 mM 2.1711 mL 10.8556 mL 21.7113 mL
5 mM 0.4342 mL 2.1711 mL 4.3423 mL
10 mM 0.2171 mL 1.0856 mL 2.1711 mL
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