1. Autophagy
  2. Autophagy
  3. PHY34

PHY34 一种抑制 ATP6V0A2CAS 进而抑制自噬 (autophagy) 的抑制剂,并具有纳摩尔效应。 PHY34通过诱导凋亡 (apoptosis) 抑制癌细胞生长并抑制荷瘤模型中肿瘤生长。PHY34 用于高级别浆液卵巢癌的研究。

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PHY34 Chemical Structure

PHY34 Chemical Structure

CAS No. : 2130033-55-3

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PHY34 is an inhibitor that inhibits ATP6V0A2 and CAS thereby inhibiting autophagy, and has a nanomolar effect. PHY34 inhibits cancer cell growth by inducing apoptosis and inhibits tumor growth in xenograft models. PHY34 can be used for research on high grade serous ovarian cancer[1][2].

IC50 & Target

ATP6V0A2, cellular apoptosis susceptibility (CAS)[2]

体外研究
(In Vitro)

PHY34 (0.001 nM-50 μM, 72 h) 通过激活基于增强 cPARP 水平的凋亡,以纳摩尔效应抑制多种癌细胞生长,并在 HGSOC 细胞系中具有最佳效果[1]
PHY34 (100 nM, 1 μM; 24 h) 分别在 100 nM 和1 μM 阻断 OVCAR8 和 OVCAR3 中自溶酶体的分解[1]
PHY34 (10 nM, 24 h) 在 OVCAR8 中抑制晚期自噬先于诱导细胞凋亡[1]
PHY34 (100 nM, 48 h) 在 OVCAR3 中抑制晚期自噬先于诱导细胞凋亡[1]
PHY34 (0.01 nM-2 μM,72 h) 在 H4 细胞中存在野生型 V0A2 而不是 V823I 突变体的情况下诱导细胞死亡[2]
PHY34 (10,100nM;48 h,72 h) 改变核内多种蛋白的亚细胞定位[2]
PHY34 (20 μM,1 h) 与 ATP6V0A2 亚基特异性结合[2]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1][2]

Cell Line: OVCAR8, OVCAR3, HT-29, MDA-MB-435, MDA-MB-231, IOSE80, FT33
Concentration: 0.001 nM-50 μM
Incubation Time: 72 h
Result: Inhibited the growth of various cancer cells with IC50 values of 4 nM(OVCAR8, OVCAR3), 43.3 nM(HT-29) , 23 nM(MDA-MB-435) , 5.2 nM(MDA-MB-231).
Exhibited no toxicity to IOSE80 and FT33 (IC50 >50 μM).

Cell Viability Assay[2]

Cell Line: H4
Concentration: 0.01 nM-2 μM
Incubation Time: 72 h
Result: Inhibited mutant cell with an IC50 value of 246 pM that was 1000-fold more potent than HTP-013(434 nM).
Conferred resistance in V8231 mutation and no impact activity in T216A mutation.

Apoptosis Analysis[1]

Cell Line: OVCAR8, OVCAR3
Concentration: 10 nM, 100 nM
Incubation Time: 72 h
Result: Increased the number of cells in early and late apoptosis in OVCAR8 and OVCAR3 at 10 nM and 100 nM, respectively.

Cell Autophagy Assay[1]

Cell Line: Hela
Concentration: 9.31 fM-20 μM
Incubation Time: 4 h
Result: Sustained high levels of LC3B puncta with an EC50 value of 2 nM.
Inhibited autophagy with an EC50 value of 3.9 nM.

Cell Autophagy Assay[2]

Cell Line: OVCAR3
Concentration: 5 nM
Incubation Time: 4 h
Result: Inhibited autophagy with an ED50 value of 6.29 nM, and was more potent than bafilomycin A1 (HY-100558) with an ED50 value of 29.1 nM.

Western Blot Analysis[1][2]

Cell Line: OVCAR8, OVCAR3, OVCAR4
Concentration: 10 nM, 100 nM
Incubation Time: 48 h, 72 h
Result: Increased cPARP levels in OVCAR8 after 48 h at 10 nM, in OVCAR4 and OVCAR3 after 72 h at 100 nM, respectively.
Reversed the conversion of PARP to cPARP combined with RAP (HY-10219) of 1 μM.

Western Blot Analysis[2]

Cell Line: OVCAR8, OVCAR3, OVCAR4
Concentration: 10 nM
Incubation Time: 24 h, 48 h, 72 h
Result: Promoted histone H3, LAMP1/2, ACSS2, and PCNA nuclear protein accumulation at 48 h.
Reduced expression of KPNA2 (Karyopherin subunit alpha 2) with time-dependent manner.
Increased nuclear accumulation of mutant p53 at 48 h.
体内研究
(In Vivo)

PHY34 (0.75 mg/kg, i.p., 每周三次, 3 周) 在OVCAR8构建的雌性裸鼠荷瘤模型中显著抑制肿瘤生长并降低肿瘤组织中 Ki67 表达[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: OVCAR8-induced xenograft models in female nude mice[1].
Dosage: 0.75 mg/kg, three times a week for three weeks
Administration: Intraperitoneal injection (i.p.)
Result: Decreased tumor burden based on average abdominal radiant efficiency with no gross toxicity through analysis of fluorescence imaging.
分子量

582.55

Formula

C30H30O12

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献

PHY34 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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PHY34
目录号:
HY-122650
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