2. Metabolic Enzyme/Protease Apoptosis
  3. Aldehyde Dehydrogenase (ALDH) Mitochondrial Metabolism Necroptosis
  4. ALDH1A inhibitor 673A

ALDH1A inhibitor 673A  (Synonyms: ALDH1Ai 673A)

目录号: HY-122912 纯度: 99.15%
COA 产品使用指南 技术支持

ALDH1A inhibitor 673A 是一种 ALDH1A 抑制剂，对 ALDH1A1、ALDH1A2 和 ALDH1A3 的 IC50 值分别为 246 nM、230 nM 和 348 nM。ALDH1A inhibitor 673A 对其他 ALDH 家族成员几乎没有或没有抑制作用。ALDH1A inhibitor 673A 可诱导卵巢癌干细胞样细胞 (CSCs) 的坏死性凋亡 (necroptosis)。ALDH1A inhibitor 673A 在癌细胞中诱导 DNA 双链断裂。ALDH1A 抑制剂 673A 可用于卵巢癌研究。

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ALDH1A inhibitor 673A

ALDH1A inhibitor 673A Chemical Structure

CAS No. : 109437-62-9

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥572
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5 mg ￥520
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10 mg ￥784
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25 mg ￥1568
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50 mg ￥2352
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100 mg ￥3520
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ALDH1A inhibitor 673A 相关抗体

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查看 Aldehyde Dehydrogenase (ALDH) 亚型特异性产品:

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ALDH1 ALDH2 ALDH3

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ALDH1A inhibitor 673A is an ALDH1A inhibitor with IC50s of 246 nM (ALDH1A1), 230 nM (ALDH1A2), 348 nM (ALDH1A3), respectively. ALDH1A inhibitor 673A has little or no inhibitory effect on other ALDH family members. ALDH1A inhibitor 673A induces necroptotic ovarian cancer stem-like cells (CSCs) death. ALDH1A inhibitor 673A induces DNA double stand breaks in cancer cells. ALDH1A inhibitor 673A can be used for the study of ovarian cancer[1][2][3].

体外研究
(In Vitro)

ALDH1A inhibitor 673A (0.0001-0.1 μM) 在 BRCA 突变型 PEO1/PEO4 细胞中诱导细胞死亡[1]。
ALDH1A inhibitor 673A (12 μM, 6 周) 降低 BPRN-FTE 类器官的肿瘤起始能力[1]。
ALDH1A inhibitor 673A (0.6-10 μM, 12 h) 导致毒性醛类物质积累，从而在 OVCAR5 和 OVCAR4 细胞中引发 DNA 损伤和细胞毒性[2]。
ALDH1A inhibitor 673A (1-2 μM, 96 h) 诱导 OVCAR5 和 OVCAR4 细胞死亡，该作用可被外源性醛类加剧，并被醛类清除剂缓解[2]。
\ ALDH1A inhibitor 673A (10-20 μM) 抑制 ALDH1A1 (IC50 = 246 nM)、ALDH1A2 (IC50 = 230 nM) 和 ALDH1A3 (IC50 = 348 nM)，对 ALDH2 (IC50 = 14 μM) 或其他众多 ALDH 家族成员的抑制作用极小或无抑制作用[3]。
ALDH1A inhibitor 673A (12.5 μM, 72 h) 在所有三个细胞系 (A2780、Ovsaho 和 OVCAR5) 中耗竭 CD133+ 癌干细胞 (CSCs)，其 CSC 选择性中位毒性剂量 (TD50) 为 3-20 μM[3]。
ALDH1A inhibitor 673A (2.5-12.5 μM, 72 h) 在 A2780 细胞中诱导非凋亡、半胱天冬酶独立的细胞死亡[3]。
ALDH1A inhibitor 673A (12.5 μM, 1.5-24 h) 在 A2780 细胞中诱导钙依赖的坏死性凋亡[3]。 ALDH1A inhibitor 673A (12.5 μM, 36-72 h) 在 PEO4 细胞中诱导线粒体解偶联蛋白的表达[3]。
ALDH1A inhibitor 673A (12.5 μM, 1.5-24 h) 处理导致原代高级别浆液性卵巢癌 (HGSC) 细胞的氧化磷酸化 (OXPHOS) 能力下降，伴随基础和备用呼吸能力以及 ATP 产生的显著减少[3]。
ALDH1A inhibitor 673A (0.3-30 μM, 0-12 days) 有效耗竭癌干细胞 (CSCs)，与化疗和放疗协同作用，并显著减少多种癌细胞系和原代患者样本中的肿瘤球形成和肿瘤起始能力[3]。

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

ALDH1A inhibitor 673A 相关抗体:

Western Blot Analysis[1]

Cell Line: OVCAR5 and OVCAR4 cells
Concentration: 1, 3, 10 μM
Incubation Time: 12 h
Result: Increased the levels of γ-H2AX, pChk1, pChk2 and pATR.

Cell Viability Assay[1]

Cell Line: OVCAR5 and OVCAR4 cells
Concentration: 1, 2 μM
Incubation Time: 96 h
Result: Increased cell death when combined with 12.5 μM Retinaldehyde or 25 μM 4-Hydroxynonenal (4-HNE) (HY-113466).
Decreased cell death when combined with 10 μM Hydralazine (HY-B0464A) or 100 μM Metformin (HY-B0627).

Apoptosis Analysis[3]

Cell Line: A2780 cells and PEO4 cells
Concentration: 2.5, 5, 12.5 μM
Incubation Time: 48, 72 h
Result: Revealed no significant early or late induction of annexin-V.
Induced cell death which was not inhibited by pretreating cells with the pan-caspase inhibitor Z-VAD-FMK (HY-16658B) or the caspase-3 inhibitor Z-DEVD-FMK (HY-12466).
Induced necroptosis through an ALDH-dependent knockdown of ALDH1A3, causing cell death in PEO4 cells without significantly inducing annexin-V.

Immunofluorescence[3]

Cell Line: A2780 cells
Concentration: 12.5 μM
Incubation Time: 24 h
Result: Demonstrated clear nuclear swelling and loss of nuclear content consistent with necroptosis.
Revealed clear nuclear-to-cytoplasm translocation of the high mobility group-1 protein.

Western Blot Analysis[3]

Cell Line: A2780 cells
Concentration: 12.5 μM
Incubation Time: 1.5, 2, 4, 5, 6, 8, 24 h
Result: Induced dephosphorylation of DRP1 and increased PGAM5 expression with the appearance of the PGAM5-S splice variant.
Increased both in the mitochondrial association of DRP1and in the proportion of MLKL protein localized to the cell membrane fraction.

Real Time qPCR[3]

Cell Line: PEO4 cells
Concentration: 12.5 μM
Incubation Time: 8, 20, 48 h
Result: Increased the expression of the mitochondrial UCPs (UCP1 and UCP3)
体内研究
(In Vivo)

ALDH1A inhibitor 673A (20 mg/kg，腹腔注射，每日一次，5-7 天) 可降低 BPRN 小鼠的 STIC 和癌症发生率[1]。
ALDH1A inhibitor 673A (20 mg/kg，腹腔注射，每周五次，持续 4 周) 在 OVCAR5 细胞异种移植小鼠模型中增强了 ATM/ATR 抑制剂 (AZD1390 (HY-109566)/Ceralasertib (AZD6738) (HY-19323)) 的肿瘤抑制效果[2]。
ALDH1A inhibitor 673A (4-20 mg/kg，腹腔注射，每日一次，持续 3 周) 抑制 Ovsaho、HEY-1 和 A2780 细胞系异种移植小鼠中的肿瘤生长[3]。

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

Animal Model: BPRN (Brca1, Trp53, Rb1, Nf1 inactivated) mouse model[1]
Dosage: 20 mg/kg
Administration: i.p. daily for 5-7 days
Result: Showed no clear toxicity or any overt evidence of malignancy.
Reduced lesions in treated animals.
Animal Model: OVCAR5 cell were subcutaneously implanted bilaterally in the axilla of NSG mice[2]
Dosage: 20 mg/kg combined with 20 mg/kg AZD1390 or 50 mg/kg AZD6738
Administration: i.p. five times a week for 4 weeks
Result: Reduced the tumor volume.
Increased the number of γ-H2AX positive nuclei.
Animal Model: 7.5 × 104 A2780 cells or 15,000 CD133+ (A2780) cells, 5 × 106 OVCAR8, 5 × 105 HEY-1, or 1 × 105 CaOV3 cells were injected, in 100 μl of Matrigel (BD Biosciences), subcutaneously into the axillae of 8-week-old female NSG mice.[3]
Dosage: 4, 20 mg/kg or a combination of Cisplatin (HY-17394) (i.p., 3 times a week)
Administration: i.p. daily for 3 weeks
Result: Prevented tumor growth and induced tumor regression.
Decreased tumor cell Ki67 expression.
Revealed necrotic morphology.
Upregulated the levels of UCP1 and UCP3 in treated tumors.
Reduced the number of ALDH1A1-expressing cells.
Decreased ALDEFLUOR activity in splenocytes of animals.
Demonstrated clear protection of the catalytic residue Cys303 in ALDH1A1, whereas no binding to noncatalytic residues was detected.
Upregulated the activity of ALDH.
分子量

223.27

Formula

C15H13NO
CAS 号
性状

固体

颜色

Off-white to light brown

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 29.17 mg/mL (130.65 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 4.4789 mL 22.3944 mL 44.7888 mL
5 mM 0.8958 mL 4.4789 mL 8.9578 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-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。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
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体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

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体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

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每只动物的给药体积

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由于实验过程有损耗，建议您多配一只动物的量
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工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.15%

COA (283 KB) HNMR (237 KB) LCMS (92 KB)

产品使用指南 (1538 KB)
参考文献

ALDH1A inhibitor 673A 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 4.4789 mL 22.3944 mL 44.7888 mL 111.9720 mL
5 mM 0.8958 mL 4.4789 mL 8.9578 mL 22.3944 mL
10 mM 0.4479 mL 2.2394 mL 4.4789 mL 11.1972 mL
15 mM 0.2986 mL 1.4930 mL 2.9859 mL 7.4648 mL
20 mM 0.2239 mL 1.1197 mL 2.2394 mL 5.5986 mL
25 mM 0.1792 mL 0.8958 mL 1.7916 mL 4.4789 mL
30 mM 0.1493 mL 0.7465 mL 1.4930 mL 3.7324 mL
40 mM 0.1120 mL 0.5599 mL 1.1197 mL 2.7993 mL
50 mM 0.0896 mL 0.4479 mL 0.8958 mL 2.2394 mL
60 mM 0.0746 mL 0.3732 mL 0.7465 mL 1.8662 mL
80 mM 0.0560 mL 0.2799 mL 0.5599 mL 1.3997 mL
100 mM 0.0448 mL 0.2239 mL 0.4479 mL 1.1197 mL
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.

Keywords:

ALDH1A inhibitor 673A109437-62-9ALDH1Ai 673AAldehyde Dehydrogenase (ALDH)Mitochondrial MetabolismNecroptosisALDH1ABPRNovarian cancerInhibitorinhibitorinhibit

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