2. Cell Cycle/DNA Damage Stem Cell/Wnt TGF-beta/Smad Apoptosis
  3. HOXA TGF-beta/Smad Apoptosis
  4. HOXA1-IN-1

HOXA1-IN-1 是一种 HOXA1 抑制剂。HOXA1-IN-1 可下调 HOXA1 蛋白水平、抑制其转录活性并改变其下游靶基因的表达。HOXA1-IN-1 可诱导癌细胞发生 DNA 损伤和凋亡 (apoptosis)。HOXA1-IN-1 在结直肠癌和三阴性乳腺癌异种移植模型中展现出显著的抗肿瘤功效。HOXA1-IN-1 与 Cisplatin (HY-17394) 联用具有协同活性。HOXA1-IN-1 可用于结直肠癌和三阴性乳腺癌的研究。

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HOXA1-IN-1

HOXA1-IN-1 Chemical Structure

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HOXA1-IN-1 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HOXA1-IN-1 is a HOXA1 inhibitor. HOXA1-IN-1 downregulates HOXA1 protein levels, suppresses its transcriptional activity, and alters the expression of its downstream target genes. HOXA1-IN-1 induces DNA damage and apoptosis in cancer cells. HOXA1-IN-1 exhibits antitumor efficacy in xenograft models of colorectal cancer and triple-negative breast cancer. HOXA1-IN-1 shows synergistic activity in combination with Cisplatin (HY-17394). HOXA1-IN-1 can be used for the research of colorectal cancer and triple-negative breast cancer[1].

体外研究
(In Vitro)

HOXA1-IN-1 (F2-15) 可在完整细胞中直接结合 HOXA1 蛋白[1]。
HOXA1-IN-1 (48 h) 可强效抑制 MCF-7、HCT116 和 HepG2 癌细胞的活力，其 IC50 值分别为 5.23 μM、24.27 μM 和 14.18 μM[1]。
HOXA1-IN-1 (10 μM; 24 h) 可通过 HOXA1 依赖的方式抑制 DNA 合成与细胞增殖，降低野生型 MCF-7、HCT116、HepG2、MDA-MB-231 和 HCT116 细胞中 EdU 阳性细胞的比例，但对 HOXA1 敲低细胞无作用[1]。
HOXA1-IN-1 (10 μM; 24 h) 可诱导 MCF-7、HCT116 和 HepG2 癌细胞发生 DNA 损伤和凋亡[1]。
HOXA1-IN-1 (10 μM; 24 h) 不会改变 HOXA1 mRNA 水平，但可在 MCF-7、HCT116 和 HepG2 细胞中抑制 HOXA1 下游靶基因 SMAD3、KHDRBS1、SHC1 和 SFXN3 的表达[1]。
HOXA1-IN-1 (10 μM; 24 h) 可下调 MCF-7、HCT116 和 HepG2 癌细胞中 HOXA1 蛋白的表达[1]。
HOXA1-IN-1 (给药 4 天) 与 Cisplatin (HY-17394) 在 HCT116 和 MDA-MB-231 癌细胞中表现出强烈的协同抗增殖活性[1]。

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

HOXA1-IN-1 相关抗体:

Cell Proliferation Assay[1]

Cell Line: MCF-7, HCT116, HepG2, MDA-MB-231, HOXA1-knockdown MDA-MB-231, HOXA1-knockdown HCT116 cell lines
Concentration: 10 μM
Incubation Time: 24 h
Result: Reduced the fraction of EdU-positive cells by 60-80% in MCF-7, HCT116, HepG2, and wild-type MDA-MB-231 and HCT116 cells.
Did not significantly reduce EdU-positive cell fractions in HOXA1-knockdown MDA-MB-231 and HCT116 cells.

Apoptosis Analysis[1]

Cell Line: MCF-7, HCT116, HepG2 cell lines
Concentration: 10 μM
Incubation Time: 24 h
Result: Significantly increased the percentage of TUNEL-positive cells in all three cell lines: MCF-7, HCT116, and HepG2, with TUNEL-positive fractions increasing from < 5% in controls to ~10-20% in treated cells.

Real Time qPCR[1]

Cell Line: MCF-7, HCT116, HepG2 cell lines
Concentration: 10 μM
Incubation Time: 24 h
Result: Had no significant effect on HOXA1 mRNA levels in any of the three cell lines.
Significantly downregulated the mRNA expression of HOXA1 target genes SMAD3, KHDRBS1, SHC1, and SFXN3 in all three cell lines.

Western Blot Analysis[1]

Cell Line: MCF-7, HCT116, HepG2 cell lines
Concentration: 10 μM
Incubation Time: 24 h
Result: Significantly reduced HOXA1 protein levels in MCF-7, HCT116, and HepG2 cells, with visible decreases in HOXA1 band intensity relative to TUBLIN loading control.
体内研究
(In Vivo)

HOXA1-IN-1 (F2-15) (20 mg/kg；腹腔注射；每日 1 次；连续 14 天) 可通过降低肿瘤细胞增殖能力并促进细胞凋亡，显著抑制荷结直肠癌 PDX 模型的雌性 nu/nu 小鼠及荷三阴性乳腺癌 PDX 模型的雌性 nu/nu 小鼠的肿瘤生长[1]。
HOXA1-IN-1 (20 mg/kg；腹腔注射；每日 1 次；连续 14 天) 与 Cisplatin (HY-17394) 联用，对荷结直肠癌 PDX 的雌性 nu/nu 小鼠和荷三阴性乳腺癌 PDX 的雌性 nu/nu 小鼠具有协同抗肿瘤作用，其肿瘤生长抑制效果优于任一单药[1]。

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

Animal Model: female nu/nu mice (6-week-old, subcutaneously transplanted xenografts)[1]
Dosage: 20 mg/kg
Administration: i.p.; once daily; 14 days
Result: Reduced tumor weights compared to vehicle control, with levels comparable to cisplatin.
Reduced tumor volume growth over time compared to vehicle control.
Reduced HOXA1 and Ki67 (proliferation marker) expression in tumor tissue compared to vehicle control.
Increased caspase-3 staining (apoptosis marker) in tumor tissue compared to vehicle control.
Animal Model: female nu/nu mice (6-week-old, subcutaneously transplanted xenografts)[1]
Dosage: 20 mg/kg
Administration: i.p.; once daily; 14 days
Result: Reduced tumor weights compared to vehicle control, with levels comparable to cisplatin.
Reduced tumor volume growth over time compared to vehicle control.
Reduced HOXA1 and Ki67 (proliferation marker) expression in tumor tissue compared to vehicle control.
Increased caspase-3 staining (apoptosis marker) in tumor tissue compared to vehicle control.
分子量

353.50

Formula

C23H31NO2
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

HOXA1-IN-1 相关分类

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  • 稀释计算器

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  • 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:

HOXA1-IN-1HOXATGF-beta/SmadApoptosisHomeobox ATransforming growth factor betaHOXA1HCT116DNA damageHepG2apoptosiscolorectal cancerpatient-derived xenograft modelsMCF-7MDA-MB-231triple-negative breast cancerInhibitorinhibitorinhibit

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