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

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.

For research use only. We do not sell to patients.

HOXA1-IN-1

HOXA1-IN-1 Chemical Structure

CAS No. : 3118854-61-5

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HOXA1-IN-1 Related Antibodies

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Description

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].

In Vitro

HOXA1-IN-1 (F2-15) directly binds to HOXA1 protein in intact cells[1].
HOXA1-IN-1 (48 h) potently inhibits the viability of MCF-7, HCT116, and HepG2 cancer cells with IC50 values of 5.23 μM, 24.27 μM, and 14.18 μM, respectively[1].
HOXA1-IN-1 (10 μM; 24 h) inhibits DNA synthesis and cell proliferation in an HOXA1-dependent manner, reducing EdU-positive cell fractions in wild-type MCF-7, HCT116, HepG2, MDA-MB-231, and HCT116 cells, but having no effect in HOXA1-knockdown cells[1].
HOXA1-IN-1 (10 μM; 24 h) induces DNA damage and apoptosis in MCF-7, HCT116, and HepG2 cancer cells[1].
HOXA1-IN-1 (10 μM; 24 h) does not alter HOXA1 mRNA levels but suppresses the expression of HOXA1 downstream target genes SMAD3, KHDRBS1, SHC1, and SFXN3 in MCF-7, HCT116, and HepG2 cells[1].
HOXA1-IN-1 (10 μM; 24 h) downregulates HOXA1 protein expression in MCF-7, HCT116, and HepG2 cancer cells[1].
HOXA1-IN-1 (4 days) exhibits strong synergistic antiproliferative activity with Cisplatin (HY-17394) in HCT116 and MDA-MB-231 cancer cells[1].

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

HOXA1-IN-1 Related Antibodies

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.
In Vivo

HOXA1-IN-1 (F2-15) (20 mg/kg; i.p.; once daily; 14 days) significantly inhibits tumor growth in female nu/nu mice bearing colorectal cancer PDXs and female nu/nu mice bearing triple-negative breast cancer PDXs by reducing tumor cell proliferation and increasing apoptosis[1].
HOXA1-IN-1 (20 mg/kg; i.p.; once daily; 14 days) in combination with Cisplatin (HY-17394) produces a synergistic antitumor effect in female nu/nu mice bearing colorectal cancer PDXs and female nu/nu mice bearing triple-negative breast cancer PDXs, resulting in greater tumor growth inhibition than either agent alone[1].

MedChemExpress (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.
Molecular Weight

353.50

Formula

C23H31NO2
CAS No.
SMILES

CC1=CC(C)=CC=C1NC(C2=C(O)C=CC(C(C)(C)CC(C)(C)C)=C2)=O
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Storage

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Purity & Documentation
References
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HOXA1-IN-1 Related Classifications

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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:

HOXA1-IN-13118854-61-5HOXATGF-beta/SmadApoptosisHomeobox ATransforming growth factor betaHOXA1HCT116DNA damageHepG2apoptosiscolorectal cancerpatient-derived xenograft modelsMCF-7MDA-MB-231triple-negative breast cancerInhibitorinhibitorinhibit

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