2. Cell Cycle/DNA Damage Cytoskeleton Epigenetics Apoptosis
  3. Microtubule/Tubulin PARP Apoptosis DNA/RNA Synthesis
  4. Tubulin/PARP1-IN-1

Tubulin/PARP1-IN-1 is a dual inhibitor of tubulin and PARP1, with IC50 values of 1.86 μM and 0.88 μM, respectively. Tubulin/PARP1-IN-1 arrests cancer cells at the G2/M phase, induces cancer cell apoptosis, enhances cellular DNA damage, inhibits tumor angiogenesis, reduces cancer cell colonization and dissemination, and exhibits antiproliferative activity against colorectal cancer cells. Tubulin/PARP1-IN-1 can be used in the research of colorectal cancer and colorectal cancer lung metastasis.

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

Tubulin/PARP1-IN-1

Tubulin/PARP1-IN-1 Chemical Structure

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Tubulin/PARP1-IN-1 Related Antibodies

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PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

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RNASE L DNA Polymerases RNA Polymerases Helicases DNA Ligase

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Description

Tubulin/PARP1-IN-1 is a dual inhibitor of tubulin and PARP1, with IC50 values of 1.86 μM and 0.88 μM, respectively. Tubulin/PARP1-IN-1 arrests cancer cells at the G2/M phase, induces cancer cell apoptosis, enhances cellular DNA damage, inhibits tumor angiogenesis, reduces cancer cell colonization and dissemination, and exhibits antiproliferative activity against colorectal cancer cells. Tubulin/PARP1-IN-1 can be used in the research of colorectal cancer and colorectal cancer lung metastasis[1].

IC50 & Target[1]

PARP-1

0.88 μM (IC50)

In Vitro

Tubulin/PARP1-IN-1 (Compound C2R) (72 h) exhibits inhibitory activity against HT-29, MCF-7, A549, PC-3, and MDA-MB-231, with an IC50 of 44 nM against HT-29[1].
Tubulin/PARP1-IN-1 (20-80 nM; 14 d) inhibits the number and size of HT-29 cell colonies in a dose-dependent manner[1].
Tubulin/PARP1-IN-1 (20-80 nM; 24 h) arrests HT-29 cells at the G2/M phase and induces apoptosis[1].
Tubulin/PARP1-IN-1 (40-80 nM; 24 h) reduces mitochondrial membrane potential and increases ROS levels in a dose-dependent manner in HT-29 cells[1].
Tubulin/PARP1-IN-1 (40-80 nM; 8 h) disrupts the microtubule network in HT-29 cells[1].
Tubulin/PARP1-IN-1 (20-40 nM; 24 h) significantly inhibits the invasion/migration capacity of A549 cells[1].
Tubulin/PARP1-IN-1 (20-40 nM; 24 h) reverses the epithelial-mesenchymal transition (EMT) phenotype of A549 cells[1].
Tubulin/PARP1-IN-1 (20-80 nM; 6 h) inhibits capillary-like tube formation in human umbilical vein endothelial cells (HUVECs) in a dose-dependent manner[1].

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

Tubulin/PARP1-IN-1 Related Antibodies

Apoptosis Analysis[1]

Cell Line: HT-29 cells
Concentration: 20, 40, 80 nM
Incubation Time: 24 h
Result: Dose-dependently induced apoptosis in HT-29 cells, with the highest tested concentration increasing the apoptotic proportion to 25.4%.

Cell Cycle Analysis[1]

Cell Line: HT-29 cells
Concentration: 20, 40, 80 nM
Incubation Time: 24 h
Result: Inducted of G2/M (M phase) blockade.

Cell Migration Assay [1]

Cell Line: A549 cells
Concentration: 20, 40 nM
Incubation Time: 24 h
Result: Inhibited cell migration.

Cell Invasion Assay[1]

Cell Line: A549 cells
Concentration: 20, 40 nM
Incubation Time: 24 h
Result: Inhibited cell invasion,

Western Blot Analysis[1]

Cell Line: HT-29 and A549 cells
Concentration: 40, 80 nM
Incubation Time: 24 h
Result: Increased Bax, Bim, Cleaved Caspase-3 and Cleaved PARP and dereased Bcl-2 in HT-29 cells.
Increased E-cadherin, decreased Vimentin and ZEB1 in A549 cells.
Parmacokinetics
Species Dose Route C0 AUC0-t AUC0-∞ T1/2 Vd/F CL/F MRT0-∞
Rat[1] 5 mg/kg i.v. 55763.18 ng/mL 3080.51 ng·h/mL 3085.78 ng·h/mL 1.76 h 4.16 L/kg 1.63 L/h/kg 0.47 h
In Vivo

Tubulin/PARP1-IN-1 (Compound C2R) (5-20 mg/kg; i.v.; once every 3 days; administered for 28 days) exerts potent in vivo anti-tumor activity against HT-29 colorectal cancer xenograft mice by inhibiting tumor cell proliferation, blocking angiogenesis and inducing DNA damage[1].
Tubulin/PARP1-IN-1 (10-20 mg/kg; i.v.; once every 3 days; administered for 14 days) potently inhibits hematogenous lung metastasis of colorectal cancer in BALB/c mice, reduces metastatic burden and alleviates pathological damage of lung tissue[1].

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

Animal Model: BALB/c nude mice (half male and half female, 4 weeks old)
[1]
Dosage: 5 mg/kg; 10 mg/kg; 20 mg/kg
Administration: i.v.; once every 3 days; administered for 28 days
Result: Achieved a tumor inhibition rate of 76.55% at 20 mg/kg, with significant reductions in tumor volume and weight compared to controls.
Decreased expression of proliferation marker Ki67, reduced vascular endothelial marker CD31, and upregulated DNA damage marker γ-H2AX in tumor tissues.
Showed no significant body weight loss, no obvious pathological abnormalities in major organs (heart, liver, spleen, lung, kidney), and blood biochemical indicators (ALT, AST, CR, BUN, CK, LDH) remained within normal ranges.
Animal Model: BALB/c mice (female, 4 weeks old)[1]
Dosage: 10 mg/kg; 20 mg/kg
Administration: i.v.; once every 3 days; administered for 14 days
Result: Significantly reduced the lung metastasis burden and the number of nodules, and inhibits hematogenous lung metastasis of colorectal cancer.
Molecular Weight

696.34

Formula

C30H24Br2N4O6
SMILES

O=C(C1=C2C(N(C)C(CN3C(COC4=O)=C4[C@H](C5=CC(Br)=C(OC)C(Br)=C5)C6=C3C=C7C(OCCO7)=C6)=N2)=CC=C1)N
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Tubulin/PARP1-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:

Tubulin/PARP1-IN-1Microtubule/TubulinPARPApoptosisDNA/RNA Synthesispoly ADP ribose polymerase PARP1colchicine-binding siteHT-29 cellstubulinubiquitin-proteasome pathwayBALB/c micecolorectal cancer cellsG2/M phaselung metastasis of colorectal cancercolorectal cancer xenograftsInhibitorinhibitorinhibit

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