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Cat. No.: HY-187459

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Topoisomerase I-IN-23

Topoisomerase I-IN-23 is a topoisomerase I inhibitor with anticancer activity. Topoisomerase I-IN-23 competitively binds to the hydrophobic pocket at the Topo I-DNA interface, stabilizes the covalent DNA-Topo I complex, downregulates Topo I protein expression in a concentration-dependent manner, induces S-phase cell cycle arrest in tumor cells, regulates the expression of apoptosis-related proteins Bax, Bcl-2 and cleaved caspase-3 to trigger apoptosis, and inhibits the migration and invasion of tumor cells. Topoisomerase I-IN-23 exhibits in vivo antitumor efficacy in xenograft models. Topoisomerase I-IN-23 can be used in research related to colorectal cancer, lung cancer and hepatocellular carcinoma.

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

Formula: C₃₂H₃₀N₂O₇
Molecular Weight:554.59

Storage:

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

Topoisomerase I-IN-23 Chemical Structure

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

Topoisomerase I

Bax

Bcl-2

Caspase-3

All Topoisomerase Isoforms :

All Bcl-2 Family Isoforms :

All Caspase Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC50	0.028 μM	Antiproliferative cytotoxicity against human lung carcinoma A549 cells. Antiproliferative cytotoxicity against human lung carcinoma A549 cells.	42497470
HCT-116	IC50	0.001 μM	Antiproliferative cytotoxicity against human colorectal carcinoma HCT116 cells. Antiproliferative cytotoxicity against human colorectal carcinoma HCT116 cells.	42497470
HepG2	IC50	0.105 μM	Antiproliferative cytotoxicity against human hepatocellular carcinoma HepG2 cells. Antiproliferative cytotoxicity against human hepatocellular carcinoma HepG2 cells.	42497470
NCM460	IC50	1.19 μM	Antiproliferative cytotoxicity against normal human colon epithelial NCM460 cells. Antiproliferative cytotoxicity against normal human colon epithelial NCM460 cells.	42497470

In Vitro

Topoisomerase I-IN-23 (compound c6) forms a highly stable complex with the human Topo I-DNA system through specific hydrogen bonds and hydrophobic interactions that enhance pocket occupancy, with a total binding free energy of -37.56 kcal/mol^[1].
Topoisomerase I-IN-23 potently inhibits the proliferation of human A549, HCT116 and HepG2 cancer cells, with the strongest inhibitory activity against HCT116 cells (IC₅₀ = 0.001 μM), and exhibits low cytotoxicity toward normal NCM460 colonic epithelial cells^[1].
Topoisomerase I-IN-23 (0.002-0.08 μM; 24 h) potently inhibits the proliferation and migration of human HCT116 colorectal cancer cells in vitro in a concentration-dependent manner^[1].
Topoisomerase I-IN-23 inhibits long-term clonogenic proliferation of human HCT116 colorectal cancer cells^[1].
Topoisomerase I-IN-23 (0.02-0.08 μM; 24 h) downregulates Topo I protein expression in human HCT116 colorectal cancer cells in a concentration-dependent manner in vitro^[1].
Topoisomerase I-IN-23 (0.01-0.1 μM; 24 h) potently inhibits the invasion of human HCT116 colorectal cancer cells in a concentration-dependent manner, with stronger activity than SN-38 (HY-13704)^[1].
Topoisomerase I-IN-23 (0.001-1 μM; 24 h) induces S-phase cell cycle arrest in human HCT116 colorectal cancer cells in a concentration-dependent manner^[1].
Topoisomerase I-IN-23 (0.02-0.08 μM; 24 h) effectively induces apoptosis in human HCT116 colorectal cancer cells^[1].
Topoisomerase I-IN-23 (0.1 μM; 6-24 h) regulates the expression of key cell cycle- and apoptosis-related proteins in human HCT116 colorectal cancer cells, induces S-phase cell cycle arrest, and subsequently triggers apoptosis^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

human colorectal carcinoma HCT116 cells
Concentration:

0.02, 0.04, 0.08 μM
Incubation Time:

24 h
Result:

Caused a concentration-dependent decrease in EdU-positive cells.
Showed significant differences in EdU-positive cell ratios relative to the control group at all tested concentrations.

Cell Migration Assay ^[1]

Cell Line:

human colorectal carcinoma HCT116 cells
Concentration:

0.002, 0.004, 0.008 μM
Incubation Time:

24 h
Result:

Significantly inhibited wound closure in a concentration-dependent manner.
Nearly completely inhibited wound closure at 0.008 μM.
Showed significant differences in wound closure rates relative to the control group at all tested concentrations.

Cell Invasion Assay^[1]

Cell Line:

human colorectal carcinoma HCT116 cells
Concentration:

0.01, 0.05, 0.1 μM
Incubation Time:

24 h
Result:

Inhibited the invasion of human HCT116 colorectal cancer cells in a concentration-dependent manner, with stronger activity than SN-38.

Cell Cycle Analysis^[1]

Cell Line:

human colorectal carcinoma HCT116 cells
Concentration:

0.001, 0.003, 1 μM
Incubation Time:

24 h
Result:

Led to a marked concentration-dependent elevation in the proportion of S-phase HCT116 cells.
Showed significant differences in S-phase cell percentage relative to the control group at all tested concentrations.

Apoptosis Analysis^[1]

Cell Line:

human colorectal carcinoma HCT116 cells
Concentration:

0.02, 0.04, 0.08 μM
Incubation Time:

24 h
Result:

Induced apoptosis in human HCT116 colorectal cancer cells.

Western Blot Analysis^[1]

Cell Line:

human colorectal carcinoma HCT116 cells
Concentration:

0.1 μM
Incubation Time:

6, 12, 24 h
Result:

Upregulated S-phase-specific cyclin A2 (6-24 h), G2-phase-specific cyclin B1 (24 h), pro-apoptotic Bax, and cleaved caspase-3 (6-24 h) in a time-dependent manner.
Downregulated G1-phase-related cyclin D1 and cyclin E1 (6-24 h) and anti-apoptotic Bcl-2 (6-24 h) in a time-dependent manner.

Western Blot Analysis^[1]

Cell Line:

human colorectal carcinoma HCT116 cells
Concentration:

0.02, 0.04, 0.08 μM
Incubation Time:

24 h
Result:

Downregulated Topo I protein expression in human HCT116 colorectal cancer cells in a concentration-dependent manner.

Parmacokinetics

Species	Dose	Route	C_max	AUC_0-∞	T_max	T_1/2	CL	V_z	MRT_0-∞	AUC_0-t	F
Rat^[1]	2.5 mg/kg	i.v.	2205.30 μg/L	991.41 μg/L·h	0.17 h	6.32 h	2.52 L/h/kg	22.97 L/kg	1.31 h	985.53 μg/L·h	32.76 %
Rat^[1]	2.5 mg/kg	i.p.	74.42 μg/L	322.90 μg/L·h	0.25 h	4.10 h	7.68 L/h/kg	45.50 L/kg	5.41 h	/	/

In Vivo

Topoisomerase I-IN-23 (compound c6) (2-5 mg/kg; i.p.; once every other day) exhibits significant in vivo anti-tumor efficacy with favorable safety in the HCT116 xenograft model^[1].

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

Animal Model:

Female BALB/c nude mice (4‑week‑old), received subcutaneous injections of HCT116 cells (1 × 10⁶ cells per mouse) in the right flank.^[1]
Dosage:

2 mg/kg; 5 mg/kg
Administration:

i.p.; every other day
Result:

Exhibited significant in vivo anti-tumor efficacy with favorable safety.

Chemical Information

Molecular Weight 554.59
Formula C₃₂H₃₀N₂O₇
SMILES

O=C(COC1=CC=C(N=C(C(N2C3)=CC([C@@](O)(CC)C(OC4)=O)=C4C2=O)C3=C5CC)C5=C1)C6=CC(OC)=C(C)C=C6
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

Handling Instructions (2659 KB)

References

[1]. Zhang Y, et al. Discovery of novel hydroxycamptothecin derivatives as potent Topo I inhibitors for antitumor guided by molecular dynamics. European journal of medicinal chemistry. 2026 Jul 22;318:119163.

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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MOQ

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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Topoisomerase I-IN-23

All Topoisomerase Isoforms

All Bcl-2 Family Isoforms

All Caspase Isoforms