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Cat. No.: HY-189210A

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TopBP1-IN-4

TopBP1-IN-4 is a TopBP1 inhibitor, with an IC₅₀ value of 2.47 to 3.8 nM against the TopBP1 BRCT7/8 domain. TopBP1-IN-4 selectively disrupts BRCT7/8-dependent oncogenic protein-protein interactions, does not interfere with other BRCT domain-mediated functions of TopBP1, and has no effect on DNA replication. TopBP1-IN-4 restores E2F1-mediated Apoptosis in cells. TopBP1-IN-4 induces mitotic catastrophe in cells. TopBP1-IN-4 overcomes Osimertinib (HY-15772) resistance in EGFR-mutant non-small cell lung cancer models. TopBP1-IN-4 can be used in studies related to triple-negative breast cancer, ovarian cancer, non-small cell lung cancer, and acute myeloid leukemia.

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

Formula: C₂₆H₂₆Cl₂N₂O₄
Molecular Weight:501.40

Storage:

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

TopBP1-IN-4 Chemical Structure

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Use of MCE Products

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

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

Description

All Topoisomerase Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
MDA-MB-468	IC50	0.15 μM	Inhibition of clonogenic survival in MDA-MB-468 triple-negative breast cancer cells assessed by clonogenic survival assay with crystal violet staining. Inhibition of clonogenic survival in MDA-MB-468 triple-negative breast cancer cells assessed by clonogenic survival assay with crystal violet staining.	42555732
MDAH 2774	IC50	0.18 μM	Inhibition of clonogenic survival in MDAH-2774 ovarian cancer cells assessed by clonogenic survival assay with crystal violet staining. Inhibition of clonogenic survival in MDAH-2774 ovarian cancer cells assessed by clonogenic survival assay with crystal violet staining.	42555732
A2780cis	IC50	0.46 μM	Inhibition of clonogenic survival in cisplatin-resistant A2780cis ovarian cancer cells assessed by clonogenic survival assay with crystal violet staining. Inhibition of clonogenic survival in cisplatin-resistant A2780cis ovarian cancer cells assessed by clonogenic survival assay with crystal violet staining.	42555732
A549	IC50	0.5 μM	Inhibition of clonogenic survival in A549 lung cancer cells assessed by clonogenic survival assay with crystal violet staining. Inhibition of clonogenic survival in A549 lung cancer cells assessed by clonogenic survival assay with crystal violet staining.	42555732
HCC95	IC50	0.54 μM	Inhibition of clonogenic survival in HCC95 lung cancer cells assessed by clonogenic survival assay with crystal violet staining. Inhibition of clonogenic survival in HCC95 lung cancer cells assessed by clonogenic survival assay with crystal violet staining.	42555732
H1975	IC50	0.32 μM	Inhibition of clonogenic survival in EGFR-mutated H1975 NSCLC cells assessed by clonogenic survival assay with crystal violet staining. Inhibition of clonogenic survival in EGFR-mutated H1975 NSCLC cells assessed by clonogenic survival assay with crystal violet staining.	42555732
Kasumi 1	IC50	0.46 μM	Reduction of cell viability in Kasumi-1 acute myelogenous leukemia cells incubated for 45 hours by CCK-8 assay using WST-8 solution. Reduction of cell viability in Kasumi-1 acute myelogenous leukemia cells incubated for 45 hours by CCK-8 assay using WST-8 solution.	42555732

In Vitro

TopBP1-IN-4 (Compound CS18) (0-0.02 μM) potently inhibits the peptide binding function of TopBP1-BRCT7/8 with an IC₅₀ between 2.47 nM and 3.8 nM in a cell-free in vitro system^[1].
TopBP1-IN-4 (0.1-2.5 μM) exhibits strong clonogenic growth inhibitory activity across a broad panel of cancer cell lines, with IC₅₀ values in the sub-micromolar range spanning 0.15 μM to 0.67 μM^[1].
TopBP1-IN-4 (3 days) potently suppresses viability of t(8;21) translocation, p53^R248Q mutant Kasumi-1 acute myelogenous leukemia cells with an IC₅₀ of 0.46 μM^[1].

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

Cell Viability Assay^[1]

Cell Line:

Kasumi-1 acute myelogenous leukemia cells
Concentration:

Titrated across a range of concentrations
Incubation Time:

3 days
Result:

Reduced Kasumi-1 cell viability with an IC₅₀ of 0.46 μM.

In Vivo

Anti-cancerApoptosis

Anti-cancer

Apoptosis

TopBP1-IN-4 (15-60 mg/kg; i.p.; 3 times weekly; 3 weeks; twice weekly; 15 days) exerts potent, well-tolerated, dose-dependent antitumor activity against BCM2665 TNBC PDX in NSG mice, with confirmed on-target engagement of TopBP1 in vivo^[1].

Anti-cancer

TopBP1-IN-4 (30 mg/kg; i.p.; 3 times weekly; 17 days) significantly inhibits the growth of Osimertinib (HY-15772)-resistant H1975 NSCLC xenografts in NSG mice with minimal normal tissue toxicity^[1].

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

Animal Model:

NOD.Cg-Prkdcscid Il2rgtm1Wjl/SzJ (NSG) female mice^[1]
Dosage:

15 mg/kg (TGI); 30 mg/kg (TGI); 45 mg/kg (TGI); 60 mg/kg (TGI); 40 mg/kg (TGI)
Administration:

i.p.; 3 times weekly; 3 weeks (15-60 mg/kg); i.p.; twice weekly; 15 days (40 mg/kg)
Result:

Suppressed TNBC PDX tumor growth at 40 mg/kg twice weekly.
Induced increased PARP1 cleavage in tumor tissue at 40 mg/kg twice weekly.
Increased the thermal stability of TopBP1 in xenograft tumor tissue confirming direct in vivo target engagement at 40 mg/kg twice weekly.
Did not induce apoptosis or alter Ki-67 staining in intestinal crypts at all tested doses.
Showed no significant mouse body weight loss or overt toxicity at all tested doses.
Exhibited dose-dependent in vivo antitumor activity across the 15 to 60 mg/kg three times weekly dose range, with no plateau in efficacy observed at the highest 60 mg/kg dose.
All doses up to 60 mg/kg were well tolerated by mice.

Animal Model:

NOD.Cg-Prkdcscid Il2rgtm1Wjl/SzJ (NSG) mice^[1]
Dosage:

30 mg/kg
Administration:

i.p.; 3 times weekly; 17 days
Result:

Reduced H1975-OsiR tumor growth significantly.
Showed no significant changes in mouse body weight at 30 mg/kg three times weekly.
Did not induce alteration of Ki-67 staining or apoptosis in mouse intestinal crypts, indicating no overt intestinal tissue toxicity.

Related Protocols :

Chemical Information

Molecular Weight 501.40
Formula C₂₆H₂₆Cl₂N₂O₄
SMILES

OC1=C(C2=CC=CC=C2)C=C(OC(C=C3CN4CCN(C5=CC=C(O)C=C5)CC4)=O)C3=C1.Cl.Cl
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]. Lin FT, et al. Development of a structurally distinct TopBP1 inhibitor that enhances PARP blockade and reverses osimertinib resistance. Sci Adv. 2026 Aug 7;12(32):eaeg1996.

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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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100 mg

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