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Cat. No.: HY-188268

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TXX-1-10

TXX-1-10 is a HPIP inhibitor. TXX-1-10 reduces HPIP expression and disrupts the formation of the EGFR-RAS-ERK signaling complex. TXX-1-10 inhibits AKT and ERK1/2 phosphorylation/activation and inhibits FAK and paxillin phosphorylation. TXX-1-10 induces G1 cell cycle arrest and apoptosis, and inhibits cancer cell proliferation, migration, invasion, epithelial-mesenchymal transition, and tumor growth/metastasis. TXX-1-10 can be used for research on breast cancer and lung cancer.

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

CAS No.: 2489250-48-6
Formula: C₂₃H₁₈Cl₃IN₄O
Molecular Weight:599.68

Storage:

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

TXX-1-10 Chemical Structure

CAS No.: 2489250-48-6

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Use of MCE Products

One-stop solution for XDC (ADC/PDC/RDC/ApDC/FDC/ISAC/VDC/SMDC)

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

Biological Activity

Description

IC₅₀ & Target

^[1]^[2]

HPIP

EGFR

Ras

ERK1

ERK2

Akt

FAK

paxillin

All EGFR Isoforms :

All Ras Isoforms :

All ERK Isoforms :

All Akt Isoforms :

In Vitro

Anti-cancerApoptosisCell Cycle RegulationCarbohydrate MetabolismOthers

Anti-cancer

TXX-1-10 (1-10 µM) reduces HPIP expression in HPIP-copGFP ZR75-1 and breast cancer cells in an HPIP-dependent manner, and inhibits AKT/ERK1/2 phosphorylation^[1].
TXX-1-10 (48 h) reduces cancer cell viability with IC₅₀ values of 2.2-7.9 µM and inhibits the proliferation and colony formation of MDA-MB-231 and ZR-751 cells^[1].
TXX-1-10 (1-10 µM; migration 0-12 h; invasion 24 h) inhibits the migration and invasion of ZR-751 and MDA-MB-231 cells^[1].
TXX-1-10 (24 h) inhibits FAK and paxillin phosphorylation in ZR75-1 and MDA-MB-231 cells and reverses EMT marker expression^[1].
TXX-1-10 broadly modulates the expression of genes related to DNA replication, cell cycle, apoptosis, adhesion, and migration/invasion in MDA-MB-231 cells, including genes regulated by HPIP^[1].
TXX-1-10 reduces HPIP expression in A549 and ZR75-1 cancer cells and decreases the interactions among components of the EGFR-RAS-ERK pathway^[2].
TXX-1-10 (10 μM; 24 h) inhibits the activation of the EGFR-RAS-ERK signaling pathway in A549 and ZR75-1 cancer cells^[2].
TXX-1-10 inhibits the proliferation of A549, ZR75-1, and Calu-3 cancer cells^[2].

Anti-cancer

Apoptosis

Cell Cycle Regulation

TXX-1-10 (36-48 h) induces G1 phase cell cycle arrest and apoptosis in ZR-751 and MDA-MB-231 cells, increasing the apoptosis rates to 42.1% and 47.2%, respectively^[1].

Anti-cancer

Carbohydrate Metabolism

TXX-1-10 inhibits EGFR-RAS-ERK signaling-mediated aerobic glycolysis in A549 and ZR75-1 cancer cells^[2].

Others

TXX-1-10 decreases the ERα target genes pS2 and cathepsin D, whereas HPIP overexpression reverses this inhibitory effect^[1].

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

Cell Migration Assay ^[1]

Cell Line:

ZR-751 and MDA-MB-231 cells
Concentration:

1, 5, 10 µM
Incubation Time:

0 and 12 h (migration); 24 h (invasion)
Result:

Wound-healing assay and matrigel invasion assay showed that TXX-1-10 specifically inhibited the migration and invasion of ZR-751 and MDA-MB-231 cells in a dose-dependent manner.

Western Blot Analysis^[2]

Cell Line:

A549 lung cancer and ZR75-1 breast cancer cells
Concentration:

10 μM
Incubation Time:

24 h
Result:

Abrogated the ability of EGFR, GRB2, KRAS, or RAF1 overexpression to stimulate GTP-bound RAS level, RAF1, MEK1/2, and ERK1/2 phosphorylation, and c-Myc, HIF-1α, and c-Fos expression; these effects were reversed by HPIP overexpression.

In Vivo

Anti-cancerApoptosis

Anti-cancer

TXX-1-10 (30 mg/kg; intraperitoneal injection) inhibits breast cancer lung metastasis and improves mouse survival^[1].
TXX-1-10 (30 mg/kg; intraperitoneal injection) inhibits tumor growth in the ZR75-1 breast cancer xenograft model^[2].
TXX-1-10 (30 mg/kg; intraperitoneal injection) inhibits tumor growth in the A549 lung cancer xenograft model^[2].

Anti-cancer

Apoptosis

TXX-1-10 (30 mg/kg; intraperitoneal injection; approximately 20 days) inhibits breast tumor growth in the MDA-MB-231 xenograft model^[1].

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

Animal Model:

nude (BALB/c background; female; 6 weeks old)^[1]
Dosage:

30 mg/kg
Administration:

i.p.; ~20 days
Result:

Compared to the Rimonabant (HY-14136) groups, the TXX-1-10 groups showed a more significant inhibitory effect on the amount of Ki67 (proliferation marker)-, CD31 (endothelial cell marker)-, and HPIP-positive tumor cells, and a more significant stimulatory effect on the amount of cleaved caspase-3 (apoptosis marker)-positive tumor cells.

Animal Model:

nude (BALB/c)^[1]
Dosage:

30 mg/kg
Administration:

i.p.
Result:

The lung metastasis of the TXX-1-10 group was significantly decreased compared with that of the Rimonabant group.
Survival rates of the TXX-1-10 groups were higher than those of the Rimonabant groups.

Animal Model:

BALB/c nude (female, 6 weeks old)^[2]
Dosage:

30 mg/kg
Administration:

i.p.
Result:

Inhibited tumor growth in the ZR75-1 breast cancer xenograft, with effects similar to HPIP knockout in KRAS- and MEK1-overexpressing tumors.

Animal Model:

nude (6 weeks old)^[2]
Dosage:

30 mg/kg
Administration:

i.p.
Result:

Inhibited tumor growth in the A549 lung cancer xenograft, with effects similar to HPIP knockout in KRAS- and MEK1-overexpressing tumors.

Related Protocols :

Chemical Information

CAS No. 2489250-48-6
Molecular Weight 599.68
Formula C₂₃H₁₈Cl₃IN₄O
SMILES

CC1=C(C2=CC=C(Cl)C=C2)N(C3=CC=C(Cl)C=C3Cl)N=C1C(NC4=CC=C[N+](C)=C4)=O.[I-]
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]. Li P, et al. A novel chemical inhibitor suppresses breast cancer cell growth and metastasis through inhibiting HPIP oncoprotein. Cell death discovery. 2021 Jul 29;7(1):198.

[2]. Jiang Q, et al. HPIP is an essential scaffolding protein running through the EGFR-RAS-ERK pathway and drives tumorigenesis. Science advances. 2023 Jun 09;9(23):eade1155.

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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.

Bioz

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

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TXX-1-10

All EGFR Isoforms

All Ras Isoforms

All ERK Isoforms

All Akt Isoforms