2. TGF-beta/Smad Cytoskeleton MAPK/ERK Pathway Apoptosis Stem Cell/Wnt
  3. TGF-β Receptor Integrin Raf RIP kinase ERK
  4. KBU2046

KBU2046 is an orally active transforming growth factor-β (TGF-β1) inhibitor. KBU2046 reduces integrin family protein expression, decreases Raf, RIPK1 and ERK phosphorylation to deactivate the ERK signaling pathway, and down-regulates genes linked to TGF-β1 maturation. KBU2046 suppresses tumor cell motility, impedes cancer invasion and metastasis, and inhibits human ESCC growth and metastasis in a murine model. KBU2046 can be used for the researches of triple-negative breast cancer and esophageal squamous cell carcinoma.

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KBU2046

KBU2046 Chemical Structure

CAS No. : 1143863-69-7

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Based on 1 publication(s) in Google Scholar

KBU2046 Related Antibodies

Top Publications Citing Use of Products

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ALK1 ALK2 ALK3 ALK4 ALK5 ALK6 ALK7 TGFβR2 ACVR2A ACVR2B BMP

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αvβ1 αvβ3 αvβ5 αvβ6 αvβ8 α5β1 α1β1 α2β1 α4β1 α9β1 αIIbβ3 α4β7 αLβ2

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B-Raf C-Raf Raf

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RIPK1 RIPK2 RIPK3

View All ERK Isoform Specific Products:

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ERK ERK1 ERK2 ERK5 ERK8

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

KBU2046 is an orally active transforming growth factor-β (TGF-β1) inhibitor. KBU2046 reduces integrin family protein expression, decreases Raf, RIPK1 and ERK phosphorylation to deactivate the ERK signaling pathway, and down-regulates genes linked to TGF-β1 maturation. KBU2046 suppresses tumor cell motility, impedes cancer invasion and metastasis, and inhibits human ESCC growth and metastasis in a murine model. KBU2046 can be used for the researches of triple-negative breast cancer and esophageal squamous cell carcinoma[1][2].

IC50 & Target[1]

RIPK1

 

ERK1

 

ERK2

 

In Vitro

KBU2046 (1-10 μM; 24-48 h) does not significantly alter the proliferation of MDA-MB-231 or BT-549 TNBC cells[1].
KBU2046 (1-10 μM; 24 h) dose-dependently inhibits TGF-β1-induced motility of MDA-MB-231 and BT-549 TNBC cells, with maximum inhibition at 10 μM, reducing motility to 50.77% and 36.09% of control levels, respectively[1].
KBU2046 (10 μM; 24 h) significantly down-regulates the mRNA expression of LRRC8E, LTBP3, DNAL1, and MAFF in MDA-MB-231 and BT-549 TNBC cells[1].
KBU2046 (1-10 μM; 48 h) dose-dependently suppresses integrin αv and integrin α6 protein expression in MDA-MB-231 and BT-549 TNBC cells, and reverses TGF-β1-mediated up-regulation of these integrins[1].
KBU2046 (10 μM; 15-60 min) time-dependently inhibits phosphorylation of Raf1 and ERK1/2 in MDA-MB-231 and BT-549 TNBC cells, with significant suppression evident within 15 min of treatment[1].
KBU2046 (1-10 μM; 24-48 h) inhibits collective migration of KYSE-30 and KYSE-410 ESCC cells in a time- and concentration-dependent manner[2].
KBU2046 (10 μM; 72 h) inhibits EGF and TGF-β-stimulated single-cell migration and invasion of KYSE-30 and KYSE-410 ESCC cells[2].
KBU2046 (1-10 μM; 72 h) does not inhibit proliferation of KYSE-30 or KYSE-410 ESCC cells after 72-hour incubation[2].
KBU2046 (10 μM; 30 min) inhibits EGF-stimulated phosphorylation of RIPK1 at Ser166 in KYSE-30 and KYSE-410 ESCC cells[2].
KBU2046 (1-10 μM) downregulates ITGA3, ITGA6, and ITGAV expression in KYSE-30 and KYSE-410 ESCC cells in a concentration-dependent manner[2].
KBU2046 (10 μM) selectively modulates expression of motility-related proteins in KYSE-30 ESCC cells, with significant downregulation of integrin family members and other ECM-adhesion proteins that are overexpressed in human ESCC[2].

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

KBU2046 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: MDA-MB-231, BT-549 cells
Concentration: 1, 5, 10 μM
Incubation Time: 24 h; 48 h;
Result: Exhibited no time- or concentration-dependent alterations in cell proliferation in either MDA-MB-231 or BT-549 cells.

Cell Migration Assay [1]

Cell Line: MDA-MB-231, BT-549 cells
Concentration: 1, 5, 10 μM
Incubation Time: 24 h
Result: Reduced TGF-β1-induced cellular motility rates to 92.97% at 1 μM, 70.59% at 5 μM, and 50.77% at 10 μM in MDA-MB-231 cells compared to control.
Reduced TGF-β1-induced cellular motility rates to 78.43% at 1 μM, 43.55% at 5 μM, and 36.09% at 10 μM in BT-549 cells compared to control.

Western Blot Analysis[1]

Cell Line: MDA-MB-231, BT-549 cells
Concentration: 1, 5, 10 μM
Incubation Time: 48 h (co-treatment with 10 ng/mL TGF-β1)
Result: Reduced integrin αv protein levels to 67.28% at 1 μM, 57.61% at 5 μM, and 42.29% at 10 μM, and integrin α6 levels to 87.15% at 1 μM, 76.54% at 5 μM, and 45.26% at 10 μM in MDA-MB-231 cells compared to control.
Reduced integrin αv levels to 96.13% at 1 μM, 58.68% at 5 μM, and 51.11% at 10 μM, and integrin α6 levels to 82.47% at 1 μM, 66.29% at 5 μM, and 61.89% at 10 μM in BT-549 cells compared to control.
Partially reversed TGF-β1-mediated up-regulation of integrin αv and α6 in both cell lines.
Exhibited no significant effects on integrin α3 or β8 protein levels.

Western Blot Analysis[1]

Cell Line: MDA-MB-231, BT-549 cells
Concentration: 10 μM
Incubation Time: 15 min; 30 min; 60 min
Result: Reduced phosphorylation levels of Raf1 (Ser338) and ERK1/2 (Thr202/Tyr204) in a time-dependent manner in both MDA-MB-231 and BT-549 cells.
Showed statistically significant reductions at 15, 30, and 60 min compared to control levels.

Cell Migration Assay[2]

Cell Line: KYSE-30, KYSE-410 esophageal squamous cell carcinoma (ESCC) cells
Concentration: 1 μM, 10 μM
Incubation Time: 24 h, 48 h
Result: Significantly inhibited wound gap closure in a time- and concentration-dependent manner.
Decreased wound closure by 46.7% in KYSE-30 cells and 47.5% in KYSE-410 cells at 48 h with 10 μM treatment compared to vehicle controls.

Cell Proliferation Assay[2]

Cell Line: KYSE-30, KYSE-410 esophageal squamous cell carcinoma (ESCC) cells
Concentration: 1 μM, 10 μM
Incubation Time: 72 h
Result: Had no significant effect on cell viability of KYSE-30 or KYSE-410 cells after 72 h, indicating no inhibition of cell proliferation.

Western Blot Analysis[2]

Cell Line: EGF-stimulated KYSE-30, KYSE-410 esophageal squamous cell carcinoma (ESCC) cells
Concentration: 10 μM (in the presence of 5 ng/mL EGF)
Incubation Time: 30 min
Result: Markedly inhibited EGF-stimulated phosphorylation of RIPK1 at Ser166 in both KYSE-30 and KYSE-410 cells.
In Vivo

KBU2046 (80 mg/kg; i.g.; every other day; 12 total doses) completely inhibits pulmonary metastasis of ESCC cells in male NOD-SCID mice[2].
KBU2046 (80 mg/kg; i.g.; every 2 days; 12 total doses) reduces mean ESCC tumor volume to 62% of control levels in male athymic nude mice, without causing significant systemic toxicity[2].

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

Animal Model: NOD-SCID (male, 4-6 weeks old, 16-18 g, tail vein injection of 1.5×106 KYSE-30 ESCC cells)[2]
Dosage: 80 mg/kg
Administration: p.o.; every other day; 12 total doses
Result: Completely inhibited pulmonary metastasis, with 0 of 4 treated mice showing pulmonary metastases compared to 3 of 4 control mice (one-sided t-test, P=0.03).
Showed no significant difference in body weight compared to control group.
Caused no histomorphological changes in heart, liver, or spleen.
Animal Model: athymic nude (male, 4-6 weeks old, SPF grade, subcutaneous implantation of 1×106 KYSE-30 ESCC cells into the right flank)[2]
Dosage: 80 mg/kg
Administration: p.o.; every 2 days; 12 total doses
Result: Reduced mean tumor volume to 62% of control levels, though the difference was not statistically significant.
Showed no significant difference in body weight compared to control group.
Molecular Weight

242.25

Formula

C15H11FO2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1C(C2=CC=C(F)C=C2)COC3=CC=CC=C13
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (206.40 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.1280 mL 20.6398 mL 41.2797 mL
5 mM 0.8256 mL 4.1280 mL 8.2559 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (10.32 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (10.32 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 4.1280 mL 20.6398 mL 41.2797 mL 103.1992 mL
5 mM 0.8256 mL 4.1280 mL 8.2559 mL 20.6398 mL
10 mM 0.4128 mL 2.0640 mL 4.1280 mL 10.3199 mL
15 mM 0.2752 mL 1.3760 mL 2.7520 mL 6.8799 mL
20 mM 0.2064 mL 1.0320 mL 2.0640 mL 5.1600 mL
25 mM 0.1651 mL 0.8256 mL 1.6512 mL 4.1280 mL
30 mM 0.1376 mL 0.6880 mL 1.3760 mL 3.4400 mL
40 mM 0.1032 mL 0.5160 mL 1.0320 mL 2.5800 mL
50 mM 0.0826 mL 0.4128 mL 0.8256 mL 2.0640 mL
60 mM 0.0688 mL 0.3440 mL 0.6880 mL 1.7200 mL
80 mM 0.0516 mL 0.2580 mL 0.5160 mL 1.2900 mL
100 mM 0.0413 mL 0.2064 mL 0.4128 mL 1.0320 mL
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KBU2046 Related Classifications

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  • 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:

KBU20461143863-69-7KBU 2046KBU-2046TGF-β ReceptorIntegrinRafRIP kinaseERKTransforming growth factor beta receptorsRaf kinasesReceptor-interacting protein kinasesRIPKExtracellular signal regulated kinasesesophageal squamous cell carcinomaKYSE-410integrin family proteintriple-negative breast cancerKYSE-30ERK signaling pathwayMDA-MB-231BT-549RIPK1TGF-β1Inhibitorinhibitorinhibit

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