2. Cell Cycle/DNA Damage Epigenetics NF-κB
  3. HDAC NF-κB
  4. ITF 3756

ITF 3756 is a selective, orally active HDAC6 inhibitor. ITF 3756 antagonizes TNF-α-induced activation of the NF-κB pathway. ITF 3756 reduces PD-L1 expression on human monocytes and CD8+ T cells, and exhibits antitumor activity. ITF 3756 can be used in colon cancer-related research.

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ITF 3756

ITF 3756 Chemical Structure

CAS No. : 2247608-27-9

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ITF 3756 Related Antibodies

Top Publications Citing Use of Products

View All HDAC Isoform Specific Products:

View All Isoforms
HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

View All NF-κB Isoform Specific Products:

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

  • Biological Activity

  • Purity & Documentation

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Description

ITF 3756 is a selective, orally active HDAC6 inhibitor. ITF 3756 antagonizes TNF-α-induced activation of the NF-κB pathway. ITF 3756 reduces PD-L1 expression on human monocytes and CD8+ T cells, and exhibits antitumor activity. ITF 3756 can be used in colon cancer-related research[1][2][3].

IC50 & Target[1]

HDAC6

 

Cellular Effect
Cell Line Type Value Description References
697 IC50
> 1 μM
Compound: 42; ITF3756
Cytotoxicity against human 697 cells after 48 hrs by CellTiter 96 aqueous one solution assay
Cytotoxicity against human 697 cells after 48 hrs by CellTiter 96 aqueous one solution assay
[PMID: 31710483]
PBMC IC50
> 1 μM
Compound: 42; ITF3756
Cytotoxicity against human PBMC cells after 72 hrs by CellTiter 96 aqueous one solution assay
Cytotoxicity against human PBMC cells after 72 hrs by CellTiter 96 aqueous one solution assay
[PMID: 31710483]
Sf9 IC50
17 nM
Compound: 42; ITF3756
Inhibition of recombinant full length human N-terminal GST-tagged HDAC6 expressed in baculovirus infected sf9 insect cells pretreated with compound followed by Fluor de Lys deacetylase substrate addition by fluorescence method
Inhibition of recombinant full length human N-terminal GST-tagged HDAC6 expressed in baculovirus infected sf9 insect cells pretreated with compound followed by Fluor de Lys deacetylase substrate addition by fluorescence method
[PMID: 31710483]
In Vitro

ITF 3756 (6 h) downregulates the expression of TNF-α-induced activation and differentiation markers by regulating the expression of specific genes, and induces a phenotype with weaker immunosuppressive properties in purified human monocytes[1].
ITF3756 (0.06-1.5 μM; 4-20 h) downregulates PD-L1 expression in a dose- and time-dependent manner, attenuates the immunosuppressive phenotype of primary human monocytes stimulated with TNF-α, and promotes the costimulatory phenotype by upregulating CD40 expression, with no cytotoxicity observed at the tested concentrations[2].
ITF3756 (1 μM; 3-6 h) upregulates CD40 gene expression and downregulates PD-L1 gene expression in TNF-α-stimulated primary human monocytes, with a significant effect on PD-L1 observed at 4 hours post-stimulation[2].
ITF3756 (1 μM; overnight) downregulates PD-L1 expression on TNF-α-stimulated primary human monocytes derived from patients with colorectal cancer and breast cancer, which is consistent with the effect observed in monocytes from healthy donors[2]
ITF3756 (1 μM; 6 h) inhibits the TNF-α, NF-κB and NOD-like receptor signaling pathways, downregulates the expression of inhibitory immune checkpoint genes and M2 macrophage markers, and upregulates metabolic pathways in primary human monocytes stimulated with TNF-α, thereby inducing their transition to a phenotype with weaker immunosuppression and stronger metabolic activity[2].
ITF3756 (1 μM; 19 h) downregulates the expression of proteins related to antigen presentation, inflammatory signaling pathways and cell death in primary human monocytes stimulated by TNF-α, while upregulating the expression of proteins related to metabolic pathways. This is consistent with the results of transcriptomic studies showing that these cells exhibit a phenotype with lower immunosuppression and higher metabolic activity[2].
ITF3756 (1 μM; 2.15 h) inhibits TNF-α-induced activation of the NF-κB pathway in primary human monocytes by reducing the phosphorylation level of p65 at the Ser536 site[2].
ITF3756 (1 μM; 6 d) enhances the capacity of TNF-α-stimulated primary human monocytes to activate allogeneic T cells; this effect is reflected by increased T cell proliferation levels in MLR assays and produces a synergistic effect when combined with anti-PD-L1 antibodies[2].
ITF3756 (0.5-1 μM; 5 d) enhances the antigen-presenting cell phenotype of monocyte-derived iDCs and mDCs by upregulating CD86 expression while slightly downregulating PD-L1 expression[2].
ITF3756 (1 μM; 10 d) enhances the ability of monocyte-derived iDCs to activate allogeneic T cells, which is confirmed by the increased T cell proliferation observed in mixed lymphocyte reaction (MLR) assays[2].
ITF3756 (1-10 μM; 48 h) reduces the viability of HCT116 colon cancer cells in a dose-dependent manner. After 48 h of treatment, cell viability decreases by approximately 50% at 5 μM, and is almost completely lost at 10 μM[3].
ITF3756 (1-10 μM; 48 h) reduces the viability of HT29 colon cancer cells in a dose-dependent manner. After 48 h of treatment, cell viability decreases by approximately 25% at 5 μM and by approximately 50% at 10 μM[3].
ITF3756 (2-7 μM; 48 h) promotes lipid accumulation in HCT116 colon cancer cells in a dose-dependent manner within 48 h, with a significant increase in lipid droplet formation observed at 7 μM[3].
ITF3756 (2-7 μM; 48 h) dose-dependently increases lipid accumulation in HT29 colon cancer cells, with an action duration exceeding 48 h, and the accumulation levels are significantly elevated at concentrations of 5 μM and 7 μM[3].
ITF3756 (2 μM; 48 h) selectively inhibits HDAC6 activity in HCT116 colon cancer cells for a duration exceeding 48 h, which is evidenced by increased levels of α-acetylated tubulin[3].
Treatment with ITF3756 (2 μM; 48 h) alone exerts mild, subtoxic cytostatic effects on HCT116 colon cancer cells within 48 h[3].
ITF3756 (2 μM; 48 h) alone exerts mild subtoxic effects on the viability of HT29 colon cancer cells within 48 h[3].
ITF3756 (2 μM; 24-48 h) alone slightly increases p53 levels in HCT116 colon cancer cells within 24-48 h, but does not activate apoptotic markers[3].
Treatment with ITF3756 (2 μM; 24 h) alone induces mild lipogenic activity in HCT116 colon cancer cells within 24 h, which is evidenced by a moderate increase in the levels of cleaved SREBP-1 and PPAR-γ[3].

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

ITF 3756 Related Antibodies

Cell Viability Assay[3]

Cell Line: HCT116 colon cancer cells
Concentration: 1, 2, 3, 4, 5, 7 and 10 μM
Incubation Time: 48 h
Result: Reduced HCT116 cell viability in a dose-dependent manner.
Reduced viability by ~50% at 5 μM relative to untreated controls.
Reduced viability to near 0% at 10 μM relative to untreated controls.
Induced cell shrinkage and detachment (signs of cell death) at 7 μM.

Cell Viability Assay[3]

Cell Line: HT29 colon cancer cells
Concentration: 1, 2, 3, 4, 5, 7 and 10 μM
Incubation Time: 48 h
Result: Reduced HT29 cell viability in a dose-dependent manner.
Reduced viability by ~25% at 5 μM relative to untreated controls.
Reduced viability by ~50% at 10 μM relative to untreated controls.
Reduced cell number but maintained viability at 7 μM.

Western Blot Analysis[3]

Cell Line: HCT116 colon cancer cells
Concentration: 2 μM
Incubation Time: 48 h
Result: Significantly increased α-acetylated tubulin levels relative to untreated controls, confirming selective HDAC6 inhibition.

Cell Viability Assay[3]

Cell Line: HCT116 colon cancer cells
Concentration: 2 μM
Incubation Time: 48 h
Result: Produced a modest reduction in HCT116 cell viability (subtoxic dose, cytostatic effect) relative to untreated controls.

Cell Viability Assay[3]

Cell Line: HT29 colon cancer cells
Concentration: 2 μM
Incubation Time: 48 h
Result: Produced a modest reduction in HT29 cell viability (subtoxic dose) relative to untreated controls.

Western Blot Analysis[3]

Cell Line: HCT116 colon cancer cells
Concentration: 2 μM
Incubation Time: 24 h; 48 h
Result: Produced a modest increase in p53 levels at 24 h and 48 h relative to untreated controls.
Did not induce cleavage of caspase 3 or PARP-1.

Western Blot Analysis[3]

Cell Line: HCT116 colon cancer cells
Concentration: 2 μM
Incubation Time: 24 h
Result: Produced a faint increase in cleaved SREBP-1 levels relative to untreated controls.
Produced a modest increase in PPAR-γ levels relative to untreated controls.
Detected a faint band of cleaved SREBP-1 in the nuclear fraction.

Cell Viability Assay[3]

Cell Line: HCT116 and HT29 colon cancer cells
Concentration: 2 μM (with 1 h pre-incubation with 7.5 μM DGAT-1i and 10 μM DGAT-2i)
Incubation Time: 24 h; 48 h
Result: Exacerbated the viability-reducing effect of the 2 μM ITF3756/5 nM bortezomib combination, with further reduced cell viability and increased signs of cell death relative to the combination alone.

Cell Viability Assay[3]

Cell Line: HCT116 colon cancer cells
Concentration: 2 μM (with 16 h pre-transfection with SREBP-1 siRNA)
Incubation Time: 24 h
Result: Potentiated the viability-reducing effect of the 2 μM ITF3756/5 nM bortezomib combination in SREBP-1-silenced cells, with greater reduction in cell viability relative to control siRNA-transfected cells.
In Vivo

ITF3756 (25-50 mg/kg; oral administration; 1-3 times daily for 14 consecutive days) inhibits tumor growth in the mouse CT26 colon cancer model in a dose- and regimen-dependent manner[2].

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

Animal Model: BALB/c (6-week-old female; subcutaneous injection of 1 x 10^6 CT26 tumor cells)[2]
Dosage: 25 mg/kg (BID, TID); 50 mg/kg (QD, BID, TID)
Administration: oral gavage; twice a day (BID); three times a day (TID); once a day (QD) for 14 days
Result: Achieved significant tumor growth inhibition starting at day 17 post-transplant, with a maximum 46% inhibition by study end (25 mg/kg TID).
Achieved significant tumor growth inhibition observed at day 19 and 24 post-transplant, with a maximum 31% inhibition (25 mg/kg BID).
Achieved significant tumor growth inhibition starting at day 17 post-transplant, with maximum inhibition of 52% (BID) and 55% (TID) by study end (50 mg/kg).
Achieved significant tumor growth inhibition observed at day 19 and 24 post-transplant, with a maximum 27% inhibition (50 mg/kg QD).
Molecular Weight

301.32

Formula

C13H11N5O2S
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(C1=CC=C(CN2N=NN=C2C3=CC=CS3)C=C1)NO
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 : 125 mg/mL (414.84 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 3.3187 mL 16.5937 mL 33.1873 mL
5 mM 0.6637 mL 3.3187 mL 6.6375 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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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (6.90 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: ≥ 2.08 mg/mL (6.90 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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 3.3187 mL 16.5937 mL 33.1873 mL 82.9683 mL
5 mM 0.6637 mL 3.3187 mL 6.6375 mL 16.5937 mL
10 mM 0.3319 mL 1.6594 mL 3.3187 mL 8.2968 mL
15 mM 0.2212 mL 1.1062 mL 2.2125 mL 5.5312 mL
20 mM 0.1659 mL 0.8297 mL 1.6594 mL 4.1484 mL
25 mM 0.1327 mL 0.6637 mL 1.3275 mL 3.3187 mL
30 mM 0.1106 mL 0.5531 mL 1.1062 mL 2.7656 mL
40 mM 0.0830 mL 0.4148 mL 0.8297 mL 2.0742 mL
50 mM 0.0664 mL 0.3319 mL 0.6637 mL 1.6594 mL
60 mM 0.0553 mL 0.2766 mL 0.5531 mL 1.3828 mL
80 mM 0.0415 mL 0.2074 mL 0.4148 mL 1.0371 mL
100 mM 0.0332 mL 0.1659 mL 0.3319 mL 0.8297 mL
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ITF 3756 Related Classifications

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:

ITF 37562247608-27-9ITF3756ITF-3756HDACNF-κBHistone deacetylasesNuclear factor-κBNuclear factor-kappaBPD-L1HT29HDAC6p65NF-κB pathwayTNF-αmurine colon carcinoma modelM2-like macrophagecolon cancer cellsHCT116Inhibitorinhibitorinhibit

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