2. Epigenetics Immunology/Inflammation
  3. Histone Methyltransferase CD44
  4. Gintemetostat

Gintemetostat (KTX-1001) is an orally active, highly specific NSD2/MMSET histone methyltransferase inhibitor with human NSD2 IC50 values ranging 0.460-2.17 nM and NSD2 SET domain IC50 of 2.32 nM and Kd values ranging 6.3-70.4 nM.Gintemetostat reduces H3K36me2 levels, impairs multiple myeloma cell adhesion and colony formation, enhances cytotoxicity, boosts T-cell activation, and sensitizes resistant multiple myeloma cells to other agents.Gintemetostat can be used for the research of multiple myeloma and relapsed and refractory multiple myeloma.

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

Gintemetostat

Gintemetostat Chemical Structure

CAS No. : 2604513-16-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
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Other Forms of Gintemetostat:

Gintemetostat Related Antibodies

Top Publications Citing Use of Products

View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms
EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 NSD3/WHSC1L1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Gintemetostat (KTX-1001) is an orally active, highly specific NSD2/MMSET histone methyltransferase inhibitor with human NSD2 IC50 values ranging 0.460-2.17 nM and NSD2 SET domain IC50 of 2.32 nM and Kd values ranging 6.3-70.4 nM[1][4].Gintemetostat reduces H3K36me2 levels, impairs multiple myeloma cell adhesion and colony formation, enhances cytotoxicity, boosts T-cell activation, and sensitizes resistant multiple myeloma cells to other agents[1][2][6].Gintemetostat can be used for the research of multiple myeloma and relapsed and refractory multiple myeloma[1][2][3][4][5][6].

In Vitro

Combination treatment with Gintemetostat (0.5-2.5 μM) and 5 nM Pomalidomide (HY-10984) synergistically reduces the viability of IMiD-resistant t (4;14) H929-POMR multiple myeloma cells by more than 33%[1].
Combination treatment with Gintemetostat (500 nM; 24 h) and 0.1 nM Mezigdomide (HY-129395) synergistically reduces the viability of IMiD-resistant t (4;14) H929-POMR multiple myeloma cells by more than 90%[1].
Gintemetostat (0.5 μM; 24 h) enhances Teclistamab (HY-P99392)-mediated lysis of t (4;14) XG26 multiple myeloma cells (resulting in a 52% cell lysis rate) and promotes the activation of early CD4+ and CD8+ T cells[1].
Combination treatment with Gintemetostat (1 μM; 24 h) and 0.1 μg/mL Talquetamab (HY-P99394) mildly enhances Talquetamab-mediated lysis of t (4;14) XG26 multiple myeloma cells, potentiates Talquetamab-induced lysis of non-t (4;14), high NSD2-expressing XG12 multiple myeloma cells, and induces mild early activation of CD4+ and CD8+ T cells[1].

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

Gintemetostat Related Antibodies

Cell Viability AssayWestern Blot AnalysisCell Proliferation AssayApoptosis AnalysisCell Cytotoxicity AssayCell Cycle AnalysisRT-PCRCell Autophagy AssayImmunofluorescenceCell Differentiation AssayCell Invasion AssayCell Migration Assay Real Time qPCRELISA Assay[3]

Cell Line: IMiD-resistant t(4;14) myeloma H929-POMR cells
Concentration: 0.5 μM、1 μM、2.5 μM
Incubation Time: /
Result: Combining with 5 nM Pomalidomide synergistically reduced the viability of IMiD-resistant t(4;14) myeloma H929-POMR cells.
The cell viability of 5 nM Pomalidomide alone was 84%, while the combined concentrations decreased to 57%, 38%, and 33%, respectively.
Molecular Weight

546.52

Formula

C25H26F4N8O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

FC(C=C(C(F)=C1)OC)=C1C2=NC=C(N3C[C@](N)(CCC3)[C@H](O)C(F)F)C(CN4C5=NC=NC(N)=C5N=C4)=C2
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 : 100 mg/mL (182.98 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 1.8298 mL 9.1488 mL 18.2976 mL
5 mM 0.3660 mL 1.8298 mL 3.6595 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.

  • Molarity Calculator

  • 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

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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 (4.57 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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+
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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

Purity: 99.81%

SDS (251 KB)

COA (261 KB) HNMR (288 KB) LCMS (94 KB)

Handling Instructions (2659 KB)
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 1.8298 mL 9.1488 mL 18.2976 mL 45.7440 mL
5 mM 0.3660 mL 1.8298 mL 3.6595 mL 9.1488 mL
10 mM 0.1830 mL 0.9149 mL 1.8298 mL 4.5744 mL
15 mM 0.1220 mL 0.6099 mL 1.2198 mL 3.0496 mL
20 mM 0.0915 mL 0.4574 mL 0.9149 mL 2.2872 mL
25 mM 0.0732 mL 0.3660 mL 0.7319 mL 1.8298 mL
30 mM 0.0610 mL 0.3050 mL 0.6099 mL 1.5248 mL
40 mM 0.0457 mL 0.2287 mL 0.4574 mL 1.1436 mL
50 mM 0.0366 mL 0.1830 mL 0.3660 mL 0.9149 mL
60 mM 0.0305 mL 0.1525 mL 0.3050 mL 0.7624 mL
80 mM 0.0229 mL 0.1144 mL 0.2287 mL 0.5718 mL
100 mM 0.0183 mL 0.0915 mL 0.1830 mL 0.4574 mL
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Gintemetostat 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:

Gintemetostat2604513-16-6KTX-1001KTX1001KTX 1001Histone MethyltransferaseCD44In (Lu)-related protein p80Pgp-1/Ly-24ECMRIIIHUTCH-1XG26 multiple myeloma cellsH3K36me2H929-POMR multiple myeloma cellsKMS11 multiple myeloma cellsmultiple myelomaNSD2/MMSET histone methyltransferaseXG12 multiple myeloma cellsT-cellrelapsed and refractory multiple myelomaNSD2 SET domainInhibitorinhibitorinhibit

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