2. Epigenetics Stem Cell/Wnt JAK/STAT Signaling
  3. Histone Demethylase Histone Methyltransferase STAT
  4. JMJD1C-IN-1

JMJD1C-IN-1 is an orally active and selective inhibitor of JMJD1C (IC50 = 0.59 μM, Kd = 1.96 μM). JMJD1C-IN-1 inhibits the binding of JMJD1C to H3K9me2 peptide substrate in the HTRF assay (IC50 = 1.47 μM). JMJD1C-IN-1 disrupts intratumoral regulatory T (Treg) cell fitness by dual mechanisms: promoting H3K9me2 accumulation to downregulate PD1 expression and reducing STAT3 demethylation to enhance STAT3 activation. JMJD1C-IN-1 demonstrates dose-dependent antitumor efficacy in multiple mouse tumor models (MCA205 fibrosarcoma, B16-F10 melanoma, LLC lung cancer, Hepa1-6 hepatocellular carcinoma, CT26 colorectal cancer). JMJD1C-IN-1 can be used for the study of tumor immunotherapy by selectively targeting intratumoral Treg cells.

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

JMJD1C-IN-1

JMJD1C-IN-1 Chemical Structure

CAS No. : 861224-48-8

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

JMJD1C-IN-1 Related Antibodies

Top Publications Citing Use of Products

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STAT3 STAT5 STAT6 STAT1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

JMJD1C-IN-1 is an orally active and selective inhibitor of JMJD1C (IC50 = 0.59 μM, Kd = 1.96 μM). JMJD1C-IN-1 inhibits the binding of JMJD1C to H3K9me2 peptide substrate in the HTRF assay (IC50 = 1.47 μM). JMJD1C-IN-1 disrupts intratumoral regulatory T (Treg) cell fitness by dual mechanisms: promoting H3K9me2 accumulation to downregulate PD1 expression and reducing STAT3 demethylation to enhance STAT3 activation. JMJD1C-IN-1 demonstrates dose-dependent antitumor efficacy in multiple mouse tumor models (MCA205 fibrosarcoma, B16-F10 melanoma, LLC lung cancer, Hepa1-6 hepatocellular carcinoma, CT26 colorectal cancer). JMJD1C-IN-1 can be used for the study of tumor immunotherapy by selectively targeting intratumoral Treg cells[1].

IC50 & Target[1]

JMJD1C

0.59 μM (IC50)

JMJD1C

1.96 μM (Kd)

In Vitro

JMJD1C-IN-1 (Compound 193D7) inhibits the binding of JMJD1C to H3K9me2 peptide substrate in the HTRF assay (IC50 = 1.47 μM) and inhibits the H3K9me2 demethylase activity of JMJD1C in the in vitro demethylation assay (IC50 = 0.59 μM)[1].

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

JMJD1C-IN-1 Related Antibodies
In Vivo

JMJD1C-IN-1 (Compound 193D7) (10-25 mg/kg, i.p., once daily, 2 weeks or 25 mg/kg, p.o., once daily, 12 days) demonstrates dose-dependent anti-tumor efficacy in C57BL/6 mice bearing MCA205 fibrosarcoma, MCA205, B16, LLC and EL4 cells[1].

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

Animal Model: 2  ×  105 MCA205, B16, LLC and EL4 cells and 1 × 106 Hepa1-6 cells were subcutaneously implanted into the right flanks of 8-12-week-old Jmjd1cTreg WT and Jmjd1cTreg KO mice [1]
Dosage: 10, 25 mg/kg
Administration: i.p., once daily for 2 weeks or p.o. for 12 days
Result: Achieved tumor growth inhibition.
Showed no significant changes in body weight, serum alanine aminotransferase (ALT) and alkaline phosphatase (ALP) levels, and no histological abnormalities in colon, liver, lung, or kidney tissues of treated mice, indicating no toxicity
Reduced PD1 and NRP1 expression in intratumoral Treg cells and increased phosphorylation of STAT3 (pSTAT3) levels in tumor Treg.
Increased IFNγ production in intratumoral Treg cells and enhanced the number of tumor-infiltrating CD4+ and CD8+ effector T cells as well as their production of IFNγ and TNF.
Showed greater tumor regression with 176.2% TGI when combined with Osimertinib.
Failed to achieve tumor growth inhibition in Rag1 KO or Jmjd1cTreg KO mice .
Molecular Weight

317.36

Formula

C16H15NO4S
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

O=C(C(CC1CC(O)=O)=C2N(CCS2)C1=O)C3=CC=CC=C3
Shipping

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

DMSO : 10 mg/mL (31.51 mM; ultrasonic and warming and heat to 60°C; 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 3.1510 mL 15.7550 mL 31.5100 mL
5 mM 0.6302 mL 3.1510 mL 6.3020 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)

Mass
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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Volume (start)

V1

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C2

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V2

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: ≥ 1 mg/mL (3.15 mM); Clear solution

    This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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: ≥ 1 mg/mL (3.15 mM); Clear solution

    This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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:

Dosage

mg/kg

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(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
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: 99.99%

SDS (393 KB)

COA (255 KB) HNMR (280 KB) LCMS (91 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 3.1510 mL 15.7550 mL 31.5100 mL 78.7749 mL
5 mM 0.6302 mL 3.1510 mL 6.3020 mL 15.7550 mL
10 mM 0.3151 mL 1.5755 mL 3.1510 mL 7.8775 mL
15 mM 0.2101 mL 1.0503 mL 2.1007 mL 5.2517 mL
20 mM 0.1575 mL 0.7877 mL 1.5755 mL 3.9387 mL
25 mM 0.1260 mL 0.6302 mL 1.2604 mL 3.1510 mL
30 mM 0.1050 mL 0.5252 mL 1.0503 mL 2.6258 mL
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JMJD1C-IN-1 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:

JMJD1C-IN-1861224-48-8Histone DemethylaseHistone MethyltransferaseSTATJMJD1C InhibitorInhibitorinhibitorinhibit

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