2. Epigenetics
  3. Histone Demethylase
  4. TK-129

TK-129 is an orally active, low-toxicity, potent KDM5B inhibitor (with high affinity; IC50=44 nM). TK-129 exerts cardioprotective effects by inhibiting KDM5B and blocking the KDM5B-associated Wnt pathway. TK-129 reduces ang II-induced activation of cardiac fibroblasts in vitro and reduces isoprenaline-induced myocardial remodelling and fibrosis in vivo. TK-129 can be used in studies of cardiovascular disease.

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TK-129 Chemical Structure

TK-129 Chemical Structure

CAS No. : 3031476-73-7

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Based on 1 publication(s) in Google Scholar

TK-129 Related Antibodies

Top Publications Citing Use of Products

View All Histone Demethylase Isoform Specific Products:

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KDM1/LSD1 KDM2 KDM3 KDM4 KDM5 KDM6

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Description

TK-129 is an orally active, low-toxicity, potent KDM5B inhibitor (with high affinity; IC50=44 nM). TK-129 exerts cardioprotective effects by inhibiting KDM5B and blocking the KDM5B-associated Wnt pathway. TK-129 reduces ang II-induced activation of cardiac fibroblasts in vitro and reduces isoprenaline-induced myocardial remodelling and fibrosis in vivo. TK-129 can be used in studies of cardiovascular disease[1].

IC50 & Target[1]

KDM5

44 nM (IC50)

In Vitro

TK-129 mediates inhibition of KDM5B activity significantly reduces the activation, migration, and proliferation of myofibroblasts induced by Ang II in vitro[1].
TK-129 (10 μM; 48 h) shows low cytotoxicity in NRCFs and NRCMs[1].
TK-129 (0.1, 0.2, 0.3, 0.4, 0.5 μM; 48 h) can engage toand inhibit KDM5B activity in NRCFs[1].

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

TK-129 Related Antibodies

Cell Cytotoxicity Assay[1]

Cell Line: NRCFs and NRCMs
Concentration: 10 μM
Incubation Time: 48 h
Result: Exhibited the cell survival rates were almost more than 90%.

Western Blot Analysis[1]

Cell Line: NRCFs
Concentration: 0.1, 0.2, 0.3, 0.4, 0.5 μM
Incubation Time: 48 h
Result: Increased the expression level of KDM5B substrate H3K4me3 protein in a concentration-dependent manner.
In Vivo

TK-129 (2 g/kg; p.o.; single) shows good bio-safety in mice[1].
TK-129 (50 mg/kg; p.o.; twice daily for 24 days) effectively reduces isoproterenol-induced pathological myocardial remodeling in vivo[1].
TK-129 (2 or 10 mg/kg; i.v. or p.o.; single) demonstrates favorable PK properties in vivo[1].

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

Animal Model: Wild C57BL/6 mice (8 to 10-week-old; half male and half female)[1].
Dosage: 2 g/kg
Administration: Oral gavage, single.
Result: Exhibited all mice in the acute toxicity group survived and gained weight normally, after 2 weeks.
Animal Model: C57BL/6 mice (isoproterenol (ISO)-induced)[1].
Dosage: 50 mg/kg
Administration: Oral gavage, twice daily for 24 days.
Result: Alleviated myocardial remodeling induced by ISO in vivo.
Animal Model: Male SD Rats (223.5-265.1 g)[1].
Dosage: 2 mg/kg (for i.v.); 10 mg/kg (for p.o.).
Administration: Intravenous injection or oral gavage; single.
Result: 1.19 Pharmacokinetic Parameters of TK-129 in Male SD Rats[1].
PO (10 mg/kg) IV (2 mg/kg)
CL (L/h/kg) 9.9 4.2
Vss (L/kg) 33.4 2.7
T1/2 (h) 2.4 0.4
Tmax (h) 0.4 -
Cmax (ng/mL) 709.7 1229.1
AUC0-24 (ng/mL•h) 1038.2 479.6
F (%) 42.37 -
Molecular Weight

305.38

Formula

C15H23N5O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N[C@H]1CN(C(C2=NNC(C(C)C)=C2)=O)CC1)NC3CC3
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 : 100 mg/mL (327.46 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 3.2746 mL 16.3730 mL 32.7461 mL
5 mM 0.6549 mL 3.2746 mL 6.5492 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
=
Concentration
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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)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

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: ≥ 2.5 mg/mL (8.19 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 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: ≥ 2.5 mg/mL (8.19 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:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(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
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 3.2746 mL 16.3730 mL 32.7461 mL 81.8652 mL
5 mM 0.6549 mL 3.2746 mL 6.5492 mL 16.3730 mL
10 mM 0.3275 mL 1.6373 mL 3.2746 mL 8.1865 mL
15 mM 0.2183 mL 1.0915 mL 2.1831 mL 5.4577 mL
20 mM 0.1637 mL 0.8187 mL 1.6373 mL 4.0933 mL
25 mM 0.1310 mL 0.6549 mL 1.3098 mL 3.2746 mL
30 mM 0.1092 mL 0.5458 mL 1.0915 mL 2.7288 mL
40 mM 0.0819 mL 0.4093 mL 0.8187 mL 2.0466 mL
50 mM 0.0655 mL 0.3275 mL 0.6549 mL 1.6373 mL
60 mM 0.0546 mL 0.2729 mL 0.5458 mL 1.3644 mL
80 mM 0.0409 mL 0.2047 mL 0.4093 mL 1.0233 mL
100 mM 0.0327 mL 0.1637 mL 0.3275 mL 0.8187 mL
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TK-129 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:

TK-1293031476-73-7TK129TK 129Histone Demethylasecardiovascular diseasewntcardiac fibroblastsmyocardial remodelingmyocardial fibrosisNRCFsNRCMsInhibitorinhibitorinhibit

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