2. PI3K/Akt/mTOR Protein Tyrosine Kinase/RTK JAK/STAT Signaling Cell Cycle/DNA Damage Stem Cell/Wnt Apoptosis
  3. MELK DYRK Pim mTOR CDK GSK-3 RIP kinase
  4. HTH-01-091 TFA

HTH-01-091 TFA is a potent and selective maternal embryonic leucine zipper kinase (MELK) inhibitor, with an IC50 of 10.5 nM. HTH-01-091 TFA also inhibits PIM1/2/3, RIPK2, DYRK3, smMLCK and CLK2. HTH-01-091 TFA can be uesd for breast cancer research.

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

HTH-01-091 TFA Chemical Structure

HTH-01-091 TFA Chemical Structure

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1 mg USD 383 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of HTH-01-091 TFA:

HTH-01-091 TFA Related Antibodies

Top Publications Citing Use of Products

View All DYRK Isoform Specific Products:

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DYRK1 DYRK2 DYRK3 DYRK4

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PIM1 PIM2 PIM3

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mTOR mTORC1 mTORC2

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

View All GSK-3 Isoform Specific Products:

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GSK-3 GSK-3α GSK-3β

View All RIP kinase Isoform Specific Products:

View All Isoforms
RIPK1 RIPK2 RIPK3

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

HTH-01-091 TFA is a potent and selective maternal embryonic leucine zipper kinase (MELK) inhibitor, with an IC50 of 10.5 nM. HTH-01-091 TFA also inhibits PIM1/2/3, RIPK2, DYRK3, smMLCK and CLK2. HTH-01-091 TFA can be uesd for breast cancer research[1].

IC50 & Target

IC50: 10.5 nM (MELK), 41.8 nM (DYRK3), 42.5 nM (RIPK2), 60.6 nM (PIM1), 108.6 nM (smMLCK), 632 nM (mTOR), 962 nM (PIK3CA), 1230 nM (CDK7), 1740 nM (GSK3A)[1]
In Vitro

HTH-01-091 (1 μM) TFA selectively inhibits 4% of the kinases over 90%[1].
HTH-01-091 (0-10 μM, 1 h) TFA is cell permeable and causes MELK degradation[1].
HTH-01-091 (0-10 μM, 3 day) TFA exhibits minor antiproliferative effects in breast cancer cells[1].

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

HTH-01-091 TFA Related Antibodies

Cell Proliferation Assay[1]

Cell Line: MDA-MB-468, BT-549, HCC70, ZR-75-1, MCF7, and T-47D cells
Concentration: 0, 0.001, 0.01, 0.1, 1.0, and 10 μM
Incubation Time: 3 day
Result: Showed antiproliferative activities in a panel of breast cancer cell lines, including MDA-MB-468, BT-549, HCC70, ZR-75-1, MCF7, and T-47D cells, with IC50 values of 4.00 μM, 6.16 μM, 8.80 μM, >10 μM, 8.75 μM, and 3.87 μM, respectively.

Western Blot Analysis[1]

Cell Line: MDA-MB-468 cells
Concentration: 0, 0.1, 1.0, and 10 μM
Incubation Time: 1 h
Result: Reduced MELK protein levels in MDA-MB-468 cells; Dose-dependently decreased MELK pull-down by streptavidin beads, demonstrating that the compound is cell permeable and binds to MELK in an ATP-competitive fashion. Had no effect on ERK1/2 pull-down, showing no binding affinity of HTH-01-091 to ERK1/2.
Molecular Weight

613.46

Formula

C28H29Cl2F3N4O4
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1N([C@H]2CC[C@H](CN(C)C)CC2)C3=C(CN1)C=NC4=CC=C(C5=CC(Cl)=C(O)C(Cl)=C5)C=C34.OC(C(F)(F)F)=O
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 (163.01 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 1.6301 mL 8.1505 mL 16.3010 mL
5 mM 0.3260 mL 1.6301 mL 3.2602 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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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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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: ≥ 2.5 mg/mL (4.08 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 (4.08 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:
%
DMSO +
% 
+
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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 1.6301 mL 8.1505 mL 16.3010 mL 40.7525 mL
5 mM 0.3260 mL 1.6301 mL 3.2602 mL 8.1505 mL
10 mM 0.1630 mL 0.8150 mL 1.6301 mL 4.0752 mL
15 mM 0.1087 mL 0.5434 mL 1.0867 mL 2.7168 mL
20 mM 0.0815 mL 0.4075 mL 0.8150 mL 2.0376 mL
25 mM 0.0652 mL 0.3260 mL 0.6520 mL 1.6301 mL
30 mM 0.0543 mL 0.2717 mL 0.5434 mL 1.3584 mL
40 mM 0.0408 mL 0.2038 mL 0.4075 mL 1.0188 mL
50 mM 0.0326 mL 0.1630 mL 0.3260 mL 0.8150 mL
60 mM 0.0272 mL 0.1358 mL 0.2717 mL 0.6792 mL
80 mM 0.0204 mL 0.1019 mL 0.2038 mL 0.5094 mL
100 mM 0.0163 mL 0.0815 mL 0.1630 mL 0.4075 mL
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HTH-01-091 TFA 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:

HTH-01-091MELKDYRKPimmTORCDKGSK-3RIP kinaseMaternal embryonic leucine zipper kinaseDual specificity tyrosine phosphorylation regulated kinaseDual specificity tyrosine regulated kinasePim kinasesMammalian target of RapamycinCyclin dependent kinaseGlycogen synthase kinase-3Glycogen synthase kinase 3Receptor-interacting protein kinasesRIPKMDA-MB-468BT-549HCC70ZR-75-1MCF7T-47D cellsbreast cancerGSK3AsmMLCKInhibitorinhibitorinhibit

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