2. Epigenetics PI3K/Akt/mTOR Stem Cell/Wnt
  3. AMPK YAP
  4. HTH-02-006

HTH-02-006 is a NUAK2 inhibitor, with an IC50 value of 126 nM. HTH-02-006 inhibits NUAK2-mediated signaling by reducing phosphorylation of its substrate MYPT1 at S445 and downstream MLC. HTH-02-006 shows growth inhibitory efficacy in YAP-high cancer cells (HuCCT-1, SNU475). HTH-02-006 significantly suppresses YAP-induced hepatomegaly (reduced liver/body weight ratio) in TetO-YAP S127A transgenic mice and demonstrates significant anti-tumor efficacy in mice bearing HMVP2 prostate cancer allografts. HTH-02-006 can be used for the study of liver cancer and prostate cancer.

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HTH-02-006

HTH-02-006 Chemical Structure

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

HTH-02-006 Related Antibodies

Top Publications Citing Use of Products

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NUAK1 NUAK2 AMPK AMPK α1β1γ1 AMPK α2β1γ1 AMPK α1β2γ1 AMPK α2β2γ1 BRSK1 BRSK2 HUNK AMPKα

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YAP/TAZ YAP/TAZ-TEAD TEAD YAP1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

HTH-02-006 is a NUAK2 inhibitor, with an IC50 value of 126 nM. HTH-02-006 inhibits NUAK2-mediated signaling by reducing phosphorylation of its substrate MYPT1 at S445 and downstream MLC. HTH-02-006 shows growth inhibitory efficacy in YAP-high cancer cells (HuCCT-1, SNU475). HTH-02-006 significantly suppresses YAP-induced hepatomegaly (reduced liver/body weight ratio) in TetO-YAP S127A transgenic mice and demonstrates significant anti-tumor efficacy in mice bearing HMVP2 prostate cancer allografts. HTH-02-006 can be used for the study of liver cancer and prostate cancer[1][2].

IC50 & Target[1]

NUAK2

126 nM (IC50)

In Vitro

HTH-02-006 inhibits NUAK2 kinase activity with an IC50 of 126 nM in vitro, as measured by reduced [γ-32P]ATP incorporation into Sakamototide in a dose-dependent manner[1].
HTH-02-006 (0.5-16 μM, 120 h) reduces phosphorylated MYPT1 (S445) and phosphorylated MLC levels in SNU475 cells, inhibiting actomyosin cytoskeleton activation[1].
HTH-02-006 (0.5-16 μM, 120 h) exhibits higher growth inhibition efficacy in YAP-high liver cancer cells (HuCCT-1, SNU475) compared to YAP-low cells (HepG2, SNU398)[1].
HTH-02-006 (0.5-16 μM, 120 h) shows reduced ability to inhibit MYPT1 phosphorylation and cell growth in NUAK2 A236T/A236T knock-in HuCCT-1 cells (drug-resistant mutant) compared to wild-type HuCCT-1 cells[1].
HTH-02-006 (0.5-20 μM, 9 days) exhibits dose-dependent inhibitory effects on the growth of LAPC-4, 22RV1, and HMVP2 prostate cancer cell spheroids, with IC50 values of 4.65 μM, 5.22 μM, and 5.72 μM respectively[2].
HTH-02-006 (1-10 μM) prevents YAP activation in HMVP2 cells, and downregulates the protein expression of YAP target genes NUAK2 and c-MYC[2].
HTH-02-006 (1-20 μM) significantly reduces the invasion area of HMVP2 cell spheroids into Matrigel, slows wound closure, and completely blocks invasion[2].
HTH-02-006 (10 μM, 72-96 h, medium change every 48 h) reduces the proliferation rate of cancer cells by nearly 50% in 1 mm3 explants[2].

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

HTH-02-006 Related Antibodies
In Vivo

HTH-02-006 (10 mg/kg, i.p., twice daily, 14 days) significantly suppresses YAP-induced hepatomegaly (reduced liver/body weight ratio) in TetO-YAP S127A transgenic mice[1].
HTH-02-006 (10 mg/kg, i.p., twice daily, 20 days) significantly inhibits tumor growth in 6-week-old male FVB mice bearing subcutaneous HMVP2 prostate cancer cell spheroid allografts[2].

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

Animal Model: 8-week-old Nude mice were subcutaneously injected with 5 × 106 HuCCT-1 TetO-YAP S127A cells (mixed with 100 μl RPMI medium and 100 μl Matrigel) into the flanks[1]
Dosage: 10 mg/kg
Administration: i.p., twice daily, 14 days
Result: Suppressed YAP-induced hepatomegaly, as evidenced by reduced liver/body weight ratio.
Decreased the number of proliferating hepatocytes, as shown by reduced Ki67-positive cell count.
Dramatically reduced phosphorylation of MYPT1 at S445 in liver tissues.
Showed no significant changes in body weight.
Showed greater tumor regression with 176.2% TGI when combined with Osimertinib.
Animal Model: 6-week-old male FVB mice were subcutaneously inoculated with HMVP2 prostate cancer cell spheroids (derived from 2 × 105 HMVP2 cells per mouse)[2]
Dosage: 10 mg/kg
Administration: i.p., twice daily, 20 days
Result: Inhibited prostate cancer allograft growth.
Reduced tumor cell proliferation, as shown by a significant decrease in the Ki67-positive proliferation index in tumor tissues.
Downregulated NUAK2 protein expression in tumors.
Molecular Weight

588.44

Formula

C25H29IN6O3
Appearance

Solid

Color

Off-white to light yellow

SMILES

CCC(NC1=CC=CC(OC2=NC(NC3=CC=C(C=C3OC)N4CCN(CC4)C)=NC=C2I)=C1)=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 (169.94 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 1.6994 mL 8.4970 mL 16.9941 mL
5 mM 0.3399 mL 1.6994 mL 3.3988 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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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

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Volume (start)

V1

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C2

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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    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (4.25 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: 2.5 mg/mL (4.25 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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

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g

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μL

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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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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 1.6994 mL 8.4970 mL 16.9941 mL 42.4852 mL
5 mM 0.3399 mL 1.6994 mL 3.3988 mL 8.4970 mL
10 mM 0.1699 mL 0.8497 mL 1.6994 mL 4.2485 mL
15 mM 0.1133 mL 0.5665 mL 1.1329 mL 2.8323 mL
20 mM 0.0850 mL 0.4249 mL 0.8497 mL 2.1243 mL
25 mM 0.0680 mL 0.3399 mL 0.6798 mL 1.6994 mL
30 mM 0.0566 mL 0.2832 mL 0.5665 mL 1.4162 mL
40 mM 0.0425 mL 0.2124 mL 0.4249 mL 1.0621 mL
50 mM 0.0340 mL 0.1699 mL 0.3399 mL 0.8497 mL
60 mM 0.0283 mL 0.1416 mL 0.2832 mL 0.7081 mL
80 mM 0.0212 mL 0.1062 mL 0.2124 mL 0.5311 mL
100 mM 0.0170 mL 0.0850 mL 0.1699 mL 0.4249 mL
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HTH-02-006 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-02-006AMPKYAPAMP-activated protein kinaseYes-associated proteinHuCCT-1 cellhepatomegalytumorigenesisaantifibroticliver cancerprostate cancerNUAK2SNU475Inhibitorinhibitorinhibit

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