Art. -Nr.: HY-156397

HTH-02-006

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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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Reinheit: 99.42%
Formel: C₂₅H₂₉IN₆O₃
Molecular Weight:588.44

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

HTH-02-006 Chemical Structure

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

NUAK2

126 nM (IC₅₀)

Alle AMPK Isoform-spezifische Produkte anzeigen :

Alle YAP Isoform-spezifische Produkte anzeigen :

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.

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.

Chemical Information

Appearance Solid
Molecular Weight 588.44
Formel C₂₅H₂₉IN₆O₃
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.6994 mL

8.4970 mL

16.9941 mL

5 mM

0.3399 mL

1.6994 mL

3.3988 mL

10 mM

0.1699 mL

0.8497 mL

1.6994 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

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:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Yuan WC, et al. NUAK2 is a critical YAP target in liver cancer. Nat Commun. 2018 Nov 16;9(1):4834. [Content Brief]

[2]. Fu W, et al. NUAK family kinase 2 is a novel therapeutic target for prostate cancer. Mol Carcinog. 2022 Mar;61(3):334-345. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

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Alle AMPK Isoform-spezifische Produkte anzeigen

Alle YAP Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

HTH-02-006 Related Classifications

HY-156397 Related Classifications