Art. -Nr.: HY-163084

HJ445A

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HJ445A is an orally active myoferlin (MYOF) inhibitor with a K_d value of 0.17 μM against human targets. HJ445A directly binds to the MYOF-C2D domain to stabilize the MYOF protein, thereby regulating vesicle trafficking, cell proliferation, colony formation, migration and apoptosis processes in cancer cells, and exhibits anti-tumor efficacy. HJ445A can be used in gastric cancer-related research.

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Reinheit: 98.02%
CAS. Nr.: 3032441-59-8
Formel: C₂₄H₂₇N₇O₂
Molecular Weight:445.52

Speicherung:

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

HJ445A Chemical Structure

CAS. Nr.: 3032441-59-8

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

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

Myoferlin

Alle Myosin Isoform-spezifische Produkte anzeigen :

MLCK

Cellular Effect

Cell Line	Type	Value	Description	References
AGS	IC₅₀	0.46 μM Compound: 2i; HJ445A	Antiproliferative activity against human AGS cells incubated for 48 hrs by SRB assay Antiproliferative activity against human AGS cells incubated for 48 hrs by SRB assay	[PMID: 38054798]
BGC-823	IC₅₀	0.29 μM Compound: 2i; HJ445A	Antiproliferative activity against human BGC-823 cells incubated for 48 hrs by SRB assay Antiproliferative activity against human BGC-823 cells incubated for 48 hrs by SRB assay	[PMID: 38054798]
BXPC-3	IC₅₀	0.13 μM Compound: 2i; HJ445A	Antiproliferative activity against human BXPC-3 cells incubated for 48 hrs by SRB assay Antiproliferative activity against human BXPC-3 cells incubated for 48 hrs by SRB assay	[PMID: 38054798]
CWR22R	IC₅₀	>10 μM Compound: 2i; HJ445A	Antiproliferative activity against human 22Rv1 cells incubated for 48 hrs by SRB assay Antiproliferative activity against human 22Rv1 cells incubated for 48 hrs by SRB assay	[PMID: 38054798]
DU-145	IC₅₀	>10 μM Compound: 2i; HJ445A	Antiproliferative activity against human DU-145 cells incubated for 48 hrs by SRB assay Antiproliferative activity against human DU-145 cells incubated for 48 hrs by SRB assay	[PMID: 38054798]
ES-2	IC₅₀	0.28 μM Compound: 2i; HJ445A	Antiproliferative activity against human ES2 cells incubated for 48 hrs by SRB assay Antiproliferative activity against human ES2 cells incubated for 48 hrs by SRB assay	[PMID: 38054798]
MGC-803	IC₅₀	0.16 μM Compound: 2i; HJ445A	Antiproliferative activity against human MGC-803 cells incubated for 48 hrs by SRB assay Antiproliferative activity against human MGC-803 cells incubated for 48 hrs by SRB assay	[PMID: 38054798]
MGC-803	IC₅₀	60 nM Compound: 2i; HJ445A	Antiinvasive activity against human MGC-803 cells incubated for 24 hrs by crystal violet staining based inverted microscopic analysis Antiinvasive activity against human MGC-803 cells incubated for 24 hrs by crystal violet staining based inverted microscopic analysis	[PMID: 38054798]
MKN-45	IC₅₀	0.14 μM Compound: 2i; HJ445A	Antiproliferative activity against human MKN-45 cells incubated for 48 hrs by SRB assay Antiproliferative activity against human MKN-45 cells incubated for 48 hrs by SRB assay	[PMID: 38054798]
SGC-7901	IC₅₀	0.44 μM Compound: 2i; HJ445A	Antiproliferative activity against human SGC-7901 cells incubated for 48 hrs by SRB assay Antiproliferative activity against human SGC-7901 cells incubated for 48 hrs by SRB assay	[PMID: 38054798]
SK-HEP1	IC₅₀	0.75 μM Compound: 2i; HJ445A	Antiproliferative activity against human SK-HEP1 cells incubated for 48 hrs by SRB assay Antiproliferative activity against human SK-HEP1 cells incubated for 48 hrs by SRB assay	[PMID: 38054798]

In Vitro

HJ445A slightly inhibits select CYP450 enzymes with micromolar IC₅₀ values in in vitro^[1].
HJ445A (48 h) potently inhibits the proliferation of MGC803 and MKN45 human gastric cancer cells with IC₅₀ values of 0.16 μM and 0.14 μM, respectively^[2].
HJ445A (50-100 μM; 1 h) directly binds to MYOF in MKN45 human gastric cancer cells^[2].
HJ445A (0.156-10 μM; association time 80 s, dissociation time 160 s) binds directly and reversibly to the purified MYOF-C2D domain with a high affinity K_D of 0.17 μM^[2].
HJ445A (50-100 nM; 10 days) represses colony formation of MKN45 human gastric cancer cells in a concentration-dependent manner at 50 nM and 100 nM, which correlates with downregulation of p-AKT^[2].
HJ445A (62.5-250 nM; 24 h) inhibits migration of MGC803 human gastric cancer cells^[2].
HJ445A (100-400 nM) reverses the EMT process in MKN45 human gastric cancer cells in vitro in a concentration-dependent manner, as shown by upregulated E-cadherin and downregulated N-cadherin and Vimentin^[2].
HJ445A (0.1-0.8 μM; 48 h) induces apoptosis of MKN45 human gastric cancer cells in a dose-dependent manner^[2].
HJ445A weakly inhibits major human CYP450 isozymes, with IC₅₀ values of 14.7 μM for CYP 2C9, 18.8 μM for CYP 2C19, 35.1 μM for CYP 3A4, and >50.0 μM for CYP 1A2 and CYP 2D6^[2].

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

Cell Proliferation Assay^[2]

Cell Line:

human gastric cancer cell line MKN45
Concentration:

50 nM, 100 nM
Incubation Time:

10 days
Result:

Inhibited colony formation of MKN45 cells in a concentration-dependent manner, with significant reduction at 50 nM and 100 nM.
Downregulated phosphorylated AKT (p-AKT) levels in a concentration-dependent manner.

Cell Migration Assay ^[2]

Cell Line:

human gastric cancer cell line MGC803
Concentration:

62.5 nM, 125 nM, 250 nM
Incubation Time:

24 h
Result:

Inhibited migration of MGC803 cells in a concentration-dependent manner.

Apoptosis Analysis^[2]

Cell Line:

human gastric cancer cell line MKN45
Concentration:

0.1 μM, 0.2 μM, 0.4 μM, 0.8 μM
Incubation Time:

48 h
Result:

Induced apoptosis of MKN45 cells in a dose-dependent manner, with apoptosis rates of 3.4%, 5.7%, 50.2%, and 54.0% at 0.1, 0.2, 0.4, and 0.8 μM, respectively.

Parmacokinetics

Species	Dose	Route	C_max	AUC_0-t	AUC_0-inf	T_1/2	CL	V_dss	MRT	F
Mice^[2]	1 mg/kg	i.v.	1907 ng/mL	751 ng·h/mL	762 ng·h/mL	13.2 min	22.0 mL/min/kg	377 mL/kg	17.2 min	/
Mice^[2]	10 mg/kg	p.o.	5821 ng/mL	4923 ng·h/mL	4942 ng·h/mL	38.4 min	/	/	40.3 min	65.5 %

In Vivo

HJ445A (15-30 mg/kg; i.p.; daily) exhibits dose-dependent antitumor efficacy in MKN45 gastric cancer xenografts with no observed toxicity^[2].

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

Animal Model:

BALB/c nude (male, 6-8 weeks old)^[2]
Dosage:

15 mg/kg; 30 mg/kg
Administration:

i.p.; daily
Result:

Achieved a tumor growth inhibition (TGI) of 55.1%.
Achieved a TGI of 68.5%.
Showed no significant difference in mouse body weight compared with the control group.
Caused no visible tissue damage in the lung, liver, heart, kidney, or spleen at 30 mg/kg/day.

Chemical Information

CAS. Nr. 3032441-59-8
Appearance Solid
Molecular Weight 445.52
Formel C₂₄H₂₇N₇O₂
Color White to off-white
SMILES

CCC1=NN(C2=CC=CC(C(NCCCCN3N=CC=N3)=O)=C2)C(C4=CC=C(C=C4)OC)=N1
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 (224.46 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

2.2446 mL

11.2228 mL

22.4457 mL

5 mM

0.4489 mL

2.2446 mL

4.4891 mL

10 mM

0.2245 mL

1.1223 mL

2.2446 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 40% PEG300 5% Tween-80 45% Saline

Solubility: 2.5 mg/mL (5.61 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 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (5.61 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 3

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

Solubility: 2.5 mg/mL (5.61 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 (278 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]. Gullo C, et al. Focal adhesion assembly and cell migration require myoferlin in PDAC cell lines. Sci Rep. 2025 Nov 28;15(1):42797. [Content Brief]

[2]. Gu H, et al. Discovery of a Highly Potent and Selective MYOF Inhibitor with Improved Water Solubility for the Treatment of Gastric Cancer. J Med Chem. 2023 Dec 28;66(24):16917-16938. [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	2.2446 mL	11.2228 mL	22.4457 mL	56.1142 mL
	5 mM	0.4489 mL	2.2446 mL	4.4891 mL	11.2228 mL
	10 mM	0.2245 mL	1.1223 mL	2.2446 mL	5.6114 mL
	15 mM	0.1496 mL	0.7482 mL	1.4964 mL	3.7409 mL
	20 mM	0.1122 mL	0.5611 mL	1.1223 mL	2.8057 mL
	25 mM	0.0898 mL	0.4489 mL	0.8978 mL	2.2446 mL
	30 mM	0.0748 mL	0.3741 mL	0.7482 mL	1.8705 mL
	40 mM	0.0561 mL	0.2806 mL	0.5611 mL	1.4029 mL
	50 mM	0.0449 mL	0.2245 mL	0.4489 mL	1.1223 mL
	60 mM	0.0374 mL	0.1870 mL	0.3741 mL	0.9352 mL
	80 mM	0.0281 mL	0.1403 mL	0.2806 mL	0.7014 mL
	100 mM	0.0224 mL	0.1122 mL	0.2245 mL	0.5611 mL

Keywords

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HJ445A

MCE Bioactive Compound Library

Alle Myosin Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

HJ445A Related Classifications

HY-163084 Related Classifications