2. Cytoskeleton Membrane Transporter/Ion Channel Apoptosis
  3. Myosin Ferlin Family Apoptosis
  4. HJ445A

HJ445A is an orally active myoferlin (MYOF) inhibitor with a Kd 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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HJ445A

HJ445A 構造式

CAS 番号 : 3032441-59-8

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 416 在庫あり
Solution
10 mM * 1 mL in DMSO USD 416 在庫あり
Solid
1 mg $150 在庫あり
5 mg $379 在庫あり
10 mg $569 在庫あり
25 mg $1139 在庫あり
50 mg $1709 在庫あり
100 mg $2564 在庫あり
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500 mg   お問い合わせ  

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HJ445A 関連抗体

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製品説明

HJ445A is an orally active myoferlin (MYOF) inhibitor with a Kd 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[1][2].

IC50 & Target[1]

Myoferlin

 

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]
体外実験

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 KD 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.

HJ445A 関連抗体

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 Cmax AUC0-t AUC0-inf T1/2 CL Vdss 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 %
体内実験

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.
分子量

445.52

分子式

C24H27N7O2
CAS 番号
Appearance

Solid

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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
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
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
×
Molecular Weight *

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

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 (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.

    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 (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.

    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.
純度とドキュメンテーション
参考文献

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 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
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HJ445A Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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:

HJ445A3032441-59-8MyosinFerlin FamilyApoptosismyoferlin (MYOF)-C2D domaingastric cancercell migrationpancreatic cancercell proliferationapoptosisMGC803MKN45colony formationvesicular traffickingInhibitorinhibitorinhibit

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製品名:
HJ445A
製品番号:
HY-163084
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