Cat. No.: HY-144707

AK-778-XXMU

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Based on 1 Customer Validation

AK-778-XXMU is a potent DNA binding inhibitor 2 (ID2) antagonist with a K_D of 129 nM. AK-778-XXMU can inhibit cell migration and invasion of glioma cell lines, induce apoptosis, and exhibits significant cancer-suppressing potency. AK-778-XXMU inhibits the ID2-KDR signaling axis, thereby down-regulating the downstream angiogenic factors (VEGFA) and invasion-related proteins (MMP2/9), and up-regulating the tumor suppressor factor (PTEN). AK-778-XXMU can be used for the study of glioma.

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

Purity: 99.96%
CAS No.: 1227045-76-2
Formula: C₂₂H₁₇ClN₂O₃
Molecular Weight:392.83

Storage:

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

AK-778-XXMU Chemical Structure

CAS No.: 1227045-76-2

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

MMP-9

MMP-2

All VEGFR Isoforms :

All MMP Isoforms :

In Vitro

AK-778-XXMU (24 h) shows cytotoxicity with an IC₅₀ values of 15.5, 18.7 and 21.3 μM against U87, HS683 and GL261 cells^[1].
AK-778-XXMU (0-50 μM, 0-24 h) effectively inhibits the migration and invasion abilities and induces apoptosis of U87 cells and GL261 cells^[1].
AK-778-XXMU (0-50 μM, 24 h) inhibits the ID2-KDR signaling axis, thereby down-regulating the downstream angiogenic factors (VEGFA) and invasion-related proteins (MMP2/9), and up-regulating the tumor suppressor factor (PTEN)^[1].

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

Cell Migration Assay ^[1]

Cell Line:

U87 cells and GL261 cells
Concentration:

0, 12.5 and 50 μM
Incubation Time:

0, 12 and 24 h
Result:

Inhibited the migration of GL261 and U87 cells in a concentration-dependent manner.

Cell Invasion Assay^[1]

Cell Line:

U87 cells and GL261 cells
Concentration:

0, 12.5 and 50 μM
Incubation Time:

24 h
Result:

Inhibited the invasion of GL261 and U87 cells in a concentration-dependent manner.

Apoptosis Analysis^[1]

Cell Line:

U87 cells and GL261 cells
Concentration:

0, 12.5 and 50 μM
Incubation Time:

24 h
Result:

Resulted in increased apoptosis.

Western Blot Analysis^[1]

Cell Line:

U87 cells and GL261 cells
Concentration:

0, 12.5, 25 and 50 μM
Incubation Time:

24 h
Result:

Downregulated the expressions of ID2, VEGFA, KDR (VEGFR2), MMP2 and MMP9, while the expression of the tumor suppressor gene PTEN was upregulated.

RT-PCR^[1]

Cell Line:

U87 cells and GL261 cells
Concentration:

0, 12.5, 25 and 50 μM
Incubation Time:

24 h
Result:

Significantly reduced the mRNA expression levels of ID2 and KDR.

In Vivo

AK-778-XXMU (2.5 mg/kg, i.p., every other day for 5 days) inhibits tumor growth in U87 glioma xenograft mice model^[1].

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

Animal Model:

U87 glioma cells xenograft model established in 8-week-old NCG mice^[1]
Dosage:

2.5 mg/kg
Administration:

Intraperitoneal injection (i.p.), twice daily for 5 days
Result:

Significantly slowed down the growth rate of tumors, and at the end of the experiment, the tumor inhibition rate (TGI) reached as high as 57.8%.
No obvious acute systemic toxicity and histopathological changes was observed, and it did not affect the body weight of the mice.
Significantly reduced the rate of Ki67-positive cells and microvessel density (MVD).

Chemical Information

CAS No. 1227045-76-2
Appearance Solid
Molecular Weight 392.83
Formula C₂₂H₁₇ClN₂O₃
Color Off-white to light yellow
SMILES

O=C(C1=CC=CC=N1)CC2(C(N(C3=C2C=CC=C3)CC4=CC=CC(Cl)=C4)=O)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 (254.56 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

2.5456 mL

12.7282 mL

25.4563 mL

5 mM

0.5091 mL

2.5456 mL

5.0913 mL

10 mM

0.2546 mL

1.2728 mL

2.5456 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.

Molarity Calculator

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

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Dilution Calculator

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 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)

References

[1]. Zhong G, et al. Discovery of novel ID2 antagonists from pharmacophore-based virtual screening as potential therapeutics for glioma. Bioorg Med Chem. 2021;49:116427. [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	2.5456 mL	12.7282 mL	25.4563 mL	63.6408 mL
	5 mM	0.5091 mL	2.5456 mL	5.0913 mL	12.7282 mL
	10 mM	0.2546 mL	1.2728 mL	2.5456 mL	6.3641 mL
	15 mM	0.1697 mL	0.8485 mL	1.6971 mL	4.2427 mL
	20 mM	0.1273 mL	0.6364 mL	1.2728 mL	3.1820 mL
	25 mM	0.1018 mL	0.5091 mL	1.0183 mL	2.5456 mL
	30 mM	0.0849 mL	0.4243 mL	0.8485 mL	2.1214 mL
	40 mM	0.0636 mL	0.3182 mL	0.6364 mL	1.5910 mL
	50 mM	0.0509 mL	0.2546 mL	0.5091 mL	1.2728 mL
	60 mM	0.0424 mL	0.2121 mL	0.4243 mL	1.0607 mL
	80 mM	0.0318 mL	0.1591 mL	0.3182 mL	0.7955 mL
	100 mM	0.0255 mL	0.1273 mL	0.2546 mL	0.6364 mL

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AK-778-XXMU

Apoptosis Compound Library

Kinase Inhibitor Library

Metabolism/Protease Compound Library

PI3K/Akt/mTOR Compound Library

Protein Tyrosine Kinase Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Glycolysis Compound Library

Cytoskeleton Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Glucose Metabolism Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Pain-Related Compound Library

Mitochondrial Protection Compound Library

Protease Inhibitor Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Cytokine Inhibitors Library

Cell Death Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Fibrosis Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

All VEGFR Isoforms

All MMP Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

AK-778-XXMU Related Classifications

HY-144707 Related Classifications