Art. -Nr.: HY-107582

JW480

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JW480 is a selective KIAA1363/AADACL1 inhibitor with oral activity, featuring IC₅₀ values of 12 nM against human KIAA1363, 20 nM against mouse KIAA1363. JW480 blocks lipid deacetylase activity to restrain HAG metabolism and lowers retinyl ester hydrolase function in hepatic stellate cells. JW480 reduces MAGE lipid levels and inhibits migration, invasion, survival and tumor growth of prostate cancer cells. JW480 lowers PKCδ phosphorylation, facilitates HAGP accumulation, diminishes platelet aggregation, dense granule secretion and Ca²⁺ flux, delays arterial thrombosis and prolongs tail bleeding time in rats. JW480 can be used for the study of prostate cancer and thrombosis.

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Reinheit: 99.82%
CAS. Nr.: 1354359-53-7
Formel: C₂₂H₂₃NO₂
Molecular Weight:333.42

Speicherung:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

JW480 Chemical Structure

CAS. Nr.: 1354359-53-7

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

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^[3]

PKCδ

Alle Calcium Channel Isoform-spezifische Produkte anzeigen :

Alle PKC Isoform-spezifische Produkte anzeigen :

In Vitro

JW480 (0.001-10 μM) potently and selectively inhibits KIAA1363 with an IC₅₀ of 0.02 μM in mouse brain membrane proteomes and an in situ IC₅₀ of 0.006 μM in living PC3 cells, with sustained inhibition^[1].
JW480 (0.001-50 μM) potently and selectively inhibits KIAA1363 in PC3 prostate cancer cell proteomes in vitro with an IC₅₀ of 0.012 μM^[1].
JW480 (1 μM; 48 hr) selectively and exclusively inhibits KIAA1363 in situ–treated PC3 prostate cancer cells. It fully abolishes KIAA1363‑dependent 2‑acetyl MAGE hydrolysis and markedly reduces C16:0, C18:0, and C18:1 MAGE lipid levels in both PC3 and DU144 prostate cancer cells^[1].
JW480 (1 μM; 48 hr) impairs cell migration and invasion in PC3 prostate cancer cells treated in situ^[1].
JW480 (1 μM; 48 hr) impairs cell survival in serum-free media over 4 days in PC3 prostate cancer cells treated in situ^[1].
JW480 (10 μM, 1 h) markedly suppresses the in vitro retinyl ester (RE) hydrolase activity of recombinant mouse and human KIAA1363 in Expi293F^TM cell lysates by 90% and 86%, respectively, and abolishes RE hydrolase activity across all subcellular fractions of mKIAA1363‑expressing Expi293F^TM cells.^[2].
JW480 (10 μM; 1 h) reduces in vitro RE hydrolase activity by 20% in whole mouse liver lysates and by 60% in primary mouse HSC lysates, with no effect on primary mouse hepatocyte lysates^[2].
JW480 (10 μM; 1 h) potently inhibits in vitro RE hydrolase activity, reducing activity by 80% in human LX-2 HSC lysates and by 92% in primary human HSC lysates^[2].
JW480 (10 μM, 8 h) significantly suppresses RE degradation in HSCs, blunting RP breakdown in primary mouse HSCs, blocking RE degradation entirely in human LX‑2 cells, and lifting RP levels by 4‑fold in primary human HSCs.^[2].
JW480 elevates HAGP levels in collagen‑stimulated human platelets, inhibits collagen‑induced platelet aggregation (rescued by ADP), and reduces dense granule ATP secretion by 45% in washed human platelets^[3].
JW480 (2-10 μM) dose-dependently inhibits collagen-induced PKCδ^T505 phosphorylation in human platelets, with no effect on PKCθ^T538 phosphorylation^[3].

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

Cell Invasion Assay^[1]

Cell Line:

human PC3 prostate cancer cells
Concentration:

1 μM
Incubation Time:

48 hr
Result:

Caused a significant reduction in invaded cells compared to control.

Cell Viability Assay^[1]

Cell Line:

human PC3 prostate cancer cells
Concentration:

1 μM
Incubation Time:

48 h (treatment), 4 d (culture)
Result:

Caused significant reductions in cell survival at days 1, 2, 3, and 4 compared to control.

In Vivo

JW480 (80 mg/kg; p.o.; daily; 33 days) significantly impairs PC3 prostate cancer xenograft growth in SCID mice and completely ablates KIAA1363 activity in explanted tumors^[1].
JW480 (1-80 mg/kg; i.p.; single dose; 5-80 mg/kg; p.o.; single dose) potently and selectively inhibits brain KIAA1363 in mice via both intraperitoneal and oral routes^[1].
JW480 (40 mg/kg; i.v.; single dose over 5 minutes) administered to 3.5 to 5 week-old Sprague Dawley rats significantly delays median time to FeCl₃-induced carotid artery occlusion to 14.8 minutes^[3].
JW480 (3.5-10 mg/kg; i.v.; single dose over 5 minutes) administered to adult (≥6 months old) Sprague Dawley rats significantly increases median tail bleeding time to 30.0 minutes^[3].
JW480 (8-11 mg/kg; i.v.; single dose) administered to adult (>6 months old) Sprague Dawley rats significantly inhibits convulxin-induced circulating platelet aggregation^[3].

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

Animal Model:

C.B17 SCID mice (immune-deficient)^[1]
Dosage:

80 mg/kg
Administration:

p.o.; daily; 33 days
Result:

Significantly reduced PC3 tumor xenograft growth compared to vehicle control.
Completely ablated KIAA1363 activity in explanted tumors.

Animal Model:

Mice^[1]
Dosage:

1-80 mg/kg (i.p., single dose); 5-80 mg/kg (p.o., single dose); 20 mg/kg (p.o., single dose for time-course analysis)
Administration:

i.p.; single dose; p.o.; single dose
Result:

Achieved complete inhibition of brain KIAA1363 at 5 mg/kg (i.p.) and 20 mg/kg (p.o.) 4 hours post-administration.
Maintained inhibition of brain KIAA1363 for up to 24 hours following a single 20 mg/kg oral dose.
Showed excellent selectivity for KIAA1363 in brain proteomes, with only carboxylesterase ES1 (likely from blood contamination) identified as an off-target.

Animal Model:

Sprague Dawley (SD) (3.5 to 5 weeks old, FeCl₃-induced common carotid artery thrombosis model)^[3]
Dosage:

40 mg/kg
Administration:

i.v.; single dose over 5 minutes
Result:

Delayed the median time to vessel occlusion (defined as blood flow reaching 25% of baseline) to 14.8 minutes.

Animal Model:

Sprague Dawley (SD) (adult, ≥ 6 months old, tail bleeding assay model)^[3]
Dosage:

3.5-10 mg/kg
Administration:

i.v.; single dose over 5 minutes
Result:

Increased median tail bleeding time to 30.0 minutes.

Animal Model:

Sprague Dawley (SD) (adult, > 6 months old)^[3]
Dosage:

8-11 mg/kg
Administration:

i.v.; single dose
Result:

Produced a pronounced inhibition of convulxin-induced whole blood platelet aggregation, normalized to vehicle control set to 1.0.

Chemical Information

CAS. Nr. 1354359-53-7
Appearance Solid
Molecular Weight 333.42
Formel C₂₂H₂₃NO₂
Color White to off-white
SMILES

O=C(NCCC1=CC2=C(C=CC=C2)C=C1)OC3=C(C(C)C)C=CC=C3
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (299.92 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

2.9992 mL

14.9961 mL

29.9922 mL

5 mM

0.5998 mL

2.9992 mL

5.9984 mL

10 mM

0.2999 mL

1.4996 mL

2.9992 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 (protect from light). 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 (7.50 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

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 (7.50 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). 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 (283 KB)
SDS (624 KB)
- English - EN (624 KB)
- Français - FR (624 KB)
- Deutsch - DE (624 KB)
- Norwegian - NO (624 KB)
- Español - ES (624 KB)
- Swedish - SV (624 KB)
- Italian - IT (624 KB)
- Korean - KR (624 KB)
- Portuguese - PT (624 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]. Chang JW, et al. A potent and selective inhibitor of KIAA1363/AADACL1 that impairs prostate cancer pathogenesis. Chem Biol. 2011;18(4):476-484. [Content Brief]

[2]. Wagner C, et al. KIAA1363 affects retinyl ester turnover in cultured murine and human hepatic stellate cells. J Lipid Res. 2022;63(3):100173. [Content Brief]

[3]. Holly SP, et al. Ether lipid metabolism by AADACL1 regulates platelet function and thrombosis. Blood Adv. 2019;3(22):3818-3828. [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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.9992 mL	14.9961 mL	29.9922 mL	74.9805 mL
	5 mM	0.5998 mL	2.9992 mL	5.9984 mL	14.9961 mL
	10 mM	0.2999 mL	1.4996 mL	2.9992 mL	7.4981 mL
	15 mM	0.1999 mL	0.9997 mL	1.9995 mL	4.9987 mL
	20 mM	0.1500 mL	0.7498 mL	1.4996 mL	3.7490 mL
	25 mM	0.1200 mL	0.5998 mL	1.1997 mL	2.9992 mL
	30 mM	0.1000 mL	0.4999 mL	0.9997 mL	2.4994 mL
	40 mM	0.0750 mL	0.3749 mL	0.7498 mL	1.8745 mL
	50 mM	0.0600 mL	0.2999 mL	0.5998 mL	1.4996 mL
	60 mM	0.0500 mL	0.2499 mL	0.4999 mL	1.2497 mL
	80 mM	0.0375 mL	0.1875 mL	0.3749 mL	0.9373 mL
	100 mM	0.0300 mL	0.1500 mL	0.2999 mL	0.7498 mL

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JW480

Epigenetics Compound Library

Kinase Inhibitor Library

Membrane Transporter/Ion Channel Compound Library

Metabolism/Protease Compound Library

Neuronal Signaling Compound Library

TGF-beta/Smad Compound Library

Anti-Cancer Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Cytoskeleton Compound Library

Orally Active Compound Library

Neuroprotective Compound Library

Calcium Channel Blocker Library

Anti-Prostate Cancer Compound Library

Cancer Stem Cells Compound Library

Coagulation and Anti-coagulation Compound Library

Antihypertensive Compound Library

Protease Inhibitor Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Ion Channel Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Alle Calcium Channel Isoform-spezifische Produkte anzeigen

Alle PKC Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

JW480 Related Classifications

HY-107582 Related Classifications