2. Metabolic Enzyme/Protease Neuronal Signaling Membrane Transporter/Ion Channel Epigenetics TGF-beta/Smad
  3. Ser/Thr Protease Calcium Channel PKC
  4. JW480

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.

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

JW480

JW480 Chemical Structure

CAS No. : 1354359-53-7

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of JW480:

JW480 Related Antibodies

Top Publications Citing Use of Products

View All Calcium Channel Isoform Specific Products:

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N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

View All PKC Isoform Specific Products:

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PKC PKCα PKCβ PKCγ PKCδ PKCε PKCη PKCζ PKCθ PKCμ PKC-ι ℩ PKCι

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1][2][3].

IC50 & Target[3]

PKCδ

 

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 Expi293FTM cell lysates by 90% and 86%, respectively, and abolishes RE hydrolase activity across all subcellular fractions of mKIAA1363‑expressing Expi293FTM 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 PKCδT505 phosphorylation in human platelets, with no effect on PKCθT538 phosphorylation[3].

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

JW480 Related Antibodies

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.
Molecular Weight

333.42

Formula

C22H23NO2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

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

Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9992 mL 14.9961 mL 29.9922 mL
5 mM 0.5998 mL 2.9992 mL 5.9984 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 (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.

  • Molarity Calculator

  • Dilution Calculator

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

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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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C2

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Volume (final)

V2

In Vivo:

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    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.

    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.
  • 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:

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g

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(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 +
%
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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).

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

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.
Purity & Documentation
References

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 (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.

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 Related Classifications

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:

JW4801354359-53-7JW 480JW-480Ser/Thr ProteaseCalcium ChannelPKCSerine proteasesSerine endopeptidasesThreonine proteasesCa2+ channelsCa channelsProtein kinase Chepatic stellate cellsLX-2Expi293F? cellsKIAA1363DU145plateletsarterial thrombosisprostate cancer cellsPC3AADACL1Inhibitorinhibitorinhibit

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