JW480
Based on 1 Customer Validation
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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- Purity: 99.82%
- CAS No.: 1354359-53-7
- 화학식: C22H23NO2
- 분자량:333.42
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보관:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Biological Activity
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PKCδ |
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.
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Cell Line:human PC3 prostate cancer cells
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Concentration:1 μM
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Incubation Time:48 hr
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Result:Caused a significant reduction in invaded cells compared to control.
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Cell Line:human PC3 prostate cancer cells
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Concentration:1 μM
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Incubation Time:48 h (treatment), 4 d (culture)
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Result:Caused significant reductions in cell survival at days 1, 2, 3, and 4 compared to control.
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.
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Animal Model:C.B17 SCID mice (immune-deficient)[1]
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Dosage:80 mg/kg
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Administration:p.o.; daily; 33 days
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Result:Significantly reduced PC3 tumor xenograft growth compared to vehicle control.
Completely ablated KIAA1363 activity in explanted tumors.
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Animal Model:Mice[1]
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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)
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Administration:i.p.; single dose; p.o.; single dose
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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.
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Animal Model:Sprague Dawley (SD) (3.5 to 5 weeks old, FeCl3-induced common carotid artery thrombosis model)[3]
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Dosage:40 mg/kg
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Administration:i.v.; single dose over 5 minutes
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Result:Delayed the median time to vessel occlusion (defined as blood flow reaching 25% of baseline) to 14.8 minutes.
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Animal Model:Sprague Dawley (SD) (adult, ≥ 6 months old, tail bleeding assay model)[3]
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Dosage:3.5-10 mg/kg
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Administration:i.v.; single dose over 5 minutes
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Result:Increased median tail bleeding time to 30.0 minutes.
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Animal Model:Sprague Dawley (SD) (adult, > 6 months old)[3]
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Dosage:8-11 mg/kg
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Administration:i.v.; single dose
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Result:Produced a pronounced inhibition of convulxin-induced whole blood platelet aggregation, normalized to vehicle control set to 1.0.
Chemical Information
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CAS No. 1354359-53-7
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Appearance Solid
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분자량 333.42
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화학식 C22H23NO2
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Color White to off-white
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SMILES
O=C(NCCC1=CC2=C(C=CC=C2)C=C1)OC3=C(C(C)C)C=CC=C3
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
용액&용해도
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
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)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
순도&문서
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Data Sheet (283 KB)
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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)
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Handling Instructions (2659 KB)
References
[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]
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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