NCGC00244536
Based on 2 publication(s) in Google Scholar
NCGC00244536 is a potent KDM4B inhibitor with an IC50 of 10 nM.
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- Pureté: 99.70%
- CAS No.: 2003260-55-5
- Formule: C25H22N2O2
- Masse moléculaire:382.45
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) NCGC00244536
More
Activité biologique
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KDM4 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| LNCaP | IC50 |
<1 μM
Compound: 72
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Antiproliferative activity against human LNCAP cells assessed as reduction in cell viability by MTT assay
Antiproliferative activity against human LNCAP cells assessed as reduction in cell viability by MTT assay
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[PMID: 26710088] |
| PC-3 | IC50 |
40 nM
Compound: 72
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Antiproliferative activity against human PC3 cells assessed as reduction in cell viability by MTT assay
Antiproliferative activity against human PC3 cells assessed as reduction in cell viability by MTT assay
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[PMID: 26710088] |
| Sf9 | IC50 |
10 nM
Compound: 72
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Inhibition of human N-terminal GST-tagged KDM4B (1 to 500 residues) expressed in baculovirus infected sf9 cells using H3K4me3 as substrate
Inhibition of human N-terminal GST-tagged KDM4B (1 to 500 residues) expressed in baculovirus infected sf9 cells using H3K4me3 as substrate
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[PMID: 26710088] |
| VCaP | IC50 |
<1 μM
Compound: 72
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Antiproliferative activity against human VCaP cells assessed as reduction in cell viability by MTT assay
Antiproliferative activity against human VCaP cells assessed as reduction in cell viability by MTT assay
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[PMID: 26710088] |
NCGC00244536 displays high selectivity for the fast-growing AR-negative PC3 cells (IC50=40 nM) and over 100-fold selectivity against the immortalized prostate epithelial cell lines PrEC1 and PrEC4. NCGC00244536 effectively inhibits AR-positive cell lines, including LNCaP and VCaP, with IC50s in the sub-micromolar range, and abolishes androgen-stimulated LNCaP cell growth. NCGC00244536 is also potent in inhibiting the growth of other cancer cell lines, including the breast cancer cell lines MDA-MB2 and MCF-7, with micromolar IC50s[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2003260-55-5
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Appearance Solid
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Masse moléculaire 382.45
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Formule C25H22N2O2
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Color Light yellow to green yellow
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SMILES
O=C(NCCCC1=CC=CC=C1)C2=CC=CC(C3=CC(O)=C4N=CC=CC4=C3)=C2
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Synonyms
KDM4B Inhibitor B3
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (2)
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Journal Impact Factor
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Most Recent
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Acta Pharmacol Sin
2022 Feb;43(2):457-469. PMID: 33850273 -
Clin Exp Med
Corin: a dual inhibitor for KDM1A/HDAC1, suppresses hepatocellular carcinoma by triggering cuproptosis. [Abstract]2025 Nov 25;26(1):33. PMID: 41286164
Solvant et solubilité
DMSO : 36.67 mg/mL (95.88 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.75 mg/mL (7.19 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.75 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 (27.5 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.
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.
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.
Protocole
LNCaP cells are treated with 0.1, 0.2, 1, 2.5, 5, 20 μM of NCGC00244536. Cell viability is measured using the MTT assay[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mouse: For xenograft animal model, PC3 cell suspension is injected into 4-6 weeks old severe combined immunodeficient (SCID) mice. When tumors become palpable, animals are randomly grouped for drug treatment. Alzet osmotic minipump containing NCGC00244536 (20 mg/kg)is subcutaneously inserted into each animal, which allowed continuous drug delivery to the tumor site for up to 5 days. Tumor volume is recorded every other days and calculated by using the ellipsoid formula[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (273 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6147 mL | 13.0736 mL | 26.1472 mL | 65.3680 mL |
| 5 mM | 0.5229 mL | 2.6147 mL | 5.2294 mL | 13.0736 mL | |
| 10 mM | 0.2615 mL | 1.3074 mL | 2.6147 mL | 6.5368 mL | |
| 15 mM | 0.1743 mL | 0.8716 mL | 1.7431 mL | 4.3579 mL | |
| 20 mM | 0.1307 mL | 0.6537 mL | 1.3074 mL | 3.2684 mL | |
| 25 mM | 0.1046 mL | 0.5229 mL | 1.0459 mL | 2.6147 mL | |
| 30 mM | 0.0872 mL | 0.4358 mL | 0.8716 mL | 2.1789 mL | |
| 40 mM | 0.0654 mL | 0.3268 mL | 0.6537 mL | 1.6342 mL | |
| 50 mM | 0.0523 mL | 0.2615 mL | 0.5229 mL | 1.3074 mL | |
| 60 mM | 0.0436 mL | 0.2179 mL | 0.4358 mL | 1.0895 mL | |
| 80 mM | 0.0327 mL | 0.1634 mL | 0.3268 mL | 0.8171 mL |
NCGC00244536 Related Classifications
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