UNC0321
Based on 2 publication(s) in Google Scholar
UNC0321 is a potent and selective histone methyltransferase G9a inhibitor with a Ki of 63 pM and with assay-dependent IC50 values of 6-9 nM. UNC0321 also inhibits GLP with assay-dependent IC50 values of 15-23 nM. UNC0321 has anti-apoptotic activity and has potential application in diabetic vascular complications.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.91%
- No. CAS: 1238673-32-9
- Fòrmula: C27H45N7O3
- Peso molecular:515.69
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Apoptosis Compound Library
HY-L003
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Epigenetics Compound Library
HY-L005
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GPCR/G Protein Compound Library
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Histone Modification Research Compound Library
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Publications Citing Use of MedChemExpress (MCE) UNC0321
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Customer Validation & Images
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WB
Ver todos los productos específicos de isoformas Histone Methyltransferase
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Actividad biológica
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EHMT1/GLP/KMT1D 15-23 nM (IC50) |
G9a 63 pM (Ki) |
G9a 6-9 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| MDA-MB-231 | EC50 |
>40 μM
Compound: 3, UNC0321
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Cytotoxicity against human MDA-MB-231 cells assessed as cell viability after 48 hrs by MTT assay
Cytotoxicity against human MDA-MB-231 cells assessed as cell viability after 48 hrs by MTT assay
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[PMID: 21780790] |
| MDA-MB-231 | IC50 |
11 μM
Compound: 3, UNC0321
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Inhibition of G9a in human MDA-MB-231 cells assessed as reduction of H3K9me2 after 48 hrs by In-Cell Western assay
Inhibition of G9a in human MDA-MB-231 cells assessed as reduction of H3K9me2 after 48 hrs by In-Cell Western assay
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[PMID: 21780790] |
UNC0321 (Compound 29) inhibits the activity of G9a ECSD, G9a CLOT, GLP ECSD and GLP CLOT with IC50 values of 9 nM, 6 nM, 15 nM and 23 nM, respectively[1].
UNC0321 (Compound 3) reduces H3K9me2 levels in MDA-MB-231 cells with an IC50 value of 11 μM[2].
UNC0321 (200 pM; 48 h) significantly inhibits the expression of Rab4 in HUVEC[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HUVEC.
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Concentration:50 pM, 100 pM, 200 pM.
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Incubation Time:48 h.
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Result:Reduced glucose induced expression of Cleared Caspase3 and Bax.
Relieved the inhibition of glucose on Bcl-2, Caspase3, p-AKT, p-mTOR and p70 expression.
Promoted proliferation and inhibited apoptosis by inhibiting Rab4.
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Cell Line:HUVEC.
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Concentration:50 pM, 100 pM, 200 pM.
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Incubation Time:48 h.
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Result:Inhibited glucose induced apoptosis.
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Cell Line:HUVEC.
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Concentration:50 pM, 100 pM, 200 pM.
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Incubation Time:48 h.
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Result:Relieved the inhibition of glucose on HUVEC proliferation.
Chemical Information
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No. CAS 1238673-32-9
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Appearance Solid
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Peso molecular 515.69
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Fòrmula C27H45N7O3
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Color White to yellow
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SMILES
CN1CCC(NC2=C3C=C(OC)C(OCCOCCN(C)C)=CC3=NC(N4CCN(C)CCC4)=N2)CC1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Proc Natl Acad Sci U S A
2019 Feb 19;116(8):2961-2966. PMID: 30718431 -
Biomed Pharmacother
2020 Nov;131:110662. PMID: 32877824
UNC0321 purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2020 Nov;131:110662. [Abstract]
UNC0321 inhibits the apoptosis by targeting Rab4 in HUVEC. After the treatment (UNC0321, 200 pM) or transfection (Rab4 overexpression plasmid) for 48 h, Western Blot is performed to detect the expression of Bax, Bcl-2, Cleaved-Caspase3, Caspase3, p-AKT, AKT and Rab4. UNC0321 may play a role in promoting proliferation and anti-apoptosis by inhibiting Rab4/AKT/mTOR signaling pathway in HUVEC.
Solvente y solubilidad
DMSO : 100 mg/mL (193.91 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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: ≥ 2.08 mg/mL (4.03 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.03 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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.
Pureza y Documentación
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Ficha de datos (276 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Liu F, et al. Protein lysine methyltransferase G9a inhibitors: design, synthesis, and structure activity relationships of 2,4-diamino-7-aminoalkoxy-quinazolines. J Med Chem. 2010 Aug 12;53(15):5844-57. [Content Brief]
[2]. Liu F, et al. Optimization of cellular activity of G9a inhibitors 7-aminoalkoxy-quinazolines. J Med Chem. 2011 Sep 8;54(17):6139-50. [Content Brief]
[3]. Nie J. UNC0321 inhibits high glucose induced apoptosis in HUVEC by targeting Rab4. Biomed Pharmacother. 2020 Nov;131:110662. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.9391 mL | 9.6957 mL | 19.3915 mL | 48.4787 mL |
| 5 mM | 0.3878 mL | 1.9391 mL | 3.8783 mL | 9.6957 mL | |
| 10 mM | 0.1939 mL | 0.9696 mL | 1.9391 mL | 4.8479 mL | |
| 15 mM | 0.1293 mL | 0.6464 mL | 1.2928 mL | 3.2319 mL | |
| 20 mM | 0.0970 mL | 0.4848 mL | 0.9696 mL | 2.4239 mL | |
| 25 mM | 0.0776 mL | 0.3878 mL | 0.7757 mL | 1.9391 mL | |
| 30 mM | 0.0646 mL | 0.3232 mL | 0.6464 mL | 1.6160 mL | |
| 40 mM | 0.0485 mL | 0.2424 mL | 0.4848 mL | 1.2120 mL | |
| 50 mM | 0.0388 mL | 0.1939 mL | 0.3878 mL | 0.9696 mL | |
| 60 mM | 0.0323 mL | 0.1616 mL | 0.3232 mL | 0.8080 mL | |
| 80 mM | 0.0242 mL | 0.1212 mL | 0.2424 mL | 0.6060 mL | |
| 100 mM | 0.0194 mL | 0.0970 mL | 0.1939 mL | 0.4848 mL |
UNC0321 Related Classifications
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