Art. -Nr.: HY-10930

UNC0321

2 Cited Publications

Kundenbewertung

Based on 2 publication(s) in Google Scholar

UNC0321 is a potent and selective histone methyltransferase G9a inhibitor with a K_i 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.

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Reinheit: 99.91%
CAS. Nr.: 1238673-32-9
Formel: C₂₇H₄₅N₇O₃
Molecular Weight:515.69

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

UNC0321 Chemical Structure

CAS. Nr.: 1238673-32-9

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (2)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

EHMT1/GLP/KMT1D

15-23 nM (IC₅₀)

G9a

63 pM (Ki)

G9a

6-9 nM (IC₅₀)

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
MDA-MB-231	EC₅₀	>40 μM Compound: 3, UNC0321	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	[PMID: 21780790]
MDA-MB-231	IC₅₀	11 μM Compound: 3, UNC0321	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	[PMID: 21780790]

In Vitro

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.

Western Blot Analysis^[3]

Cell Line:

HUVEC.
Concentration:

50 pM, 100 pM, 200 pM.
Incubation Time:

48 h.
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.

Apoptosis Analysis^[3]

Cell Line:

HUVEC.
Concentration:

50 pM, 100 pM, 200 pM.
Incubation Time:

48 h.
Result:

Inhibited glucose induced apoptosis.

Cell Proliferation Assay^[3]

Cell Line:

HUVEC.
Concentration:

50 pM, 100 pM, 200 pM.
Incubation Time:

48 h.
Result:

Relieved the inhibition of glucose on HUVEC proliferation.

Chemical Information

CAS. Nr. 1238673-32-9
Appearance Solid
Molecular Weight 515.69
Formel C₂₇H₄₅N₇O₃
Color White to yellow
SMILES

CN1CCC(NC2=C3C=C(OC)C(OCCOCCN(C)C)=CC3=NC(N4CCN(C)CCC4)=N2)CC1
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Proc Natl Acad Sci U S A

MGMT-activated DUB3 stabilizes MCL1 and drives chemoresistance in ovarian cancer. [Abstract]

2019 Feb 19;116(8):2961-2966. PMID: 30718431
Biomed Pharmacother

UNC0321 inhibits high glucose induced apoptosis in HUVEC by targeting Rab4. [Abstract]

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.

Lösungsmittel & Löslichkeit

In Vitro:

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)

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

1.9391 mL

9.6957 mL

19.3915 mL

5 mM

0.3878 mL

1.9391 mL

3.8783 mL

10 mM

0.1939 mL

0.9696 mL

1.9391 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, 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.

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 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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (4.03 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 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 (276 KB)
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)
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]. 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]

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

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
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

2 Cited Publications

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UNC0321

Apoptosis Compound Library

Epigenetics Compound Library

GPCR/G Protein Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Reprogramming Compound Library

Anti-diabetic Compound Library

Anti-Blood Cancer Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Cell Death Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

Epigenetics Compound Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Methylation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) UNC0321

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

UNC0321

Apoptosis Compound Library

Epigenetics Compound Library

GPCR/G Protein Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Reprogramming Compound Library

Anti-diabetic Compound Library

Anti-Blood Cancer Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Cell Death Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

Epigenetics Compound Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Methylation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) UNC0321

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

UNC0321 Related Classifications

HY-10930 Related Classifications