Cat. No.: HY-13807

UNC0646

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UNC0646 is a potent and selective histone methyltransferase G9a inhibitor with an IC₅₀ of 6 nM. UNC0646 is also a potent GLP inhibitor (IC₅₀ <15 nM) and highly selective for G9a/GLP over SETD7, SUV39H2, SETD8 and PRMT3. UNC0646 reduces H3K9me2 levels in MDA-MB-231 cells with an IC₅₀ of 26 nM.

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Pureté: 99.38%
CAS No.: 1320288-17-2
Formule: C₃₆H₅₉N₇O₂
Masse moléculaire:621.90

Stockage:

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

UNC0646 Chemical Structure

CAS No.: 1320288-17-2

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Fluorescent Dye

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

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (1)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[1]

G9a

6 nM (IC₅₀)

GLP

<15 nM (IC₅₀)

Voir tous les produits spécifiques à Isoform Histone Methyltransferase :

Cellular Effect

Cell Line	Type	Value	Description	References
CWR22R	EC₅₀	7.2 μM Compound: 6, UNC0646	Cytotoxicity against human 22Rv1 cells assessed as cell viability after 48 hrs by MTT assay Cytotoxicity against human 22Rv1 cells assessed as cell viability after 48 hrs by MTT assay	[PMID: 21780790]
CWR22R	IC₅₀	0.014 μM Compound: 6, UNC0646	Inhibition of G9a in human 22Rv1 cells assessed as reduction of H3K9me2 after 48 hrs by In-Cell Western assay Inhibition of G9a in human 22Rv1 cells assessed as reduction of H3K9me2 after 48 hrs by In-Cell Western assay	[PMID: 21780790]
HCT-116	EC₅₀	12 μM Compound: 6, UNC0646	Cytotoxicity against p53-deficient human HCT116 cells assessed as cell viability after 48 hrs by MTT assay Cytotoxicity against p53-deficient human HCT116 cells assessed as cell viability after 48 hrs by MTT assay	[PMID: 21780790]
HCT-116	EC₅₀	8.7 μM Compound: 6, UNC0646	Cytotoxicity against human HCT116 cells assessed as cell viability after 48 hrs by MTT assay Cytotoxicity against human HCT116 cells assessed as cell viability after 48 hrs by MTT assay	[PMID: 21780790]
HCT-116	IC₅₀	0.068 μM Compound: 6, UNC0646	Inhibition of G9a in human HCT116 cells assessed as reduction of H3K9me2 after 48 hrs by In-Cell Western assay Inhibition of G9a in human HCT116 cells assessed as reduction of H3K9me2 after 48 hrs by In-Cell Western assay	[PMID: 21780790]
HCT-116	IC₅₀	0.086 μM Compound: 6, UNC0646	Inhibition of G9a in p53-deficient human HCT116 cells assessed as reduction of H3K9me2 after 48 hrs by In-Cell Western assay Inhibition of G9a in p53-deficient human HCT116 cells assessed as reduction of H3K9me2 after 48 hrs by In-Cell Western assay	[PMID: 21780790]
IMR-90	EC₅₀	3.6 μM Compound: 6, UNC0646	Cytotoxicity against human IMR90 cells assessed as cell viability after 48 hrs by MTT assay Cytotoxicity against human IMR90 cells assessed as cell viability after 48 hrs by MTT assay	[PMID: 21780790]
IMR-90	IC₅₀	0.01 μM Compound: 6, UNC0646	Inhibition of G9a in human IMR90 cells assessed as reduction of H3K9me2 after 48 hrs by In-Cell Western assay Inhibition of G9a in human IMR90 cells assessed as reduction of H3K9me2 after 48 hrs by In-Cell Western assay	[PMID: 21780790]
MCF7	IC₅₀	0.01 μM Compound: 6, UNC0646	Inhibition of G9a in human MCF7 cells assessed as reduction of H3K9me2 after 48 hrs by In-Cell Western assay Inhibition of G9a in human MCF7 cells assessed as reduction of H3K9me2 after 48 hrs by In-Cell Western assay	[PMID: 21780790]
MDA-MB-231	EC₅₀	3.3 μM Compound: 6, UNC0646	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	0.026 μM Compound: 6, UNC0646	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]
PC-3	EC₅₀	2.8 μM Compound: 6, UNC0646	Cytotoxicity against human PC3 cells assessed as cell viability after 48 hrs by MTT assay Cytotoxicity against human PC3 cells assessed as cell viability after 48 hrs by MTT assay	[PMID: 21780790]
PC-3	IC₅₀	0.012 μM Compound: 6, UNC0646	Inhibition of G9a in human PC3 cells assessed as reduction of H3K9me2 after 48 hrs by In-Cell Western assay Inhibition of G9a in human PC3 cells assessed as reduction of H3K9me2 after 48 hrs by In-Cell Western assay	[PMID: 21780790]

In Vitro

UNC0646 (Compound 6) has high cellular potency and excellent separation of functional potency versus cell toxicity in a variety of cell lines. UNC0646 is highly potent in reducing H3K9me2 levels and has low cell toxicity. UNC0646 reduces H3K9me2 levels with ICW IC₅₀ values of 26 nM, 10 nM, 12 nM, 14 nM, 68 nM, 86 nM and 10 nM in MDA-MB-231, MCF7, PC3, 22RV1, HCT116 wt, HCT 116 p53^-/- and IMR90 cell lines, respectively^[1].

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

Chemical Information

CAS No. 1320288-17-2
Appearance Solid
Masse moléculaire 621.90
Formule C₃₆H₅₉N₇O₂
Color White to light yellow
SMILES

COC1=CC2=C(NC3CCN(C4CCCCC4)CC3)N=C(N5CCN(C(C)C)CCC5)N=C2C=C1OCCCN6CCCCC6
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

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

Publications (1)

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Journal Impact Factor

Cell Death Dis

Global crotonylome reveals hypoxia-mediated lamin A crotonylation regulated by HDAC6 in liver cancer. [Abstract]

2022 Aug 17;13(8):717. PMID: 35977926

Solvant et solubilité

In Vitro:

DCM : ≥ 50 mg/mL (80.40 mM)

DMSO : 33.33 mg/mL (53.59 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

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

1.6080 mL

8.0399 mL

16.0798 mL

5 mM

0.3216 mL

1.6080 mL

3.2160 mL

10 mM

0.1608 mL

0.8040 mL

1.6080 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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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: ≥ 4.55 mg/mL (7.32 mM); Clear solution

This protocol yields a clear solution of ≥ 4.55 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (45.5 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (4.02 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

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.

Protocol 3

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

Solubility: ≥ 2.5 mg/mL (4.02 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:

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (275 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)
Instruction de manipulation (2659 KB)

Références

[1]. 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]

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 / DCM	1 mM	1.6080 mL	8.0399 mL	16.0798 mL	40.1994 mL
	5 mM	0.3216 mL	1.6080 mL	3.2160 mL	8.0399 mL
	10 mM	0.1608 mL	0.8040 mL	1.6080 mL	4.0199 mL
	15 mM	0.1072 mL	0.5360 mL	1.0720 mL	2.6800 mL
	20 mM	0.0804 mL	0.4020 mL	0.8040 mL	2.0100 mL
	25 mM	0.0643 mL	0.3216 mL	0.6432 mL	1.6080 mL
	30 mM	0.0536 mL	0.2680 mL	0.5360 mL	1.3400 mL
	40 mM	0.0402 mL	0.2010 mL	0.4020 mL	1.0050 mL
	50 mM	0.0322 mL	0.1608 mL	0.3216 mL	0.8040 mL
DCM	60 mM	0.0268 mL	0.1340 mL	0.2680 mL	0.6700 mL
DCM	80 mM	0.0201 mL	0.1005 mL	0.2010 mL	0.5025 mL

Keywords

UNC0646

1 Cited Publications

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Voir tous les produits spécifiques à Isoform Histone Methyltransferase

Activité biologique

Chemical Information

Publications (1)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

UNC0646

UNC0638

UNC 0631

UNC0642

A-366

SGC0946

BIX-01294

UNC1999

UNC 0631 (Standard)

UNC0224

Pinometostat

3-Deazaneplanocin A hydrochloride

UNC0379

Publications Citing Use of MedChemExpress (MCE) UNC0646

Voir tous les produits spécifiques à Isoform Histone Methyltransferase

Activité biologique

Chemical Information

Publications (1)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

UNC0646 Related Classifications

HY-13807 Related Classifications