UNC0321

Name: UNC0321
Brand: MedChemExpress
SKU: HY-10930
Rating: 5.0 (3 reviews)

Cat. No.: HY-10930 Purity: 99.91%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

For research use only. We do not sell to patients.

UNC0321 Chemical Structure

CAS No. : 1238673-32-9

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 132	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 132	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 116	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 180	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 350	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 550	In-stock	Estimated Time of Arrival: December 31
100 mg		Get quote
200 mg		Get quote

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Customer Review

Based on 3 publication(s) in Google Scholar

2 Publications Citing Use of MCE UNC0321

: 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.

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•Related Screening Libraries:

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View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms

EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

EHMT1/GLP/KMT1D

15-23 nM (IC₅₀)

G9a

63 pM (Ki)

G9a

6-9 nM (IC₅₀)

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.

Molecular Weight

515.69

Formula

C₂₇H₄₅N₇O₃

CAS No.

1238673-32-9

Appearance

Solid

Color

White to yellow

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
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.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 99.91%

Select Batch:

Data Sheet (282 KB) SDS (393 KB)

COA (247 KB) HNMR (267 KB) RP-HPLC (207 KB) MS (69 KB)

Handling Instructions (2659 KB)

References

[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

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 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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UNC0321

Customer Review

UNC0321 Related Antibodies

2 Publications Citing Use of MCE UNC0321

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Histone Methyltransferase Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

UNC0321 Related Antibodies

Molarity Calculator

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Complete Stock Solution Preparation Table

UNC0321 Related Classifications

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