UNC0379 TFA

Cat. No.: HY-12335A: FAQs
Data Sheet
SDS

COA
Handling Instructions Technical Support

UNC0379 TFA is a selective, substrate-competitive inhibitor of lysine methyltransferase SETD8 (KMT5A) with an IC₅₀ of 7.3 μM, K_D value of 18.3 μM. UNC0379 TFA can be used in the research of inflammation and cancers, such as pulmonary fibrosis, ovarian cancer, neuroblastoma.

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

UNC0379 TFA Chemical Structure

CAS No. : 1620401-83-3

Size	Price	Stock
2 mg		Ask For Quote & Lead Time
5 mg		Ask For Quote & Lead Time

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Other In-stock Forms of UNC0379 TFA:

UNC0379

Other Forms of UNC0379 TFA:

UNC0379 In-stock

7 Publications Citing Use of MCE UNC0379 TFA

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•Related Small Molecules:

•Related Proteins:

View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms

EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H 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

SETD8 (KMT5A)^[1]

In Vitro

UNC0379 TFA (1-10 μM, 9 days) inhibits HGSOC cells proliferation^[2].
UNC0379 TFA (10 μM, 96 h) increases in the proportion of sub-G1 phase cells in HGSOC cells^[2].
UNC0379 TFA (10 μM, 48 h) induces myofibroblast de-differentiation and inhibits additional fibroblast to myofibroblast differentiation^[3].

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

Cell Viability Assay^[1]

Cell Line:	JHOS2, JHOS3, JHOS4, OVCAR3, OVCAHO, OVKATE, KURAMOCHI, TYKnu
Concentration:	1-10 μM
Incubation Time:	9 days
Result:	Inhibited HGSOC cells proliferation with IC₅₀s ranging from 0.39 to 3.20 µM.

Cell Cycle Analysis^[1]

Cell Line:	JHOS3, OVCAR3
Concentration:	10 µM
Incubation Time:	96 h
Result:	Arrested cells in sub-G1 phase.

In Vivo

UNC0379 TFA (intratracheal administration, 1 mg/kg/day, 1 mg/kg/day, on day7, 8, and 9) ameliorates the lung fibrosis in Bleomycin (BLM)-induced lung fibrosis mouse^[3].

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

Animal Model:	Bleomycin (BLM)-induced lung fibrosis mouse model^[3]
Dosage:	1 mg/kg/day
Administration:	Intratracheal administration, on day7, 8, and 9.
Result:	Ameliorated BLM-induced lung fibrosis (supported by the evaluation of the Ashcroft score and changes in the collagen content in the lung samples) without affecting pulmonary inflammation.

Molecular Weight

527.58

Formula

C₂₅H₃₆F₃N₅O₄

CAS No.

1620401-83-3

Appearance

Solid

Color

Light yellow to khaki

SMILES

COC1=C(OC)C=C2C(N=C(N3CCCC3)N=C2NCCCCCN4CCCC4)=C1.O=C(O)C(F)(F)F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

H₂O : 100 mg/mL (189.54 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.8954 mL	9.4772 mL	18.9545 mL
5 mM	0.3791 mL	1.8954 mL	3.7909 mL
10 mM	0.1895 mL	0.9477 mL	1.8954 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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 Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

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).

Purity & Documentation

Purity: 99.91%

Select Batch:

Data Sheet (280 KB) SDS (0 KB)

COA (251 KB)

Handling Instructions (2659 KB)

References

[1]. Ma A, et al. Discovery of a Selective, Substrate-Competitive Inhibitor of the Lysine Methyltransferase SETD8. J Med Chem. 2014 Aug 14;57(15):6822-33. [Content Brief]

[2]. Miku Wada, et al. Epigenetic Modifier SETD8 as a Therapeutic Target for High-Grade Serous Ovarian Cancer. Biomolecules. 2020 Dec 16;10(12):1686. [Content Brief]

[3]. Keita Ugai, et al. Inhibition of the SET8 Pathway Ameliorates Lung Fibrosis Even Through Fibroblast Dedifferentiation. Front Mol Biosci. 2020 Aug 5;7:192. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O	1 mM	1.8954 mL	9.4772 mL	18.9545 mL	47.3862 mL
	5 mM	0.3791 mL	1.8954 mL	3.7909 mL	9.4772 mL
	10 mM	0.1895 mL	0.9477 mL	1.8954 mL	4.7386 mL
	15 mM	0.1264 mL	0.6318 mL	1.2636 mL	3.1591 mL
	20 mM	0.0948 mL	0.4739 mL	0.9477 mL	2.3693 mL
	25 mM	0.0758 mL	0.3791 mL	0.7582 mL	1.8954 mL
	30 mM	0.0632 mL	0.3159 mL	0.6318 mL	1.5795 mL
	40 mM	0.0474 mL	0.2369 mL	0.4739 mL	1.1847 mL
	50 mM	0.0379 mL	0.1895 mL	0.3791 mL	0.9477 mL
	60 mM	0.0316 mL	0.1580 mL	0.3159 mL	0.7898 mL
	80 mM	0.0237 mL	0.1185 mL	0.2369 mL	0.5923 mL
	100 mM	0.0190 mL	0.0948 mL	0.1895 mL	0.4739 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

UNC0379 TFA 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.

Keywords:

UNC03791620401-83-3UNC 0379UNC-0379Histone MethyltransferaseOvarian cancerlysine methyltransferaseantitumorHGSOCOVCAR3JHOS3neuroblastomapulmonary fibrosisInhibitorinhibitorinhibit

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