UNC6535 TFA

Cat. No.: HY-168992A: Data Sheet
SDS
Handling Instructions
FAQs
Technical Support

UNC6535 TFA is a covalent ligand targeting the triple Tudor domain (3TD) of SETDB1. UNC6535 TFA reversibly binds to the aromatic cages of both TD2 and TD3 within SETDB1 3TD simultaneously, weakly inhibits the methyltransferase activity of SETDB1, and displaces the H3K9Me2K14Ac peptide from SETDB1 3TD.

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

UNC6535 TFA Chemical Structure

Size	Stock	Quantity
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	Get quote
100 mg	Get quote

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Other Forms of UNC6535 TFA:

UNC6535 Get quote

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•Related Screening Libraries:

•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 NSD3/WHSC1L1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

Biological Activity
Purity & Documentation
References
Customer Review

Description

In Vitro

UNC6535 TFA reversibly binds to the purified tripartite Tudor domain of SETDB1 and displaces the H3K9Me2K14Ac peptide, with an IC₅₀ of 3.4 μM^[1].
UNC6535 TFA binds to the purified triple Tudor domain of SETDB1, with a measured K_d of 4.2 μM determined by isothermal titration calorimetry^[1].
UNC6535 TFA inhibits the methyltransferase activity of purified full-length SETDB1 protein, with an IC₅₀ of 84 μM^[1].
UNC6535 TFA inhibits the methyltransferase activity of purified truncated SETDB1-S (lacking the triple Tudor domain) with an IC₅₀ of 30 μM^[1].
UNC6535 TFA displaces the H3K9Me2K14Ac peptide from purified truncated SETDB1-S (lacking the tripartite Tudor domain) via fluorescence polarization, with an IC₅₀ of 8.6 μM^[1].

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

Molecular Weight

688.70

Formula

C₂₉H₄₆F₆N₆O₆

Appearance

Oil

SMILES

COC1=CC2=C(C(NCCCCCCN(C)C)=NC(NCCCCCN(C)C)=N2)C=C1OC.O=C(O)C(F)(F)F.O=C(O)C(F)(F)F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Pure form	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL (145.20 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.4520 mL	7.2601 mL	14.5201 mL
5 mM	0.2904 mL	1.4520 mL	2.9040 mL
10 mM	0.1452 mL	0.7260 mL	1.4520 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Data Sheet (270 KB) SDS (252 KB) Handling Instructions (2659 KB)

References

[1]. Uguen M, et al. Potent and selective SETDB1 covalent negative allosteric modulator reduces methyltransferase activity in cells. Nat Commun. 2025;16(1):1905. Published 2025 Feb 24. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.4520 mL	7.2601 mL	14.5201 mL	36.3003 mL
	5 mM	0.2904 mL	1.4520 mL	2.9040 mL	7.2601 mL
	10 mM	0.1452 mL	0.7260 mL	1.4520 mL	3.6300 mL
	15 mM	0.0968 mL	0.4840 mL	0.9680 mL	2.4200 mL
	20 mM	0.0726 mL	0.3630 mL	0.7260 mL	1.8150 mL
	25 mM	0.0581 mL	0.2904 mL	0.5808 mL	1.4520 mL
	30 mM	0.0484 mL	0.2420 mL	0.4840 mL	1.2100 mL
	40 mM	0.0363 mL	0.1815 mL	0.3630 mL	0.9075 mL
	50 mM	0.0290 mL	0.1452 mL	0.2904 mL	0.7260 mL
	60 mM	0.0242 mL	0.1210 mL	0.2420 mL	0.6050 mL
	80 mM	0.0182 mL	0.0908 mL	0.1815 mL	0.4538 mL
	100 mM	0.0145 mL	0.0726 mL	0.1452 mL	0.3630 mL

UNC6535 TFA Related Classifications

Others

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:

UNC6535UNC 6535UNC-6535Histone Methyltransferasecovalent ligand targeting the 3TD of SETDB1Inhibitorinhibitorinhibit

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