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UNC6934 NSD antagonist

Name: UNC6934
Brand: Selleck Chemicals
SKU: E1059
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.E1059

UNC6934 is a a chemical probe targeting the N-terminal PWWP (PWWP1) domain of NSD2. This compound is a potent antagonist of NSD2-PWWP1 with a Kd (SPR) of 80 nM and is selective for NSD2-PWWP1 over 14 other PWWP domains including NSD3-PWWP1. It disrupts the NSD2-PWWP1 interaction with H3K36me2 nucleosomes in U2OS cells as measured by a NanoBret assay with an IC50 of 1.09 μM.

Chemical Structure

Molecular Weight: 443.46

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: E105901 DMSO]22 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.55%

99.55

Related Targets	PRMT EZH1/2 DNA Methyltransferase LSD1 MLL JMJD G9a/GLP FTO SETD SMYD DOT1 MAT2A COMT WDR5 NNMT HNMT SAM MTase PPMTase

Chemical Information, Storage & Stability

Molecular Weight	443.46	Formula	C₂₄H₂₁N₅O₄	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	2561494-77-5	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent

Solubility

In vitro
Batch:

DMSO : 22 mg/mL ( (49.6 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	NSD2 ^[1] 80 nM(Kd) NSD2 ^[1] (in the NanoBret assay) 1.09 μM
In vitro	UNC6934-mediated antagonism of PWWP1 leads to accumulation of endogenous NSD2 in the nucleolus. ^[1]
References	https://pubmed.ncbi.nlm.nih.gov/34782742/

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