2. Epigenetics
  3. Histone Methyltransferase
  4. UNC6934

UNC6934 is a selective NSD2-PWWP1 antagonist with IC50 values of 78 nM and 104 nM, and a Ka of 91 nM against human targets. UNC6934 binds to the canonical methyl-lysine binding pocket of NSD2-PWWP1 and directly competes with H3K36me2 for binding. UNC6934 induces the aggregation of NSD2 within the nucleolus, without altering ribosomal RNA transcription, global H3K36me2 levels or the proliferation of KMS-11 cells. UNC6934 can be used in studies related to multiple myeloma and diffuse intrinsic pontine glioma.

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UNC6934

UNC6934 Chemical Structure

CAS No. : 2561494-77-5

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UNC6934 Related Antibodies

Top Publications Citing Use of Products

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

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  • Customer Review

Description

UNC6934 is a selective NSD2-PWWP1 antagonist with IC50 values of 78 nM and 104 nM, and a Ka of 91 nM against human targets. UNC6934 binds to the canonical methyl-lysine binding pocket of NSD2-PWWP1 and directly competes with H3K36me2 for binding. UNC6934 induces the aggregation of NSD2 within the nucleolus, without altering ribosomal RNA transcription, global H3K36me2 levels or the proliferation of KMS-11 cells. UNC6934 can be used in studies related to multiple myeloma and diffuse intrinsic pontine glioma.[1][2]

In Vitro

UNC6934 (2 μM; 60 s contact time, 120 s dissociation time) potently binds purified human NSD2-PWWP1 domain with a Kd of 91 nM, as measured by SPR[1].
UNC6934 (100 μM) selectively binds the aromatic cage of purified human NSD2-PWWP1 domain, as indicated by a significant thermal shift, with no measurable binding to 15 other human PWWP domains[1].
UNC6934 (serial dilutions; 15 min pre-incubation, 30 min incubation with nucleosomes) inhibits the interaction between purified human NSD2-PWWP1 domain and H3K36me2 nucleosomes with an IC50 of 104 nM, as measured by AlphaScreen[1].
UNC6934 (serial dilutions; 15 min pre-incubation, 30 min incubation with nucleosomes) inhibits the interaction between purified full-length human NSD2 and H3K36me2 nucleosomes (in the presence of salmon sperm DNA) with an IC50 of 78 nM, as measured by AlphaScreen[1].
UNC6934 (up to 25 μM; 30 min) does not inhibit the interaction between purified human NSD2-PWWP1 domain and double-stranded DNA, as measured by fluorescence polarization[1].
UNC6934 (20 μM; 1 h) selectively engages endogenous NSD2 in KMS-11 multiple myeloma whole-cell lysates, as demonstrated by competition with the biotinylated analog UNC7096[1].
UNC6934 (serial dilutions; 20 h) selectively engages the wild-type human NSD2-PWWP1 domain in live U2OS cells, with an EC50 of 1.23 μM as measured by NanoBRET PPI assay[1].
UNC6934 (5 μM; 4 h) induces accumulation of endogenous NSD2 in the nucleolus of U2OS cells, as measured by increased colocalization with the nucleolar marker fibrillarin[1].
UNC6934 (10 μM; 30 min) partially displaces endogenous NSD2 from chromatin in KMS-11 multiple myeloma cells, as measured by cellular fractionation[1].
UNC6934 (10 nM-10000 nM, 1 μM-100 μM; 3-5 days) reduces the viability of DIPG 13 cells in a dose- and time-dependent manner, with an IC50 of 17.99 μM after 5-day treatment[2].
UNC6934 (10 nM-10000 nM; 5 days) produces only a minimal reduction in the viability of DIPG IV cells, with 94.83% viability remaining after 5-day treatment with 10000 nM UNC6934[2].
UNC6934 (1 μM-100 μM; 5 days) reduces fibroblast cell viability to a lesser degree than it reduces DIPG 13 cell viability, indicating greater selectivity for DIPG 13 cells over non-transformed fibroblast cells[2].
UNC6934 (5 μM-10 μM alone, 5 μM-10 μM in combination with 2 μM-4 μM ONC201; 5 days) produces an additive reduction in DIPG IV cell viability for three of the four tested dose combinations, with the most effective combination being 5 μM UNC6934 and 2 μM ONC201 after 5-day treatment[2].

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

UNC6934 Related Antibodies

Immunofluorescence[1]

Cell Line: U2OS cells
Concentration: 5 μM
Incubation Time: 4 h
Result: Significantly increased the colocalization of endogenous NSD2 with fibrillarin (median PCC = 0.86) compared to DMSO control (median PCC = 0.70) and UNC7145 control (median PCC = 0.71).

Western Blot Analysis[1]

Cell Line: KMS-11 multiple myeloma cells
Concentration: 10 μM
Incubation Time: 30 min on ice
Result: Increased the amount of NSD2 in the 150 mM NaCl-extracted nucleoplasmic fraction (S3), indicating partial displacement from chromatin.

Cell Viability Assay[2]

Cell Line: DIPG 13 cells
Concentration: 10 nM-10000 nM (5-day treatment); 1 μM-100 μM (3-day treatment, 5-day treatment)
Incubation Time: 3 days (1 μM-100 μM); 5 days (10 nM-10000 nM, 1 μM-100 μM)
Result: Reduced DIPG 13 cell viability to a maximum of 80.98% relative to DMSO control at 10 nM-10000 nM (5-day treatment).
Reduced DIPG 13 cell viability in a dose-dependent manner, with an IC50 of 17.99 μM at 1 μM-100 μM (5-day treatment).
Produced a greater reduction in DIPG 13 cell viability with 5-day treatment compared to 3-day treatment across all tested concentrations.

Cell Viability Assay[2]

Cell Line: fibroblast cells (non-transformed, noncancerous brain cells)
Concentration: 1 μM-100 μM
Incubation Time: 5 days
Result: Reduced fibroblast cell viability to a lesser extent than it reduced DIPG 13 cell viability, with a larger difference observed at 10 μM, 25 μM, 50 μM, and 100 μM doses.

Cell Viability Assay[2]

Cell Line: DIPG IV cells
Concentration: 5 μM, 10 μM (alone); 5 μM (in combination with 2 μM ONC201); 5 μM (in combination with 4 μM ONC201); 10 μM (in combination with 2 μM ONC201); 10 μM (in combination with 4 μM ONC201)
Incubation Time: 5 days
Result: Produced the largest relative drop in DIPG IV cell viability with combinatorial treatment of 5 μM UNC6934 and 2 μM ONC201.
Showed an additive reduction in cell viability beyond the effect of UNC6934 alone for three of the four tested combinatorial doses.
Molecular Weight

443.45

Formula

C24H21N5O4
CAS No.
Appearance

Solid

Color

Off-white to gray

SMILES

O=C(C1=CC=C(CN(C2CC2)C(C3=CC=C4NC(COC4=C3)=O)=O)C=C1)NC5=CC=NC=N5
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (56.38 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 2.2550 mL 11.2752 mL 22.5505 mL
5 mM 0.4510 mL 2.2550 mL 4.5101 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.

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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: ≥ 2.5 mg/mL (5.64 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 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: ≥ 2.5 mg/mL (5.64 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.

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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

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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2550 mL 11.2752 mL 22.5505 mL 56.3761 mL
5 mM 0.4510 mL 2.2550 mL 4.5101 mL 11.2752 mL
10 mM 0.2255 mL 1.1275 mL 2.2550 mL 5.6376 mL
15 mM 0.1503 mL 0.7517 mL 1.5034 mL 3.7584 mL
20 mM 0.1128 mL 0.5638 mL 1.1275 mL 2.8188 mL
25 mM 0.0902 mL 0.4510 mL 0.9020 mL 2.2550 mL
30 mM 0.0752 mL 0.3758 mL 0.7517 mL 1.8792 mL
40 mM 0.0564 mL 0.2819 mL 0.5638 mL 1.4094 mL
50 mM 0.0451 mL 0.2255 mL 0.4510 mL 1.1275 mL
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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:

UNC69342561494-77-5UNC 6934UNC-6934Histone MethyltransferaseH3K36me2fibrillarinDIPG IV cellsnucleolusfibroblast cellU2OS cellsDIPG 13 cellsKMS-11NSD2-PWWP1diffuse intrinsic pontine gliomaInhibitorinhibitorinhibit

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