2. Epigenetics
  3. Histone Methyltransferase
  4. UNC8153

UNC8153 is a potent and selective nuclear receptor-binding SET domain-containing 2 (NSD2)-targeted degrader with a Kd of 24 nM. UNC8153 reduces the cellular levels of both NSD2 protein (DC50 in cell U2OS is 0.35 μM) and the H3K36me2 chromatin mark. UNC8153 contains a simple warhead that confers proteasome-dependent degradation of NSD2.

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UNC8153

UNC8153 Chemical Structure

CAS No. : 2929304-60-7

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Based on 1 publication(s) in Google Scholar

Other Forms of UNC8153:

UNC8153 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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Description

UNC8153 is a potent and selective nuclear receptor-binding SET domain-containing 2 (NSD2)-targeted degrader with a Kd of 24 nM. UNC8153 reduces the cellular levels of both NSD2 protein (DC50 in cell U2OS is 0.35 μM) and the H3K36me2 chromatin mark. UNC8153 contains a simple warhead that confers proteasome-dependent degradation of NSD2[1].

In Vitro

UNC8153 (0-20 μM, 96 h) exhibits anti-adhesion effect in KMS11 cell, and exhibits mild cytotoxicity against MM1S cell[1].

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

UNC8153 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: MM1S
Concentration: 0-50 μM
Incubation Time: 96 h
Result: Inhibited the cell proliferation.
Molecular Weight

583.68

Formula

C33H37N5O5
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CC=C2NC(COC2=C1)=O)N(CC3=CC=C(C(NC4=CC=C(C(NCCCCCCN)=O)C=C4)=O)C=C3)C5CC5
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -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 (171.33 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 1.7133 mL 8.5663 mL 17.1327 mL
5 mM 0.3427 mL 1.7133 mL 3.4265 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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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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.
Calculation results:
Working solution concentration: mg/mL
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 1.7133 mL 8.5663 mL 17.1327 mL 42.8317 mL
5 mM 0.3427 mL 1.7133 mL 3.4265 mL 8.5663 mL
10 mM 0.1713 mL 0.8566 mL 1.7133 mL 4.2832 mL
15 mM 0.1142 mL 0.5711 mL 1.1422 mL 2.8554 mL
20 mM 0.0857 mL 0.4283 mL 0.8566 mL 2.1416 mL
25 mM 0.0685 mL 0.3427 mL 0.6853 mL 1.7133 mL
30 mM 0.0571 mL 0.2855 mL 0.5711 mL 1.4277 mL
40 mM 0.0428 mL 0.2142 mL 0.4283 mL 1.0708 mL
50 mM 0.0343 mL 0.1713 mL 0.3427 mL 0.8566 mL
60 mM 0.0286 mL 0.1428 mL 0.2855 mL 0.7139 mL
80 mM 0.0214 mL 0.1071 mL 0.2142 mL 0.5354 mL
100 mM 0.0171 mL 0.0857 mL 0.1713 mL 0.4283 mL
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UNC8153 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:

UNC81532929304-60-7UNC 8153UNC-8153Histone MethyltransferaseNSD2 degraderH3K36me2proteasome-dependent degradation of NSD2antiproliferative effectsantiadhesive effectsInhibitorinhibitorinhibit

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