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UNC8153 TFA

Catalog No. T83867   CAS 2929304-61-8

UNC8153 is a NSD2-specific histone-lysine N-methyltransferase degrader, showing selective activity towards NSD2 over NSD1 and NSD3 at 20 µM, and demonstrating a 50% degradation constant (DC50) of 350 nM. At a concentration of 10 µM, UNC8153 induces NSD2 degradation and significantly diminishes histone H3 lysine 36 dimethylation (H3K36me2) levels in MM.1S multiple myeloma cells. This degradation effect can be blocked by MLN4924, an inhibitor of the ubiquitin-activating enzyme. Furthermore, UNC8153 at 20 µM inhibits the proliferation of MM.1S cells harboring an NSD2E1099K activating mutation, but not in other cell lines (MDA-MB-231, U2OS, or HEK293) expressing wild-type NSD2. Additionally, UNC8153 at the same concentration impedes the attachment and migration of MM.1S cells, indicating its potential therapeutic implications for certain cancers.

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UNC8153 TFA Chemical Structure
UNC8153 TFA, CAS 2929304-61-8
Pack Size Availability Price/USD Quantity
1 mg 35 days $ 178.00
5 mg 35 days $ 690.00
10 mg 35 days $ 1,140.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description UNC8153 is a NSD2-specific histone-lysine N-methyltransferase degrader, showing selective activity towards NSD2 over NSD1 and NSD3 at 20 µM, and demonstrating a 50% degradation constant (DC50) of 350 nM. At a concentration of 10 µM, UNC8153 induces NSD2 degradation and significantly diminishes histone H3 lysine 36 dimethylation (H3K36me2) levels in MM.1S multiple myeloma cells. This degradation effect can be blocked by MLN4924, an inhibitor of the ubiquitin-activating enzyme. Furthermore, UNC8153 at 20 µM inhibits the proliferation of MM.1S cells harboring an NSD2E1099K activating mutation, but not in other cell lines (MDA-MB-231, U2OS, or HEK293) expressing wild-type NSD2. Additionally, UNC8153 at the same concentration impedes the attachment and migration of MM.1S cells, indicating its potential therapeutic implications for certain cancers.
Molecular Weight 697.70
Formula C33H37N5O5.CF3COOH
CAS No. 2929304-61-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMF: 30 mg/mll

Ethanol: 30 mg/ml

DMSO: 30 mg/ml

PBS pH 7.2: 5 mg/ml

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Keywords

UNC8153 TFA 2929304-61-8 inhibitor inhibit

 

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