This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.
This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.
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 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
Dose Conversion
You can also refer to dose conversion for different animals.
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Method for preparing DMSO master liquid: mg
drug pre-dissolved in μL DMSO (Master liquid concentration
mg/mL),
Method for preparing in vivo formulation:Take μL
DMSO master liquid, next add μL PEG300, mix and clarify, next add μL
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:
Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.