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UNC1999

HY-15646

(UNC-1999; UNC 1999)

UNC1999

UNC1999 Chemical Structure

UNC1999 is a potent, orally bioavailable and selective inhibitor of EZH2 and EZH1 with IC50 of 2 nM and 45 nM, respectively.

Size Price Stock Quantity
Free sample   Apply now  
10 mM * 1 mL in DMSO $85 In-stock
5 mg $68 In-stock
10 mg $120 In-stock
50 mg $360 In-stock
100 mg $576 In-stock
200 mg Get quote
500 mg Get quote
Size Price Stock Quantity
Free sample   Apply now  
10 mM * 1 mL in DMSO €83 In-stock
5 mg €67 In-stock
10 mg €118 In-stock
50 mg €353 In-stock
100 mg €564 In-stock
200 mg Get quote
500 mg Get quote

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Product name: UNC1999
Cat. No.: HY-15646

UNC1999 Data Sheet

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    Purity: 99.53%

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    DataSheet

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    MSDS

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    COA

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Biological Activity of UNC1999

UNC1999 is a potent, orally bioavailable and selective inhibitor of EZH2 and EZH1 with IC50 of 2 nM and 45 nM, respectively.
IC50 Value: 2 nM(EZH2); 45 nM(EZH1)
Target: EZH2
UNC1999 was the first orally bioavailable EZH2 inhibitor that has high in vitro potency for wild-type and mutant EZH2 as well as EZH1, UNC1999 was highly selective for EZH2 and EZH1 over a broad range of epigenetic and non-epigenetic targets, competitive with the cofactor SAM and non-competitive with the peptide substrate. This inhibitor potently reduced H3K27me3 levels in cells and selectively killed diffused large B cell lymphoma cell lines harboring the EZH2Y641N mutant. Importantly, UNC1999 was orally bioavailable in mice, making this inhibitor a valuable tool for investigating the role of EZH2 and EZH1 in chronic animal studies. We also designed and synthesized UNC2400, a close analogue of UNC1999 with potency >1,000-fold lower than that of UNC1999 as a negative control for cell-based studies [1].

Protocol (Extracted from published papers and Only for reference)

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Chemical Information

M.Wt 569.74 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C₃₃H₄₃N₇O₂
CAS No 1431612-23-5
Solvent & Solubility

10 mM in DMSO

Preparing Stock Solutions

1 mg 5 mg 10 mg
1 mM 1.7552 mL 8.7759 mL 17.5519 mL
5 mM 0.3510 mL 1.7552 mL 3.5104 mL
10 mM 0.1755 mL 0.8776 mL 1.7552 mL

References on UNC1999

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