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Product Name:UNC2400
CAS:1433200-49-7
Purity:98% Package:5MG;10MG;50MG;100MG,1G,5G,100G
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BOC Sciences
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| Products Intro: |
Product Name:UNC 2400
CAS:1433200-49-7
Purity:≥98% by HPLC Remarks:UNC 2400 is a negative control of UNC 1999 that displays 1000-fold lower potency than active analog (IC50 = 62 and >200 μM for EZH1 and EZH2, respectively).
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| | UNC 2400 Basic information |
| Product Name: | UNC 2400 | | Synonyms: | UNC 2400;N-[(1,6-dimethyl-2-oxo-4-propylpyridin-3-yl)methyl]-N-methyl-1-propan-2-yl-6-[6-(4-propan-2-ylpiperazin-1-yl)pyridin-3-yl]indazole-4-carboxamide;N-[(1,2-Dihydro-1,6-dimethyl-2-oxo-4-propyl-3-pyridinyl)methyl]-N-methyl-1-(1-methylethyl)-6-[6-[4-(1-methylethyl)-1-piperazinyl]-3-pyridinyl]-1H-indazole-4-carboxamide;1H-Indazole-4-carboxamide, N-[(1,2-dihydro-1,6-dimethyl-2-oxo-4-propyl-3-pyridinyl)methyl]-N-methyl-1-(1-methylethyl)-6-[6-[4-(1-methylethyl)-1-piperazinyl]-3-pyridinyl]- | | CAS: | 1433200-49-7 | | MF: | C35H47N7O2 | | MW: | 597.79 | | EINECS: | | | Product Categories: | API | | Mol File: | 1433200-49-7.mol |  |
| | UNC 2400 Chemical Properties |
| storage temp. | Store at -20°C | | solubility | Soluble to 100 mM in DMSO and to 100 mM in 1eq. HCl | | form | solid | | color | Off White |
| | UNC 2400 Usage And Synthesis |
| Uses | UNC 2400 is an inactive analog compound of UNC 19999, which itself is a selective inhibitor of EZH2 and EZH1. | | Biological Activity | unc 2400, a close analogue of unc1999, is a negative control of unc1999 that inhibits ezh2 and ezh1 [1].histone-lysine n-methyltransferase (ezh1 or ezh2) is the catalytic subunit of the polycomb repressive complex 2 that catalyzes methylation of histone h3 lysine 27 (h3k27). the trimethylation of h3k27 (h3k27me3) is a transcriptionally repressive post-translational modification. hypertrimethylation of h3k27 and overexpression of ezh2 are involved in cancers [1].unc 2400 is a negative control of unc1999. unc 2400 inhibited ezh2 with ic50 value of 13 μm and exhibited >1,000-fold less potency than unc1999. also, unc 2400 inhibited ezh1 and ezh2 y641f with ic50 values of 62 and >200 μm, respectively. in mcf10a cells, unc 2400 exhibited little inhibition of h3k27me3 levels and had low cellular toxicity with ec50 value of 27.5 μm that was similar to unc1999. in db cells, unc 2400 (3 μm) did not significantly inhibit db cell proliferation and had no influence on h3k27me3 or ezh2 levels [1]. | | references | [1]. konze kd, ma a, li f, et al. an orally bioavailable chemical probe of the lysine methyltransferases ezh2 and ezh1. acs chem biol, 2013, 8(6): 1324-1334. |
| | UNC 2400 Preparation Products And Raw materials |
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