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技术文章

Chaetocin说明

点击次数:655 发布时间:2018/4/19 12:55:25

Chaetocin是组蛋白甲基转移酶(HMT) SU(VAR)3-9的特异性抑制剂,对SU(VAR)3-9的IC50值为0.6 μM。Chaetocin抑制硫氧还蛋白还原酶(TrxR)的IC50值为4 μM。
PYZD-4409产品描述:PYZD-4409 is a novel small molecule inhibitor of Ubiquitin-activating enzyme UBA1/E1 enzyme with an IC50 of 20 uM (cell-free enzymatic assay). IC50 Value: 20 uM (cell-free enzymatic assay) [1] Target: E1 enzyme (Ubiquitin-activating enzyme) in vitro: PYZD-4409 inhibited the ATP-dependent activation of ubiquitin and subsequent transfer of the activated ubiquitin from the E1 to the common human E2 enzyme UBE2E2 in a gel-based assay. The IC50 of inhibition was estimated to be 20μM in a cell-free enzymatic assay. Suggesting specificity of PYZD-4409 for the E1 enzyme, the compound had no effect on unrelated enzymes such as α-Mannosidase II glycosylation enzyme or Luciferase at concentrations up to 100μM (data not shown). It also did not inhibit the summo E1, Uba2, at concentrations up to 100μM. In 5 of 8 leukemia and myeloma cell lines, PYZD-4409 induced cell death with a LD50 less than 10μM. Myeloma cell lines were particularly sensitive to E1 inhibition because PYZD-4409 induced cell


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Purity:98%
MWt:696.8399
Formula:C30H28N6O6S4
SMILES:O=C([C@@](N1C)(SS2)CO)N3[C@](NC4=CC=CC=C54)([H])[C@]5([C@@]6(C7=CC=CC=C7N8)[C@@]8([H])N(C9=O)[C@](C%10=O)(SS[C@]9(CO)N%10C)C6)C[C@]32C1=O
Pathway:Epigenetics;
Mechanisms:Histone Methyltransferase;
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