Chaetocin是組蛋白甲基轉(zhuǎn)移酶(HMT) SU(VAR)3-9的特異性抑制劑，對SU(VAR)3-9的IC50值為0.6 μM。Chaetocin抑制硫氧還蛋白還原酶(TrxR)的IC50值為4 μM。
PYZD-4409產(chǎn)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
公司介紹：MedChemExpress(MCE)專注于各種抑制劑、激動劑、API及化合物庫，總部位于美國新澤西，分別在瑞典和上海設(shè)有歐洲區(qū)子公司和亞洲區(qū)總代理，營銷網(wǎng)點遍及全球20多個國家地區(qū)。MCE經(jīng)過多年努力已成為全球生物活性小分子領(lǐng)域的一流供應(yīng)商， 產(chǎn)品涵蓋癌癥、神經(jīng)科學(xué)、抗感染、表觀遺傳學(xué)等20個熱門研究領(lǐng)域，PI3K、MAPK等近千個細分靶點，超過4000個活性小分子化合物現(xiàn)貨，以及GPCR、API、離子通道等超過20種不同類型的化合物庫，同時提供從毫克到千克的專業(yè)定制合成服務(wù)。
MCE 對每批產(chǎn)品都進行嚴(yán)格的LCMS和NMR檢驗，其產(chǎn)品已被全球近萬名客戶廣泛使用并發(fā)表大量文章、專利；
MCE 定期增加各領(lǐng)域熱門抑制劑、激動劑，不斷擴增已有化合物庫，以滿足最新的科研需求；
數(shù)千種產(chǎn)品在上海有充足備貨，24-48小時內(nèi)送達客戶；
大量產(chǎn)品提供免費試用裝； 已為全球多個知名企業(yè)、院校構(gòu)建各種定制型化合物庫。
產(chǎn)品鏈接：www.medchemexpress.cn/PYZD-4409.html
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;
Research Area:Cancer
電話： 021-58955995
網(wǎng)址： www.MedChemExpress.cn
地址： 上海市浦東新區(qū)蔡倫路720號2號樓3層
PYZD-4409產(chǎn)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
公司介紹：MedChemExpress(MCE)專注于各種抑制劑、激動劑、API及化合物庫，總部位于美國新澤西，分別在瑞典和上海設(shè)有歐洲區(qū)子公司和亞洲區(qū)總代理，營銷網(wǎng)點遍及全球20多個國家地區(qū)。MCE經(jīng)過多年努力已成為全球生物活性小分子領(lǐng)域的一流供應(yīng)商， 產(chǎn)品涵蓋癌癥、神經(jīng)科學(xué)、抗感染、表觀遺傳學(xué)等20個熱門研究領(lǐng)域，PI3K、MAPK等近千個細分靶點，超過4000個活性小分子化合物現(xiàn)貨，以及GPCR、API、離子通道等超過20種不同類型的化合物庫，同時提供從毫克到千克的專業(yè)定制合成服務(wù)。
MCE 對每批產(chǎn)品都進行嚴(yán)格的LCMS和NMR檢驗，其產(chǎn)品已被全球近萬名客戶廣泛使用并發(fā)表大量文章、專利；
MCE 定期增加各領(lǐng)域熱門抑制劑、激動劑，不斷擴增已有化合物庫，以滿足最新的科研需求；
數(shù)千種產(chǎn)品在上海有充足備貨，24-48小時內(nèi)送達客戶；
大量產(chǎn)品提供免費試用裝； 已為全球多個知名企業(yè)、院校構(gòu)建各種定制型化合物庫。
產(chǎn)品鏈接：www.medchemexpress.cn/PYZD-4409.html
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;
Research Area:Cancer
電話： 021-58955995
網(wǎng)址： www.MedChemExpress.cn
地址： 上海市浦東新區(qū)蔡倫路720號2號樓3層
110102000668（1）號