CAY-10603

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种高效、选择性的 HDAC6 抑制剂，IC50 为 2 pM。

A highly potent and selective HDAC6 inhibitor with IC50 of 2 pM; 200-fold less potent for HDAC3 (IC50=0.42 nM) and no inhibition on HDAC1/2/8/10 (IC50> 100 nM); downregulates the levels of EGFR protein and synergizes with gefitinib to induce apoptosis of the lung adenocarcinoma cell lines.(In Vitro):CAY10603 (Compound 7) shows potent inhibitory activities against pancreatic cancer cell lines, with IC50s of 1, 0.3, 0.1, 0.1, 0.6, <1, 0.5 μM for BxPC-3, HupT3, Mia Paca-2, Panc 04.03, SU.86.86, HMEC, HPDE6c7, respectively. CAY10603 (100 nM, 200-300 nM) is active against both the Mia Paca-2 and Panc04.03 cell lines. CAY10603 inhibits HDAC6 deacetylase activity, and supresses the proliferation of lung adenocarcinoma cells. CAY10603 also induces apoptosis of lung adenocarcinoma cells. Furthermore, CAY10603 synergizes with gefitinib to induce apoptosis in lung adenocarcinoma cell lines, partly through the destabilization of EGFR and inactivation of the EGFR pathway.

CAY10603 (Compound 7) shows potent inhibitory activities against pancreatic cancer cell lines, with IC50s of 1, 0.3, 0.1, 0.1, 0.6, <1, 0.5 μM for BxPC-3, HupT3, Mia Paca-2, Panc 04.03, SU.86.86, HMEC, HPDE6c7, respectively. CAY10603 (100 nM, 200-300 nM) is active against both the Mia Paca-2 and Panc04.03 cell lines. CAY10603 inhibits HDAC6 deacetylase activity, and supresses the proliferation of lung adenocarcinoma cells. CAY10603 also induces apoptosis of lung adenocarcinoma cells. Furthermore, CAY10603 synergizes with gefitinib to induce apoptosis in lung adenocarcinoma cell lines, partly through the destabilization of EGFR and inactivation of the EGFR pathway.

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CAY10603

Cell Cycle/DNA Damage

HDAC

HDAC1|HDAC6

Cancer

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1045792-66-2

446.4968

C22H30N4O6

>98% (HPLC)

10 mM in DMSO

O=C(OC(C)(C)C)NC1=CC=C(C2=CC(C(NCCCCCCC(NO)=O)=O)=NO2)C=C1

Carbamic acid, N-[4-[3-[[[7-(hydroxyamino)-7-oxoheptyl]amino]carbonyl]-5-isoxazolyl]phenyl]-, 1,1-dimethylethyl ester

(-20℃)

With Ice Pack

≥ 2 years