API-1, a potent Akt/PKB inhibitor, binds to the PH domain and inhibits Akt membrane translocation. API-1 efficiently reduces the phosphorylation levels of Akt with an IC50 of ∼0.8 μM. API-1 is selective for PKB and does not inhibit the activation of PKC, and PKA. API-1 also induces apoptosis by synergizing with TNF-related apoptosis-inducing ligand (TRAIL)[1][2].
分子量
337.29
Formula
C13H15N5O6
CAS 号
36707-00-3
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Donghwa Kim, et al. A small molecule inhibits Akt through direct binding to Akt and preventing Akt membrane translocation. J Biol Chem. 2016 Oct 21;291(43):22856.
[2]. Donghwa Kim, et al. A small molecule inhibits Akt through direct binding to Akt and preventing Akt membrane translocation. J Biol Chem. 2016 Oct 21;291(43):22856.
API-1, a potent Akt/PKB inhibitor, binds to the PH domain and inhibits Akt membrane translocation. API-1 efficiently reduces the phosphorylation levels of Akt with an IC50 of ∼0.8 μM. API-1 is selective for PKB and does not inhibit the activation of PKC, and PKA. API-1 also induces apoptosis by synergizing with TNF-related apoptosis-inducing ligand (TRAIL)[1][2].
分子量
337.29
Formula
C13H15N5O6
CAS 号
36707-00-3
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Donghwa Kim, et al. A small molecule inhibits Akt through direct binding to Akt and preventing Akt membrane translocation. J Biol Chem. 2016 Oct 21;291(43):22856.
[2]. Donghwa Kim, et al. A small molecule inhibits Akt through direct binding to Akt and preventing Akt membrane translocation. J Biol Chem. 2016 Oct 21;291(43):22856.
API-1, a potent Akt/PKB inhibitor, binds to the PH domain and inhibits Akt membrane translocation. API-1 efficiently reduces the phosphorylation levels of Akt with an IC50 of ∼0.8 μM. API-1 is selective for PKB and does not inhibit the activation of PKC, and PKA. API-1 also induces apoptosis by synergizing with TNF-related apoptosis-inducing ligand (TRAIL)[1][2].
分子量
337.29
Formula
C13H15N5O6
CAS 号
36707-00-3
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Donghwa Kim, et al. A small molecule inhibits Akt through direct binding to Akt and preventing Akt membrane translocation. J Biol Chem. 2016 Oct 21;291(43):22856.
[2]. Donghwa Kim, et al. A small molecule inhibits Akt through direct binding to Akt and preventing Akt membrane translocation. J Biol Chem. 2016 Oct 21;291(43):22856.
PIN1 inhibitor API-1 is a specific Pin1 (peptidyl-prolyl cis–trans isomerase NIMA-interacting 1) inhibitor (API-1) with an IC50 of 72.3 nM. PIN1 inhibitor API-1 directly and specifically binds to the Pin1 peptidyl-prolyl isomerase (PPIase) domain and potently inhibits Pin1 cis–trans isomerizing activity. PIN1 inhibitor API-1 retains the active conformation of pXPO5 and restores the ability of pXPO5 to transport pre-miRNAs from nucleus to cytoplasm, thus up-regulating the anticancer miRNA biogenesis to suppress both in vitro and in vivo hepatocellular carcinoma development[1].
IC50 & Target
IC50: 72.3 nM (Pin1)[1]
体外研究 (In Vitro)
PIN1 inhibitor API-1 obviously inhibits SK-Hep-1, SNU-423, and Hep3B cell proliferation with low IC50 values (IC50=0.683-4.16 μM)[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)
PIN1 inhibitor API-1 suppresses tumor growth in mice by up-regulating mature miRNA biogenesis[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
366.30
Formula
C15H13F3N6O2
CAS 号
680622-70-2
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Pu W, et al. Targeting Pin1 by inhibitor API-1 regulates microRNA biogenesis and suppresses hepatocellularcarcinoma development. Hepatology. 2018 Aug;68(2):547-560.