mTOR is a serine/threonine kinase and the catalytic subunit of the mTORC1 and mTORC2 complexes. mTORC1 is involved in energy homeostasis signaling. Akt phosphorylation regulates TSC2, inhibiting the activity of the TSC1/TSC2 heterodimer, relieving its suppression of mTORC1 and sustaining activation. mTORC2 is involved in cell survival, responsible for phosphorylating Akt, activating it, and triggering anti-apoptotic effects. mTOR inhibitors have therapeutic benefits in the treatment of cancers.

Figure 1 Chemical structure of PP-242
Name | ID |
Aloe-emodin | |
AZD2014 | |
AZD-8055 | |
BEZ235 | |
Curcumin | |
Emodin | |
Everolimus | |
GDC-0980 | |
GSK2126458 | |
INK128 | |
MHY-1685 | |
NVP-BGT226 | |
OSI-027 | |
PF-04691502 | |
PKI-402 | |
PP-242 | |
Rapamycin | |
Sunitinib Malate | |
Temsirolimus | |
Torin 1 | |
Torin 2 | |
Triacetyl Aloe-emodin |
PI3K
PI3Ks are a class of enzymes responsible for generating phosphatidylinositol-3-phosphate (PIP) and its derivatives (such as PIP2 and PIP3). PI3Ks are divided into three classes, with class I PI3Ks primarily involved in cell survival signaling. Class I PI3Ks consist of a p85 regulatory subunit and a p110 catalytic subunit. Growth factors and survival factor receptor tyrosine kinases activate PI3Ks, promoting the generation of PIP3 and activating Akt in conjunction with mTOR. Specific isoforms of the p110 subunit of class I PI3Ks are being investigated as novel targets for anticancer compounds.

Figure 2 Chemical structure of BKM120

Figure 3 Chemical structure of CUDC - 907
Name | ID |
A66 | |
Apigenin | |
AS-252424 | |
BAY80-6946 | |
BEZ235 | |
BKM120 | |
BYL719 | |
CAL101 | |
CUDC-907 | |
GDC-0032 | |
GSK2636771 | |
GDC-0980 | |
GSK2126458 | |
LY294002 | |
3-Methyladenine | |
PF-04691502 | |
Piceatannol | |
PKI-402 | |
PP-121 | |
PX-866 | |
Wogonin | |
Wortmannin | |
ZSTK474 |
AKT
Akt is a serine/threonine kinase involved in anti-apoptotic signaling. Akt inhibits pro-apoptotic protein Bad through phosphorylation and inactivation, and regulates IκB kinase activity, activating NF-κB and promoting expression of anti-apoptotic genes. The tumor suppressor protein PTEN suppresses Akt activation by dephosphorylating PIP3. Akt activity is closely linked to cancer progression and tumor development.

Figure 4 Chemical structure of Pelitinib
Name | ID |
AZD5363 | |
Canertinib 2HCl | |
CCT-128930 | |
Curcumin | |
Dacomitinib | |
Gabexate Mesylate | |
Gambogic Acid | |
GDC-0068 | |
Goserelin | |
GSK-690693 | |
MK2206 | |
Nitidine Chloride | |
Pelitinib | |
Perifosine | |
PHT-427 | |
Piceatannol | |
SU-1498 | |
Tandutinib | |
Withaferin A |
PDK1
PDK1 is a key enzyme in the PI3K-Akt signaling pathway that regulates AGC protein kinase activity and is involved in cell survival, metabolism, and tumorigenesis. Targeting PDK1 with small molecule inhibitors can delay tumor growth and metastasis.
Name | ID |
BX-795 | |
BX-12 | |
GSK-2334470 | |
OSU-03012 | |
PHT-427 |
Aladdin: https://www.aladdinsci.com/
