3-Methyladenine (3-MA) is a selective PI3K inhibitor for Vps34 and PI3Kγ with IC50 of 25 μM and 60 μM.

A novel mitochondrial and mTOR inhibitor with potent anti-cancer activity, inhibits leukemia cell lines with IC50 of 70-260 nM.

A novel potent, orally active 3-phosphoinositide-dependent kinase-1 (PDK-1) with IC50 of 2 uM.

A novel potent, pan-AMPK activator with similar potency for all AMPK heterotrimers.

A novel potent, selective, orally available PI3Kδ inhibitor with IC50 of 31 nM.

A novel specific p110β inhibitor with IC50 of 5.74 nM.

A novel VPS34 inhibitor.

A novel, potent, and selective p110δ PI3K inhibitor with IC50 of 0.1 nM in cell-based assays.

A potent, allosteric, α1-selective small molecule activator of AMPK (EC50=20 nM).

A potent, selective dual mTORC1 and mTORC2 inhibitor with enzyme IC50 of 1.5 nM.

A potent, selective, orally bioavailable PI3Kδ inhibitor with IC50 of 2.6 nM.

A66 is a potent and specific p110α inhibitor with IC50 of 32 nM, >100 fold selectivity for p110α over other class-I PI3K isoforms.

A-674563 is a potent, orally available Akt1 inhibitor with an IC50 value of 11nM. Also displays activity against PKA and CDK2 with IC50 values of 16nM and 46nM respectively.

A-769662 is a potent, reversible AMPK activator with EC50 of 0.8 μM, little effect on GPPase/FBPase activity.

Acadesine results in accumulation of ZMP, which mimics the stimulating effect of AMP on AMPK and AMPK kinase. Phase 3.

Acalisib (GS-9820) is a potent and selective inhibitor of PI3Kδ with IC50 value of 12.7 nM.

Afuresertib (GSK2110183) is a potent pan-AKT inhibitor that demonstrated synergy with bortezomib in preclinical models of multiple myeloma (MM).

Afuresertib (GSK2110183) is a potent, orally bioavailable Akt inhibitor with Ki of 0.08 nM, 2 nM, and 2.6 nM for Akt1, Akt2, and Akt3, respectively. Phase 2.

Akt Inhibitor VIII is a cell-permeable quinoxaline compound that has been shown to potently, selectively, allosterically, and reversibly inhibit Akt1, Akt2, and Akt3 activity (IC50 = 58 nM, 210 nM, and 2.12 μM; respectively).

Akt1 and Akt2-IN-1 is an allosteric inhibitor of Akt1 (IC50 = 3.5 nM) and Akt2 (IC50 = 42 nM), with potent and balanced activity.

AMG 319 is an investigational, highly selective, small molecule inhibitor of PI3Kδ that blocks B cell proliferation following BCR stimulation both in vitro and in vivo, inhibits basal AKT phosphorylation, and inhibits proliferation in lymphoid tumor cells

AMPK activator 991 is an allosteric AMPK activator, activates non-phosphorylated Thr172 AMPK in vitro binds to α1β1γ1 and α2β1γ1 with Kd of 0.13 and 0.17 uM, respectively..

AMPK activator SC4 is a potent, specific activator of α2β2-AMPK complexes with EC50 of 17.2 and 82.1 nM for α2β2γ1 and α2β2γ3, the predominant AMPK isoform complexes in human skeletal muscle.

An immunosuppressive agent and macrolide antibiotic.

Apilimod(STA 5326) is a potent IL-12/IL-23 inhibitor, IL-12 production in cultures of IFN-r/LPS–stimulated human PBMCs is strongly inhibited by STA-5326 with an IC50 of 10 nM.

APY0201 is a potent, highly selective PIKfyve kinase inhibitor.

ARQ 092 is an oral activie, potent and selective AKT inhibitor with IC50 values: 5.0 nM (AKT1); 4.5 nM (AKT2); 16 nM (AKT3).

AS-605240 is a potent and selective inhibitor of PI 3-kinase γ (PI3Kγ) (IC50 = 8 nM). AS-605240 displays 30-fold selectivity over PI3Kδ and PI3Kβ and 7.5-fold selectivity over PI3Kα.

AT7867 Hcl is a potent ATP-competitive inhibitor of Akt1/2/3 and p70S6K/PKA with IC50 of 32 nM/17 nM/47 nM and 85 nM/20 nM, respectively; little activity outside the AGC kinase family.

AT7867 is a potent ATP-competitive inhibitor of Akt1/2/3 and p70S6K/PKA with IC50 of 32 nM/17 nM/47 nM and 85 nM/20 nM, respectively; little activity outside the AGC kinase family.

Autophinib is a novel potent autophagy inhibitor, inhibiting autophagy induced by starvation or Rapamycin by targeting the lipid kinase VPS34.

AZD6482 is a PI3Kβ inhibitor with IC50 of 10 nM, 8-, 87- and 109-fold more selective to PI3Kβ than PI3Kδ, PI3Kα and PI3Kγ.

AZD-8055 is a potent, selective, and orally bioavailable ATP-competitive mTOR kinase inhibitor with an IC50 of 0.8 nM.

AZD8186 is an inhibitor of the beta isoform of phosphoinositide-3 kinase (PI3K), with potential antineoplastic activity.

AZD8835 ia a novel mixed inhibitor of PI3Kα and PI3Kδ with IC50 of 6.2 nM and 5.7 nM, respectively, also with selectivity against PI3Kβ (IC50=431 nM) and PI3Kγ (IC50=90 nM).

BAY 1082439 is a highly selective and balanced PI3Kα/β inhibitor demonstrated potent activity in tumors with activated PI3Kα and loss-of-function of PTEN.

BAY1125976 is a selective allosteric Akt1/2 inhibitor; inhibits Akt1 and Akt2 activity with IC50 values of 5.2 nM and 18 nM at 10 μM ATP, respectively.

BAY-3827 (BAY3827) is a potent, selective inhibitor of AMPK as tool compound to evaluate the therapeutic potential of AMPK inhibition in MYC-dependent tumors; strongly inhibits Acetyl-CoA carboxylase (ACC) phosphorylation in COLO 320DM and IMR-32 cells, but fails to inhibit the proliferation of cells with dysregulated c-MYC or N-MYC.

BEBT-908（CUDC-908）is a novel PI3K/HDAC inhibitor.

BEZ235 (NVP-BEZ235) is a dual ATP-competitive PI3K and mTOR inhibitor of p110α, p110γ, p110δ and p110β with IC50 of 4 nM, 5 nM, 7 nM and 75 nM, respectively, and also inhibits ATR with IC50 of 21 nM.

BKM120 is a selective PI3K inhibitor of p110α/β/δ/γ with IC50 of 52 nM/166 nM/116 nM/262 nM, respectively. Reduced potency against VPS34, mTOR, DNAPK, with little activity to PI4Kβ.

BX795 is a potent and selective dual inhibitor of TBK1/PDK1 with IC50s of 2 nM/6 nM respectively; > 50 fold selectivity over PKA, PKC, c-Kit, GSK3β etc.

BX-912 is a selective inhibitor of 3-Phosphoinositide-dependent Kinase-1 (PDK1) with IC50 of 12 nM; >10 fold selectivity over PKA, PKC, C-Kit, EGFR etc.

CAL-101 is a selective p110δ inhibitor with IC50 of 2.5 nM; shown to have 40- to 300-fold greater selectivity for p110δ thanp110α/β/γ, and 400- to 4000-fold more selectivity to p110δ than C2β, hVPS34, DNA-PK and mTOR.

CC-115 is a dual inhibitor of DNA-dependent protein kinase (DNA-PK) and mammalian target of rapamycin (mTOR), with potential antineoplastic activity.

CC-223 is a potent mTOR kinase inhibitor (IC50=16 nM), with >150-fold sensitivity over the related lipid kinase PI3Kα (IC50=4 μM).

Ch-319 (Ch319) is a triphenyltin (IV) carboxylate derivative that modulates AKT/FOXO3a signaling and inhibits progression of prostate cancer.

CZ415 is a potent and highly selective mTOR inhibitor.

Desmethyl VS-5584 is a PI3K/mTOR kinase inhibitor

Dorsomorphin 2Hcl (Compound C; BML-275) has been shown to act as a potent and selective inhibitor of AMPK (AMP-activated protein kinase; Ki = 109 nM), induced by AICAR and metformin; also inhibits ALK2, ALK3, and ALK 6 .

ETC-1002(ESP-55016) is a novel, first-in-class, orally available, once-daily LDL-C lowering small molecule; activator of hepatic AMP-activated protein kinase (AMPK); also has potent inhibitory activity against hepatic ATP-citrate lyase(IC50=29 uM).

ETP-46321 is a potent and orally bioavailable PI3K α/δ inhibitor with IC50 of 2.3/14.2 nM for p110α/p110β; exhibits potency on mutated p110α(IC50=1.77-2.33 nM, p110a E542K; E545K; H1047R).

Everolimus (RAD001) is an mTOR inhibitor of FKBP12 with IC50 of 1.6-2.4 nM.

EX229 is a small molecule AMPK activator that dose-dependently increases AMPK activity of α1-, α2-, β1- and β2-containing complexes at 50 uM

For the detailed information of GPI-1046, the solubility of GPI-1046 in water, the solubility of GPI-1046 in DMSO, the solubility of GPI-1046 in PBS buffer, the animal experiment (test) of GPI-1046, the cell expriment (test) of GPI-1046, the in vivo, in vitro and clinical trial test of GPI-1046, the EC50, IC50,and Affinity of GPI-1046, Please contact DC Chemicals..

GDC-0077 is an orally available PI3K inhibitor with potential antineoplastic activity. GDC-0077 is extracted from patent WO 2017001645 A1, formula I.

GDC-0084 （RG7666）, is a phosphatidylinositol 3-kinase (PI3K) inhibitor with potential antineoplastic activity.

GDC-0326 is a potent and selective inhibitor of α-Isoform of Phosphoinositide 3-Kinase (PI3Kalpha inhibitor).

GDC-0941 2 MeSO3H salt is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold).

GDC-0941 is a potent inhibitor of PI3Kα, PI3Kβ, PI3Kδ and PI3Kγ with IC50 of 3 nM, 33 nM, 3 nM and 75 nM, respectively.

GDC-0980 (RG7422) is a potent, class I PI3K inhibitor for PI3Kα/β/δ/γ with IC50 of 5 nM/27 nM/7 nM/14 nM, respectively. Also a mTOR inhibitor with Ki of 17 nM, and highly selective versus others PIKK family kinases.

GNE-317 is a potent, brain-penetrant PI3K inhibitor.

GNE-477 is a potent and efficacious dual PI3K/mTOR inhibitor with IC50 of 4 nM for PI3Kα, Kiapp is 21 nM for mTOR.

GNE-490 is a highly selective pan-PI3K inhibitor and demonstrates selectivity over mTOR.

GNE-493 is a potent, selective, and orally available dual pan-PI3K/mTOR inhibitor with IC50s of 3.4/12/16/16/32 nM for PI3Kα/PI3Kβ/PI3Kγ/PI3Kδ/mTOR respectively.

GSK1059615 is a dual inhibitor of PI3Kα/β/δ/γ (reversible) and mTOR with IC50 of 0.4 nM/0.6 nM/2 nM/5 nM and 12 nM, respectively.

GSK2126458 is a highly selective and potent inhibitor of PI3K with Ki of 0.019 nM/0.13 nM/0.024 nM/0.06 nM and 0.18 nM/0.3 nM for p110α/β/δ/γ, mTORC1/2 , respectively.

GSK-2269557 is a potent and selective PI3Kδ inhibitor over the closely related isoforms.

GSK2292767 is a potent and selective PI3Kδ inhibitor.

GSK690693 is a pan-Akt inhibitor targeting Akt1, Akt2 and Akt3 with IC50 of 2 nM, 13 nM, and 9 nM, respectively.

GSK-A1 is a potent inhibitor of PI4KA. In vitro using HEK-AT1 cells, GSK-A1 had an IC50 of about 3 nM.

HTH-01-015 is a selective inhibitor of NUAK1 kinase with an IC50 value of 100 nM.

IC-87114 was the first isoform-selective PI3K inhibitor. p110δ(IC50 = 0.13 μM) vs. p110α(IC50 = 200 μM), p110β(IC50 = 16 μM) and p110γ(IC50 = 61 μM).

ICSN3250 (ICSN-3250) hydrochloride is a halitulin-analogue that acts as a new-class, specific mTOR inhibitor through a mechanism distinct from previous mTOR inhibitors.

ICSN3250 (ICSN-3250) is a halitulin-analogue that acts as a new-class, specific mTOR inhibitor through a mechanism distinct from previous mTOR inhibitors.

INK 128 is a potent and selective mTOR inhibitor with IC50 of 1 nM; >200-fold less potent to class I PI3K isoforms.

INK055 is a dual PI3Kg/d inhibitor.

IPI-145 is an orally bioavailable, highly selective and potent small molecule inhibitor of the delta and gamma isoforms of phosphoinositide-3 kinase (PI3K) with potential immunomodulating and antineoplastic activities.

IPI-549 is an orally administered immuno-oncology development candidate that selectively inhibits PI3K-gamma.

KDU691 is a PI4K inhibitor.

KU-0063794 is a potent and highly specific mTOR inhibitor for both mTORC1 and mTORC2 with IC50 ~10 nM.

Leniolisib (CDZ173) is a potent and selective PI3Kδ inhibitor currently in phase II/III clinical trials for the treatment of immunodeficiency disorders.

LX-2343 is a novel non-ATP competitive PI3K inhibitor, negatively regulating AKT/mTOR signaling, thus promoting autophagy, and increasing A-beta clearance.

LY294002 is a PI3K inhibitor for p110α, p110δ and p110β with IC50 of 0.5 μM, 0.57 μM and 0.97 μM, respectively.

LY3023414 is an oral ATP competitive inhibitor of the class I PI3K isoforms, mTOR and DNA-PK.

LY303511, an inactive analogue of LY294002, is a mTOR inhibitor that did not inhibit PI3-K.

MELK-8a is a novel MELK inhibitor.

MELK-T1 is a potent and selective inhibitor of protein kinase MELK.

MK-2206 2HCl is a highly selective inhibitor of Akt1/2/3 with IC50 of 8 nM/12 nM/65 nM, respectively; no inhibitory activities against 250 other protein kinases observed. Phase 2.

MK-3903 is a potent and selective AMP-activated protein kinase (AMPK) activator with an EC50 of 8 nM. generation of catalytically active enzyme.

MK-8722 is a systemic, Direct Pan-Activator of AMP-Activated Protein Kinase.

MTX-211 is a dual inhibitor of EGFR and PI3K, used for the treatment of cancer and other diseases.

NVP-BAG956(BAG 956) is a potent, ATP-competitive and selective dual PI3K and PDK1 inhibitor in vitro and in vivo,with IC50 values to be 56, 444, 34, 117 and 240 nM for PI3K p110 alpha, beta, delta and gamma and PDK1 kinases, respectively.

NVP-BGT226 is a novel dual PI3K/mTOR inhibitor with IC50 of 1 nM.

NVP-BQR695 is a novel PI3K inhibitor.

OSI-027 is a selective and potent dual inhibitor of mTORC1 and mTORC2 with IC50 of 22 nM and 65 nM, respectively.

OSU-03012(AR-12) is a potent inhibitor of recombinant PDK-1 with IC50 of 5 μM and 2-fold increase in potency over OSU-02067.

OTSSP167 is a highly potent MELK inhibitor (IC50 = 0.41 nM) and inhibited the phosphorylation of PSMA1 (proteasome subunit alpha type 1) and DBNL (drebrin-like).

OTSSP167 is a highly potent MELK inhibitor (IC50 = 0.41 nM) and inhibited the phosphorylation of PSMA1 (proteasome subunit alpha type 1) and DBNL (drebrin-like).

PDK1 inhibitor is a potent and selective inhibitor of PDK1 with potential as anticancer agent..

Perifosine (KRX-0401) is a novel Akt inhibitor with IC50 of 4.7 μM.

PF-04979064 is a highly potent and orally bioavailable PI3K/mTOR dual inhibitor developed through structure-based drug design. It inhibited mTOR, PI3Kα, β, δ and γ isoforms and AKT phosphorylation with IC50 as 2.64 nM, 0.395 nM, 0.111 nM, 0.122 nM and 28.

PF-06409577 is a potent and selective allosteric activator of AMPK α1β1γ1 isoform with an EC50 of 7 nM.

PF-4989216 is a potent and selective PI3K inhibitor with IC50 of 2 nM, 142 nM, 65 nM, 1 nM, and 110 nM for p110α, p110β, p110γ, p110δ, and VPS34, respectively.

PHT-427 is a dual Akt and PDPK1 inhibitor (high affinity binding for the PH domains of Akt and PDPK1) with Ki of 2.7 μM and 5.2 μM, respectively.

PI103 is a potent inhibitor with low IC50 values against recombinant PI3K isoforms p110alpha (IC50= 2 nM), p110beta (IC50= 3 nM), p110delta (IC50= 3 nM), and p110gamma (IC50= 15 nM), less potent to mTOR/DNA-PK with IC50 of 30 nM/23 nM.

PI-3065 is a novel potent and selective PI3K p110δ inhibitor with IC50 of 15 nM; exhibits > 100 fold selectivity against p110α, p110β, p110γ, DNA-PK and mTOR.

PI3K-IN-2 is a PI3K inhibitor, inhibits pPKB and pS6 with "++++/+++(+)" in A2058 melanoma cell.

PIK-293 is a PI3K inhibitor, mostly for PI3Kδ with IC50 of 0.24 μM, 500-, 100- and 50-fold less potent to PI3Kα/β/γ, respectively.

PIK-294 is a highly selective p110δ inhibitor with IC50 of 10 nM, 1000-, 49- and 16-fold less potent to PI3Kα/β/γ, respectively.

PIK-90 is a potent and cell permeable inhibitor of p110α, p110β, p110γ and p110δ with IC50 of 11 nM, 350 nM, 18 nM and 58 nM, respectively.

PIK-93 is the first potent, synthetic PI4K (PI4KIIIβ) inhibitor with IC50 of 19 nM; shown to inhibit PI3Kα with IC50 of 39 nM.

PIK-III, which is a selective inhibitor of ​VPS34 enzymatic activity, inhibits autophagy and de novo lipidation of LC3 and leads to the stabilization of autophagy substrates.

PKI-402 is a potent dual pan-PI3K/mTOR inhibitor targeting PI3Kα/β/γ/δ and mTOR with IC50 of 2 nM/7 nM/16 nM/14 nM and 3 nM, respectively; also potent to PI3Kα mutants E545K and H1047R.

PKI-587 is a highly potent dual PI3K/mTOR kinase inhibitor with IC50 of 0.4 nM and <0.1 μM for PI3K-α and mTOR, respectively.

PP-121 is a multi-targeted inhibitor of PDGFR, Hck, mTOR, VEGFR2, Src and Abl with IC50 of 2 nM, 8 nM, 10 nM, 12 nM, 14 nM and 18 nM, also inhibits DNA-PK with IC50 of 60 nM.

PP242 is a selective mTOR inhibitor with IC50 of 8 nM; targets both mTOR complexes with >10- and 100-fold selectivity for mTOR than PI3Kδ or PI3Kα/β/γ, respectively; also showed slightly weaker activity against BRD4 (Kd= 1.7 uM).

PQR530 is a selective, orally bioavailable, potent dual PI3K/mTORC1/2 inhibitor.

RapaLink-1 is a third-generation mTOR inhibitor that overcomes resistance to existing first- and second-generation inhibitors; blocks mTOR signaling of the F2108L mTOR and M2327I mTOR drug resistant mutants; RapaLink-1 is more potent mTOR inhibitor than rapamycin.

Rapamycin (Sirolimus, AY-22989, WY-090217) is a specific mTOR inhibitor with IC50 of ~0.1 nM. -

SC-66 is an allosteric inhibitor of Akt; interferes with pleckstrin homology domain binding to PIP3 and facilitates Akt ubiquitination.

SC-79 is an activator of Akt; binds to the pleckstrin homology domain of Akt.

Seco-rapamycin(Secorapamycin A) is the first in vivo open-ring metabolite of rapamycin that does not affect mTOR..

Seletalisib (UCB5857) is potent and selective PI3Kδ inhibitor with an IC50 of 12 nM.

SF-1126 is a pan PI3K/BRD4 inhibitor, RGDS-conjugated LY294002 prodrug that exhibits increased solubility and binds to specific integrins.

SF2523 is a highly selective and potent inhibitor of PI3K and BRD4with IC50 values of 16 and 241 nM for PI3Kα and BD1, respectively.

SN-32976 is a novel, potent and selective class I PI3K and mTOR inhibitor with IC50 of 15.1/461/110/134/194 nM for PI3Kα/PI3Kβ/PI3Kγ/PI3Kδ/mTOR, respectively.

TAK-117(INK1117,MLN1117) is an orally bioavailable inhibitor of the class I phosphoinositide 3-kinase (PI3K) alpha isoform with potential antineoplastic activity.

Temsirolimus is an inhibitor of ribosomal protein S6 phosphorylation and inhibits cell growth and clonogenic survival of cells in a concentration-dependent manner.

Tenalisib (RP6530) is a novel, potent, and selective PI3Kδ and PI3Kγ inhibitor with IC50 values of 25 and 33 nM, respectively.

TG100115 is a PI3Kγ/δ inhibitor with IC50 of 83 nM/235 nM, with little effect on PI3Kα/β. Phase 1/2.

TGR-1202 hydrochloride is an orally available, next generation PI3Kdelta inhibitor, inhibits PI3Kδ activity in enzyme and cell based assays with IC50 and EC50 values of 22.2 and 24.3 nM respectively.

TGR-1202 is an orally available, next generation PI3Kdelta inhibitor, inhibits PI3Kδ activity in enzyme and cell based assays with IC50 and EC50 values of 22.2 and 24.3 nM respectively.

TGX-221 is a potent, selective, and cell permeable inhibitor of PI3K p110β .

The compound (Akt-I-1,2) inhibited both Akt1 and Akt2 with IC50 values of 2.7 and 21 μM respectively.

Torin 2 is a highly potent and selective mTOR inhibitor with IC50 of 0.25 nM, and also exhibits potent cellular activity against ATM/ATR/DNA-PK with EC50 of 28 nM, 35 nM and 118 nM, respectively.

Torin1 is a potent inhibitor of mTOR with IC50 of 2-10 nM.

UCB9608 is a Potent, Orally Bioavailable PI4KIIIβ Inhibitor.

UCT943 (UCT-943) is a potent, selective, next generation Plasmodium falciparum PI4K inhibitor with IC50 of 23 nM.

VO-Ohpic is a potent inhibitor of PTEN (phosphatase and tensin homolog) with IC50 of 35 nM.

Voxtalisib (SAR245409, XL765) Analogue is a dual inhibitor of mTOR/PI3K, mostly for p110γ with IC50 of 9 nM; also inhibits DNA-PK and mTOR.

Voxtalisib (SAR245409, XL765) is a dual inhibitor of mTOR/PI3K, mostly for p110γ with IC50 of 9 nM; also inhibits DNA-PK and mTOR.

VPS34 inhibitor 1 (Compound 19, PIK-III analogue) is a potent and selective inhibitor of VPS34 with an IC50 of 15 nM.

VPS34-IN1 is a potent and highly selective Vps34 inhibitor with IC50 of 25 nM invitro,which does not significantly inhibit the isoforms of class I as well as class II PI3Ks.

WYE125132 is a highly potent, ATP-competitive, and specific mTOR kinase inhibitor

XL147 analogue (SAR245408) is a selective and reversible class I PI3K inhibitor for wild type and mutant p110α with IC50 of 40 nM and 40 nM, respectively.

YM201636 is a selective PIKfyve inhibitor with IC50 of 33 nM, less potent to p110α.

ZLN024 Hcl is a novel AMPK allosteric activator; activated α1β1γ1 and α2β1γ1 by around 2–2.5 fold with an EC50 of about 1–2 uM. IC50 value: 1-2 uM (EC50) [1] Target: AMPK activator ZLN024 activated AMPK in L6 myotubes and stimulated glucose uptake and

ZSTK474 is a potent pan-class I PI3K inhibitor with IC50 of 37 nM.

Parsaclisib (INCB050465) is a potent, selective and orally active inhibitor of PI3Kδ, with an IC50 of 1 nM at 1 mM ATP. Parsaclisib shows approximately 20000-fold selectivity over other PI3K class I isoforms. Parsaclisib can be used for the research of relapsed or refractory B-cell malignancies.

Deforolimus(AP23573; MK-8669; Ridaforolimus) is a selective mTOR inhibitor with IC50 of 0.2 nM; while not classified as a prodrug, mTOR inhibition and FKBP12 binding is similar to rapamycin. IC50 value: 0.2 nM [1] Target: mTOR in vitro: Treatment of HT

Dorsomorphin(Compound C; BML-275) has been shown to act as a potent and selective inhibitor of AMPK (AMP-activated protein kinase; Ki = 109 nM), induced by AICAR and metformin; also inhibits the bone morphogenetic protein type 1 receptors ACTR-I (ALK2), B

PF-04691502 is an ATP-competitive PI3K(α/β/δ/γ)/mTOR dual inhibitor with Ki of 1.8 nM/2.1 nM/1.6 nM/1.9 nM and 16 nM, little activity against either Vps34, AKT, PDK1, p70S6K, MEK, ERK, p38, or JNK.

PDK1-IN-RS2 is a mimic of peptide docking motif (PIFtide) and is a substrate-selective PDK1 inhibitor with a Kd of 9 μM. PDK1-IN-RS2 suppresses the activation of the downstream kinases S6K1 by PDK1.

PI3K-IN-9 (compound 1-14) is a potent and selective PI3Kδ inhibitor with an IC50 of 8.9 nM.

CRTh2 antagonist 3 is a potent chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTh2) antagonist. CRTh2 antagonist 3 (compound 4) also enhances the activity of PDK1 toward a short peptide substrate, with an EC50 of 2 μM and a Kd of 8.4 μM. CRTh2 antagonist 3 has the potential for cardiovascular inflammation.

(R)-PS210, the R enantiomer of PS210 (compound 4h-eutomer), is a substrate-selective allosteric activator of PDK1 with an AC50 value of 1.8 μM. (R)-PS210 targets to the PIF-binding pocket of PDK1. PIF: The protein kinase C-related kinase 2 (PRK2)-interacting fragment.

Copanlisib dihydrochloride (BAY 80-6946 dihydrochloride) is a potent, selective and ATP-competitive pan-class I PI3K inhibitor, with IC50s of 0.5 nM, 0.7 nM, 3.7 nM and 6.4 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ, respectively. Copanlisib dihydrochloride has

FPA-124, a cell-permeable copper complex, is a selective Akt inhibitor with an IC50 of 0.1 μM. FPA-124 interacts with both the pleckstrin homology (PH) and the kinase domains of Akt. FPA-124 induces apoptosis.

PDK1/Akt/Flt Inhibitor 1 is a PI3-K/Akt pathway inhibitor.

GSK621 (GSK-621) is a potent, specific AMPK agonist (activator), induces cytotoxicity in AML (IC50=13-30 uM) but not in normal hematopoietic cells; GSK621 is more potent than A-769662 at inducing AMPK activation, as measured by the level of ACC phosphoryl

IM156, a metformin derivative, is a potent activator of AMPK that increases AMPK phosphorylation. IM156 blocks oxidative phosphorylation (OXPHOS) through the inhibition of complex I and increases apoptosis. IM156 ameliorates various types of fibrosis and

RSVA405 is a potent, orally active activator of AMPK, with an EC50 of 1 μM. RSVA405 facilitates CaMKKβ-dependent activation of AMPK, inhibits mTOR, and promotes autophagy to increase Aβ degradation. RSVA405 has anti-inflammatory effects through the inhibition of STAT3 function. RSVA405 also can be used for the research of obesity.

Metformin D6 hydrochloride is a deuterium labeled Metformin hydrochloride. Metformin hydrochloride inhibits the mitochondrial respiratory chain in the liver, leading to activation of AMPK, enhancing insulin sensitivity for type 2 diabetes research. Metformin hydrochloride triggers autophagy.

BpV(HOpic) is a potent and selective inhibitor of PTEN with an IC50 of 14 nM. Nanocarrier-BpV(HOpic) has neuroprotective activity.

TG 100713 is an inhibitor of PI3K, with IC50s of 24, 50, 165, and 215 nM for PI3Kδ, γ, α and β isoforms respectively.

MSC2360844 is a potent, orally active and selective PI3Kδ inhibitor, with an IC50 of 145 nM. MSC2360844 shows highly selective against a panel of 278 additional kinases.

MSC2360844 hemifumarate is a potent, orally active and selective PI3Kδ inhibitor, with an IC50 of 145 nM. MSC2360844 hemifumarate shows highly selective against a panel of 278 additional kinases.

bpV(phen) hydrate is a potent protein tyrosine phosphatase (PTP) and PTEN inhibitor with IC50s of 38 nM, 343 nM and 920 nM for PTEN, PTP-β and PTP-1B, respectively. bpV(phen) hydrate inhibits proliferation of the protozoan parasite Leishmania in vitro. bpV(phen) hydrate strongly induces the secretion of a large number of chemokines and pro-inflammatory cytokines, and it activates a Th1-type pathway (IL-12, IFNγ). bpV(phen) hydrate can also induce cell apoptosis, and has anti-angiogenic and anti-tumor activity.

PQR626 is an orally available, and brain-penetrant mTOR inhibitor extracted from patent WO2017198346A1, compound example 44, has an IC50 of 5 nM for mTOR. PQR626 can be used for the research of neurological disorder.

Quercetin D5 is a deuterium labeled Quercetin. Quercetin, a natural flavonoid, is a stimulator of recombinant SIRT1 and also a PI3K inhibitor with IC50 of 2.4 μM, 3.0 μM and 5.4 μM for PI3K γ, PI3K δ and PI3K β, respectively.

Buformin (1-Butylbiguanide) is a potent and orally active biguanide antidiabetic agent, an?AMPK?activator. Buformin decreases hepatic gluconeogenesis and lowers blood glucose production in vivo. Buformin also has anti-cancer activities and is applied in cancer study (such as, cervical cancer and breast cancer, et al).

Hirsutenone is an active botanical diarylheptanoid present in Alnus species and exhibits many biological activities, including anti-inflammatory, anti-tumor promoting and anti-atopic dermatitis effects. Hirsutenone attenuates adipogenesis by binding directly to PI3K and ERK1 in a non-ATP competitive manner. Hirsutenone can be used for the study of obesity.

Marein has the neuroprotective effect due to a reduction of damage to mitochondria function and activation of the AMPK signal pathway. Marein improves insulin resistance induced by high glucose in HepG2 cells through CaMKK/AMPK/GLUT1 to promote glucose uptake, through IRS/Akt/GSK-3β to increase glycogen synthesis, and through Akt/FoxO1 to decrease gluconeogenesis. Marein is a HDAC inhibitor with an IC50 of 100 μM. Marein has beneficial antioxidative, antihypertensive, antihyperlipidemic and antidiabetic effects.

AKTide-2T is an excellent in vitro substrate for AKT and shows competitive inhibition of histone H2B phosphorylation with a Ki of 12 nM. AKTide-2T mimics the optimal phosphorylation sequence of Akt and is an inhibitory peptide with the wildtype AKTide lacking Thr in the S22 position.

AKTide-2T TFA is an excellent in vitro substrate for AKT and shows competitive inhibition of histone H2B phosphorylation with a Ki of 12 nM. AKTide-2T TFA mimics the optimal phosphorylation sequence of Akt and is an inhibitory peptide with the wildtype AKTide lacking Thr in the S22 position.

MOTS-c(human) acetate is a mitochondrial-derived peptide. MOTS-c(human) acetate induces the accumulation of AMP analog AICAR, increases activation of AMPK and expression of its downstream GLUT4. MOTS-c(human) acetate induces glucose uptake and improves insulin sensitivity. MOTS-c(human) acetate has implications in the regulation of obesity, diabetes, exercise, and longevity.

Zandelisib is a phosphatidylinositol 3-kinase (PI3K) extracted from patent WO2019183226 A1, Compound Example 1. Zandelisib selectively inhibits p110δ with an IC50 of 3.5 nM. Zandelisib functions as an antineoplastic.

IHMT-PI3Kδ-372 is a potent and selective PI3Kδ with an IC50 of 14 nM. IHMT-PI3Kδ-372 shows high selectivity over other class I PI3Ks (56∼83 fold) and other protein kinases. IHMT-PI3Kδ-372 can be uesd for chronic obstructive pulmonary disease (COPD) research.

PI3Kδ-IN-8 is a potent, selective and orally active PI3Kδ, with an IC50 of 3.3 nM. PI3Kδ-IN-8 shows selectivity for PI3Kδ over PI3Kα, PI3Kβ, and PI3Kγ (IC50=377.2, 241.6, 17.9 nM, respectively). PI3Kδ-IN-8 has anti-tumor activity.

AMPK activator 4 is a potent AMPK activator without inhibition of mitochondrial complex I. AMPK activator 4 selectively activates AMPK in the muscle tissues. AMPK activator 4 dose-dependently improves glucose tolerance in normal mice, and significantly lowers fasting blood glucose level and ameliorates insulin resistance in db/db diabetic mice. Anti-hyperglycemic effect.

Parsaclisib hydrochloride (INCB050465 hydrochloride) is a potent, selective and orally active inhibitor of PI3Kδ, with an IC50 of 1 nM at 1 mM ATP. Parsaclisib hydrochloride shows approximately 20000-fold selectivity over other PI3K class I isoforms. Parsaclisib hydrochloride can be used for the research of relapsed or refractory B-cell malignancies.

mTOR inhibitor-8 is an mTOR inhibitor and autophagy inducer. mTOR inhibitor-8 inhibits the activity of mTOR via FKBP12 and induces autophagy of A549 human lung cancer cells.

(S)-PI3Kα-IN-4 is a potent inhibitor of PI3Kα, with an IC50 of 2.3 nM. (S)-PI3Kα-IN-4 shows 38.3-, 4.25-, and 4.93-fold selectivity for PI3Kα over PI3Kβ, PI3Kδ, and PI3Kγ, respectively. (S)-PI3Kα-IN-4 can be used for the research of cancer.

PI3Kα-IN-4 is a potent, selective and orally active inhibitor of PI3Kα, with an IC50 of 1.8 nM. PI3Kα-IN-4 has antitumor activity.

PF-06843195 is a highly selective PI3Kα inhibitor with an IC50 of 18 nM in Rat1 fibroblasts. The Kis of PF-06843195 for PI3Kα and PI3Kδ in biochemical kinase assay are less than 0.018 nM and 0.28 nM, respectively. PF-06843195 has great suppression of the PI3K/mTOR signaling pathway and durable antitumor efficacy.

Metformin (1,1-Dimethylbiguanide), a widely used drug for treatment of type 2 diabetes, activates AMP-activated protein kinase (AMPK) in hepatocytes. Metformin promotes mitophagy in mononuclear cells. Metformin induces apoptosis of lung cancer cells throu

RMC-5552 is a potent and selective inhibitor of mTORC1. RMC-5552 inhibits phosphorylation of mTORC1 pS6K and p4EBP1 with IC50s of 0.14 nM and 0.48 nM, respectively. RMC-5552 has anti-cancer activity.

AS-041164 is a potent, selective and orally active PI3Kγ isoform inhibitor with an IC50 of 70 nM. AS-041164 shows less activity against PI3Kα, PI3Kβ, and PI3Kδ (IC50s of 240 nM, 1.45 μM, and 1.70 μM, respectively). AS-041164 has anti-inflammatory effects.

(E)-Akt inhibitor-IV ((E)-AKTIV) is a PI3K-Akt inhibitor, with potent cytotoxic.

Galegine hydrochloride, a guanidine derivative, contributes to weight loss in mice. Guanidine hydrochloride is the compound derived from G. officinalis, which gave rise to the biguanides, metformin and phenformin. Galegine hydrochloride activates AMPK in 3T3-L1 adipocytes and L6 myotubes, as well as in the H4IIE rat hepatoma and HEK293 human kidney cell lines. Galegine hydrochloride has antibacterial activity, with minimum inhibitory concentration of 4 mg/L against Staphylococcus aureus strains.

24-Methylenecycloartanyl ferulate is a γ-oryzanol compound. 24-Methylenecycloartanyl ferulate promotes parvin-beta expression in human breast cancer cells. 24-Methylenecycloartanyl ferulate is a potential ATP-competitive Akt1 inhibitor (EC50= 33.3μM).

NVS-PI3-4 is a specific PI3Kγ inhibitor. NVS-PI3-4 can be used for the research of allergies, inflammatory and cancer diseases.

PKI-179 is a potent and orally active dual PI3K/mTOR inhibitor, with IC50s of 8 nM, 24 nM, 74 nM, 77 nM, and 0.42 nM for PI3K-α, PI3K-β, PI3K-γ, PI3K-δ and mTOR, respectively. PKI-179 also exhibits activity over E545K and H1047R, with IC50s of 14 nM and 11 nM, respectively. PKI-179 shows anti-tumor activity in vivo.

FD223 is a potent and selective phosphoinositide 3-kinase delta (PI3Kδ) inhibitor. FD223 displays high potency (IC50=1 nM) and good selectivity over other isoforms (IC50s of 51 nM, 29 nM and 37 nM, respectively for α, β and γ). FD223 exhibits efficient inhibition of the proliferation of acute myeloid leukemia (AML) cell lines by suppressing p-AKT Ser473 thus causing G1 phase arrest during the cell cycle. FD223 has potential for the research of leukemia such as AML.

PKI-179 hydrochloride is a potent and orally active dual PI3K/mTOR inhibitor, with IC50s of 8 nM, 24 nM, 74 nM, 77 nM, and 0.42 nM for PI3K-α, PI3K-β, PI3K-γ, PI3K-δ and mTOR, respectively. PKI-179 hydrochloride also exhibits activity over E545K and H1047R, with IC50s of 14 nM and 11 nM, respectively. PKI-179 hydrochloride shows anti-tumor activity in vivo.

AZ2 is a highly selective PI3Kγ inhibitor. AZ2 can be used for the research of inflammatory and immune diseases.

PP2A Cancerous-IN-1 is a strong and potent CIP2A (Cancerous inhibitor of PP2A) and p-Akt inhibitor. PP2A Cancerous-IN-1 shows the most potent antiproliferative activities.

Malvidin-3-O-arabinoside chloride ameliorates ethyl carbamate-induced oxidative damage by stimulating AMPK-mediated autophagy.

PI3K-IN-20 is a PI3k inhibitor extracted from WO2017101847 A1, compound 1.