Search Result
Results for "
mTOR kinase inhibitor
" in MedChemExpress (MCE) Product Catalog:
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-16956
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CC-223; ATG-008
|
mTOR
Apoptosis
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Cancer
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Onatasertib (CC-223) is a potent, selective, and orally bioavailable inhibitor of mTOR kinase, with an IC50 value for mTOR kinase of 16 nM. Onatasertib inhibits both mTORC1 and mTORC2.
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-
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- HY-153120A
-
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PI3K
mTOR
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Cancer
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PI3K/mTOR Inhibitor-13 sodium is an orally active dual inhibitor of phosphoinositol 3-kinase (PI3K) and mTOR kinase. PI3K/mTOR Inhibitor-13 sodium has potential applications in sexual diseases, solid tumor and idiopathic pulmonary fibrosis (IPF) .
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-
-
- HY-13328
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INK-128; MLN0128; TAK-228
|
mTOR
Autophagy
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Cancer
|
Sapanisertib (INK-128; MLN0128; TAK-228) is an orally available, ATP-dependent mTOR1/2 inhibitor with an IC50 of 1 nM for mTOR kinase.
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-
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- HY-109633
-
|
mTOR
PI3K
|
Cancer
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PI3K-IN-18 (Compound 1) is a PI3K inhibitor, and can also effectively inhibit the homologous enzymemTOR. The IC50 values of PI3K-IN-18 for mTOR and PI3K-α were 49 nM and 41 nM, respectively .
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-
-
- HY-100398
-
|
PI3K
mTOR
|
Cancer
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PF-04979064 is a potent and selective PI3K/mTOR dual kinase inhibitor with Kis of 0.13 nM and 1.42 nM for PI3Kα and mTOR, respectively.
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-
-
- HY-111373
-
|
mTOR
Autophagy
|
Cancer
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RapaLink-1, the third-generation bivalent mTOR inhibitor, combines Rapamycin (HY-10219) with MLN0128 (HY-13328, a second-generation mTOR kinase inhibitor) by an inert chemical linker. RapaLink-1 shows better efficacy than Rapamycin or mTOR kinase inhibitors (TORKi), potently blocking cancer-derived, activating mutants of mTOR. RapaLink-1 can cross the blood-brain barrier. RapaLink-1 binding to FKBP12 results in targeted and durable inhibition of mTORC1. RapaLink-1 plays an antithrombotic role in antiphospholipid syndrome by improving autophagy. Anticancer activity .
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-
- HY-10372
-
PP121
3 Publications Verification
|
mTOR
PDGFR
VEGFR
Src
Apoptosis
|
Cancer
|
PP121 is a multi-targeted kinase inhibitor with IC50s of 10, 60, 12, 14, 2 nM for mTOR, DNK-PK, VEGFR2, Src, PDGFR, respectively.
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-
-
- HY-153120
-
|
PI3K
mTOR
|
Cancer
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PI3K/mTOR Inhibitor-13 is an orally active dual inhibitor of phosphoinositol 3-kinase (PI3K) and mTOR kinase. PI3K/mTOR Inhibitor-13 has potential applications in sexual diseases, solid tumor and idiopathic pulmonary fibrosis (IPF) .
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-
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- HY-116191
-
|
PI3K
mTOR
|
Cancer
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WJD008 is a potent dual phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitor with antiproliferative and anticlonogenic activity in tumor cells and transformed cells with PIK3CA mutant. WJD008 inhibits kinase activity of PI3K α and mTOR and abrogates insulin-like growth factor-I-activated PI3K-Akt-mTOR signaling cascade. WJD008 is promising for research of cancers .
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- HY-161509
-
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mTOR
|
Cancer
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PT-88 is a highly selective inhibitor of mTOR (Mammalian target of rapamycin) (IC50=1.2 nM). PT-88 inhibits both mTORC1 and mTORC2 complexes, both of which are active forms of mTOR protein kinases and are closely associated with cell growth, proliferation, and survival. PT-88 can be used to study the role of mTOR in tumorigenesis and development, especially in the treatment of breast cancer .
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- HY-154910
-
|
mTOR
|
Cancer
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CC214-1 is a potentially efficacious mTOR inhibitor that induces autophagy ,with an IC50 is 0.002 μM. CC214-1 proved to be useful as an in vitro tool compound for the exploration of mTOR kinase biology. CC214-1 can be used for Glioblastoma study .
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- HY-10422
-
|
mTOR
Autophagy
Apoptosis
|
Cancer
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AZD-8055 is a potent, selective, and orally bioavailable ATP-competitive mTOR kinase inhibitor with an IC50 of 0.8 nM. AZD-8055 inhibits both mTORC1 and mTORC2 .
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- HY-P10323
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Tumstatin (74-98), human
|
Integrin
FAK
mTOR
Apoptosis
|
Cancer
|
T7 peptide is an endothelial cell-specific inhibitor. T7 peptide interacts with αVβ3 integrin to inhibit the FAK, PI3-kinase, PKB/Akt, and mTOR signaling pathways in endothelial cells, ultimately suppressing protein synthesis and inducing apoptosis .
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- HY-16962
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CC-115
2 Publications Verification
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DNA-PK
mTOR
|
Cancer
|
CC-115 is a potent and dual DNA-PK and mTOR kinase inhibitor with IC50s of 13 nM and 21 nM, respectively. CC-115 blocks both mTORC1 and mTORC2 signaling.
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- HY-16962A
-
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DNA-PK
mTOR
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Cancer
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CC-115 hydrochloride is a potent and dual DNA-PK and mTOR kinase inhibitor with IC50s of 13 nM and 21 nM, respectively. CC-115 blocks both mTORC1 and mTORC2 signaling.
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- HY-117923
-
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mTOR
PI3K
|
Cancer
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PF-06465603 is a highly potent and selective ATP-competitive kinase inhibitor and a class 1 PI3K and mTOR inhibitor. PF-06465603 is a metabolite of PF-04691502 with a terminal carboxylic acid structure .
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- HY-10811
-
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PI3K
mTOR
|
Cancer
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GNE-493 is a potent, selective, and orally available dual pan-PI3-kinase/mTOR inhibitor with IC50s of 3.4 nM, 12 nM, 16 nM, 16 nM and 32 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ and mTOR.
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- HY-13246
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GDC-0980; GNE 390; RG 7422
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PI3K
mTOR
Apoptosis
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Cancer
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Apitolisib (GDC-0980; GNE 390; RG 7422) is a selective, potent, orally bioavailable Class I PI3 kinase and mTOR kinase (TORC1/2) inhibitor with IC50s of 5 nM/27 nM/7 nM/14 nM for PI3Kα/PI3Kβ/PI3Kδ/PI3Kγ, and with a Ki of 17 nM for mTOR.
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-
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- HY-15174
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BEZ235 Tosylate; NVP-BEZ 235 Tosylate
|
PI3K
mTOR
Autophagy
|
Cancer
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Dactolisib Tosylate (BEZ235 Tosylate) is a dual PI3K and mTOR kinase inhibitor with IC50 values of 4, 75, 7, 5 nM for PI3Kα, β, γ, δ, respectively. Dactolisib Tosylate (BEZ235 Tosylate) inhibits mTORC1 and mTORC2.
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- HY-N10754
-
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mTOR
Cytochrome P450
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Infection
Cardiovascular Disease
Cancer
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Aschantin, a bisepoxylignan, can be isolated from Magnolia biondii. Aschantin has antiplasmodial, Ca 2+-antagonistic, platelet activating factor-antagonistic, and chemopreventive activities. Aschantin is a mTOR kinase inhibitor. Aschantin is also an inhibitor of Cytochrome P450 and UGT enzyme .
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- HY-16585
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VS-5584
5 Publications Verification
SB2343
|
PI3K
mTOR
|
Cancer
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VS-5584 is a pan-PI3K/mTOR kinase inhibitor with IC50s of 16 nM, 68 nM, 42 nM, 25 nM, and 37 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ and mTOR, respectively. VS-5584 simultaneously blocks mTORC2 as well as mTORC1.
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- HY-10971A
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MLN 8237 sodium
|
Aurora Kinase
Autophagy
Apoptosis
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Cancer
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Alisertib (MLN 8237) sodium is an orally active and selective Aurora A kinase inhibitor (IC50=1.2 nM), which binds to Aurora A kinase resulting in mitotic spindle abnormalities, mitotic accumulation. Alisertib sodium induces apoptosis and autophagy through targeting the AKT/mTOR/AMPK/p38 pathway in leukemic cells. Antitumor activity .
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-
- HY-50673
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Dactolisib
Maximum Cited Publications
56 Publications Verification
BEZ235; NVP-BEZ235
|
PI3K
mTOR
Autophagy
|
Cancer
|
Dactolisib (BEZ235) is an orally active and dual pan-class I PI3K and mTOR kinase inhibitor with IC50s of 4 nM/5 nM/7 nM/75 nM, and 20.7 nM for p110α/p110γ/p110δ/p110β and mTOR, respectively. Dactolisib (BEZ235) inhibits both mTORC1 and mTORC2.
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- HY-10971
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MLN 8237
|
Aurora Kinase
Autophagy
Apoptosis
|
Cancer
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Alisertib (MLN 8237) is an orally active and selective Aurora A kinase inhibitor (IC50=1.2 nM), which binds to Aurora A kinase resulting in mitotic spindle abnormalities, mitotic accumulation. Alisertib (MLN 8237) induces apoptosis and autophagy through targeting the AKT/mTOR/AMPK/p38 pathway in leukemic cells. Antitumor activity .
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-
- HY-10620
-
|
PI3K
mTOR
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Cancer
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PI3K-IN-22 is a PI3Kα/mTOR dual kinase inhibitor. PI3K-IN-22 has IC50s of 0.9, 0.6 nM for PI3Kα and mTOR, respectively. PI3K-IN-22 can be used for the research of cancer .
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- HY-123849
-
|
PI3K
mTOR
|
Cancer
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SN32976 is a potent and selective class I PI3K and mTOR inhibitor with IC50s of 15.1 nM, 461 nM, 110 nM, 134 nM and 194 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ and mTOR, respectively. SN32976 shows high selectivity among other 442 kinases. SN32976 shows anticancer effects .
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- HY-10423
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ASP7486
|
mTOR
Autophagy
|
Cancer
|
OSI-027 (ASP7486) is a potent, selective, orally active and ATP-competitive mTOR kinase activity inhibitor with an IC50 of 4 nM. OSI-027 targets both mTORC1 and mTORC2 with IC50s of 22 nM and 65 nM, respectively .
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- HY-144687
-
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ATM/ATR
PI3K
mTOR
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Cancer
|
ATM Inhibitor-4 (compound 39) is a potent and selective ATM inhibitor, with an IC50 of 0.32 nM. ATM Inhibitor-4 shows stronger inhibition of PI3K kinases family. ATM Inhibitor-4 shows a full inhibition of mTOR at 1 μM. ATM Inhibitor-4 exhibits favorable metabolic stability .
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-
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- HY-162143
-
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SphK
Akt
mTOR
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Cancer
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SKI-349 is a dual-targeted inhibitor of sphingosine kinase 1/2 (SPHK1/2) and microtubule assembly (MDA). SKI-349 has anticancer activity. SKI-349 can inhibit the vitality, invasion, and AKT/mTOR signaling pathway of liver cells .
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- HY-10044
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WYE-125132
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mTOR
Apoptosis
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Cancer
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WYE-132 (WYE-125132) is a highly potent, ATP-competitive, and specific mTOR kinase inhibitor (IC50: 0.19±0.07 nM; >5,000-fold selective versus PI3Ks). WYE-132 (WYE-125132) inhibits mTORC1 and mTORC2.
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-
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- HY-139609
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RP-3500; ATR inhibitor 4
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ATM/ATR
mTOR
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Cancer
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Camonsertib (RP-3500) is an orally active, selective ATR kinase inhibitor (ATRi) with an IC50 of 1.00 nM in biochemical assays. Camonsertib shows 30-fold selectivity for ATR over mTOR (IC50=120 nM) and >2,000-fold selectivity over ATM, DNA-PK, and PI3Kα kinases. Camonsertib has potent antitumor activity .
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- HY-15901A
-
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Pim
mTOR
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Cancer
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LGB321 monohydrochloride is a potent, selective, orally active and ATP competitive inhibitor of all three PIM kinases. LGB321 monohydrochloride inhibits proliferation, mTOR-C1 signaling and phosphorylation of BAD in a number of cell lines derived from diverse hematologic malignancies. LGB321 monohydrochloride can be used for the research of hematologic malignancies .
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- HY-126077
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LXI-15029
|
mTOR
|
Inflammation/Immunology
Cancer
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MTI-31 (LXI-15029) is a potent, orally active and highly selective inhibitor of mTORC1 and mTORC2. MTI-31 is selective for mTOR (Kd: 0.20 nM) versus PIK3CA, PIK3CB and PIK3G with >5,000 fold selectivity in mTOR binding assays. MTI-31 shows an IC50 of 39 nM for mTOR in LANCE assay of mTOR substrate phosphorylation with 100 μM ATP. MTI-31 can be used for the research of breast cancer .
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- HY-164460
-
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Pim
|
Cancer
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AZD1897 is a PIM1, PIM2, and PIM3 inhibitor with IC50 values of less than 3 nM for these three PIM kinases. AZD1897 exhibits anticancer activity and synergistically inhibits the activity of acute myeloid leukemia (AML) cells in combination with Capivasertib (HY-15431). This synergistic inhibitory effect is achieved through the inhibition of the mTOR and MCL1 pathways .
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- HY-N1050
-
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mTOR
|
Cancer
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Zederone, a germacrane-type sesquiterpene, has potently cytotoxic against human white blood cancer cells and human prostate cancer cells. Zederone significantly inhibits the proliferation and downregulates the protein expressions of mTOR, and phosphorylated p70 S6 kinase (p-p70s6K) in SKOV3 cells .
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-
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- HY-124760
-
|
mTOR
PI3K
CDK
|
Cancer
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hSMG-1 inhibitor 11e is a potent and selective hSMG-1 kinase inhibitor with an IC50 of <0.05 nM. hSMG-1 inhibitor 11e shows >900-fold selectivity over mTOR (IC50 of 45 nM), PI3Kα/γ (IC50s of 61 nM and 92 nM) and CDK1/CDK2 (IC50s of 32 μM and 7.1 μM) .
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-
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- HY-144059
-
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Akt
|
Cancer
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AKT-IN-9 is a potent inhibitor of AKT. Protein kinase B (PKB, also known as AKT) is central to PI3K/AKT/mTOR signaling in cells, and its function is important for cell growth, survival, differentiation and metabolism. AKT-IN-9 has the potential for the research of breast and prostate cancer (extracted from patent WO2021185238A1, compound 1) .
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- HY-144060
-
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Akt
|
Cancer
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AKT-IN-10 is a potent inhibitor of AKT. Protein kinase B (PKB, also known as AKT) is central to PI3K/AKT/mTOR signaling in cells, and its function is important for cell growth, survival, differentiation and metabolism. AKT-IN-10 has the potential for the research of breast and prostate cancer (extracted from patent WO2021185238A1, compound 4) .
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-
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- HY-158688
-
|
PI3K
|
Inflammation/Immunology
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PI3Kδ-IN-21 (Compound 31) is a selective inhibitor for phosphoinositide 3-kinases δ (PI3Kδ), with an IC50 of 13.6 nM. PI3Kδ-IN-21 inhibits proliferation and differentation of T cells through PI3K/AKT/mTOR signaling pathway. PI3Kδ-IN-21 exhibits good pharmacokinetic characters in rat model, and attenuates the experimental autoimmune encephalomyelitis in myelin oligodendrocyte glycoprotein (MOG)-induced EAE model .
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-
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- HY-15268
-
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c-Met/HGFR
PI3K
DNA-PK
mTOR
Bcr-Abl
Src
VEGFR
EGFR
PDGFR
|
Cancer
|
PP487 is a dual inhibitor of tyrosine kinase/PI(3)Ks with IC50 values of 0.017 μM, 0.072 μM, 0.004 μM, 0.01 μM, 0.55 μM, 0.22 μM, and < 0.01 μM against DNA-PK, mTOR, Hck, Src, EGFR, EphB4, and PDGFR, respectively. PP487 can be used for cancer research .
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-
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- HY-124652
-
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IKK
|
Cancer
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TBK1/IKKε-IN-4 is a 6-aminopyrazolopyrimidine derivative and a potent, selective TBK1 and IKKε inhibitor with IC50 values of 13 nM and 59 nM, respectively. TBK1/IKKε-IN-4 shows 100- to 1000-fold less activity against other protein kinases including PDK1, PI3K family members and mTOR .
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-
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- HY-131972
-
|
PI3K
|
Cancer
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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 .
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-
-
- HY-W348485
-
|
mTOR
|
Cancer
|
WRX606 is an inhibitor for mTOR complex 1 (mTORC1). WRX606 inhibits the phosphorylation of mTORC1 substrate S6 kinase 1 S6K1 (IC50=10 nM), and the phosphorylation of the eukaryotic translation initiation factor 4E binding protein (p-4E-BP1) (IC50=0.27 μM) in MCF-7. WRX606 exhibits cytotoxicity to HepG2 with IC50 of 17 nM. WRX606 exhibits antitumor efficacy in mouse models .
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-
-
- HY-139534
-
|
ROR
Apoptosis
|
Cancer
|
ARI-1 is an inhibitor of receptor tyrosine kinase-like orphan receptor 1 (ROR1) inhibitor. ARI-1 effectively inhibits aberrant ROR1 expression, which is associated with the development of non-small cell lung cancer (NSCLC) and EGFR-TKI-induced drug resistance. ARI-1 binds to the extracellular Frizzled domain of ROR1 and regulates PI3K/AKT/mTOR signaling in a ROR1-dependent manner. ARI-1 potently inhibits NSCLC cell proliferation and migration and has antitumor activity in vivo [1] .
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-
-
- HY-164384
-
|
PI3K
Akt
mTOR
Apoptosis
|
Cancer
|
DFX117 is a selective, orally active inhibitor for PI3Kα and c-Met tyrosine kinase. DFX117 inhibits PI3K/Akt/mTOR pathway, inhibits the proliferation of NCI-H1975, NCI-H1993, and HCC827 with IC50s 0.02-0.08 µM. DFX117 arrests cell cycle at G0/G1 phase, induces apoptosis in A549 and NCI-H1975. DFX117 exhibits antitumor efficacy in mice .
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-
-
- HY-145931
-
|
mTOR
Autophagy
|
Cancer
|
CC214-2 is an oral active and selective mTOR kinase inhibitor. CC214-2 targets to both of mTORC1 (pS6) and mTORC2 (pAktS473). CC214-2 induces autophagy, which is a potential target for host-directed therapy (HDT) in tuberculosis. CC214-2 exhibits synergistic bactericidal and sterilizing activity agasinst tuberculosis (TB), and shortens the treatment duration. CC214-2 also inhibits Rapamycin (HY-10219)-resistant signaling and the growth of glioblastomas in vitro and in vivo .
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-
-
- HY-15346
-
BAY 80-6946
|
PI3K
Apoptosis
|
Cancer
|
Copanlisib (BAY 80-6946) 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 has more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR. Copanlisib has superior antitumor activity .
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-
-
- HY-15346A
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BAY 80-6946 dihydrochloride
|
PI3K
Apoptosis
|
Cancer
|
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 more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR. Copanlisib dihydrochloride has superior antitumor activity .
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-
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- HY-136765
-
|
PI3K
|
Cancer
|
PI3K-IN-11 (compound 13) is a PI3K inhibitor, which selectively inhibits PI3Kα, PI3Kβ, PI3K, and PI3Kδ (IC50s=6.4, 13, 8, and 11 nM, respectively) over mTOR (IC50=2.9 μM). PX-13-17OH is greater than 420-fold selective for PI3K in a panel of 20 lipid and protein kinases. PX-13-17OH inhibits phosphorylation of Akt and S6 kinase (S6K) in PTEN-negative U87MG cells when used at concentrations ranging from 0.03 to 1 μg/mL. It inhibits tumor growth in a U87MG mouse xenograft model when administered at doses ranging from 2.5 to 10 mg/kg.
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-
-
- HY-N0281
-
7,8-Dihydroxycoumarin
|
EGFR
PKA
PKC
Autophagy
Apoptosis
AMPK
Akt
mTOR
Reactive Oxygen Species
Caspase
Bcl-2 Family
PARP
Parasite
|
Inflammation/Immunology
Cancer
|
Daphnetin (7,8-dihydroxycoumarin), one coumarin derivative can be found in plants of the Genus Daphne, is a potent, oral active protein kinase inhibitor, with IC50s of 7.67 μM, 9.33 μM and 25.01 μM for EGFR, PKA and PKC in vitro, respectively. Daphnetin triggers ROS-induced cell apoptosis and induces cytoprotective autophagy by modulating the AMPK/Akt/mTOR pathway. Daphnetin has anti-inflammation activitity and inhibits TNF-α, IL-1ß, ROS, and MDA production. Daphnetin has schizontocidal activity against malaria parasites. Daphnetin can be used for rheumatoid arthritis , cancer and anti-malarian research .
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- HY-15346R
-
|
PI3K
Apoptosis
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Cancer
|
Copanlisib (Standard) is the analytical standard of Copanlisib. This product is intended for research and analytical applications. Copanlisib (BAY 80-6946) 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 has more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR. Copanlisib has superior antitumor activity .
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- HY-N0281R
-
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EGFR
PKA
PKC
Autophagy
Apoptosis
AMPK
Akt
mTOR
Reactive Oxygen Species
Caspase
Bcl-2 Family
PARP
Parasite
|
Inflammation/Immunology
Cancer
|
Daphnetin (Standard) is the analytical standard of Daphnetin. This product is intended for research and analytical applications. Daphnetin (7,8-dihydroxycoumarin), one coumarin derivative can be found in plants of the Genus Daphne, is a potent, oral active protein kinase inhibitor, with IC50s of 7.67 μM, 9.33 μM and 25.01 μM for EGFR, PKA and PKC in vitro, respectively. Daphnetin triggers ROS-induced cell apoptosis and induces cytoprotective autophagy by modulating the AMPK/Akt/mTOR pathway. Daphnetin has anti-inflammation activitity and inhibits TNF-α, IL-1 , ROS, and MDA production. Daphnetin has schizontocidal activity against malaria parasites. Daphnetin can be used for rheumatoid arthritis , cancer and anti-malarian research .
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- HY-136265
-
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Aminoacyl-tRNA Synthetase
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Cancer
|
BC-LI-0186 is a potent and selective inhibitor of Leucyl-tRNA synthetase (LRS; LeuRS) and Ras-related GTP-binding protein D (RagD) interaction (IC50=46.11 nM). BC-LI-0186 competitively binds to the RagD interacting site of LRS (Kd=42.1 nM) and has on effects on LRS-Vps34, LRS-EPRS, RagB-RagD association, mTORC1 complex formation or the activities of 12 kinases. BC-LI-0186 can effectively suppress the activity of cancer-associated?MTOR?mutants and the growth of rapamycin-resistant cancer cells.?BC-LI-0186 is a promising agent for lung cancer research .
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-
-
-
HY-L015
-
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616 compounds
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The PI3K/Akt/mTOR pathway controls many cellular processes that are important for the formation and progression of cancer, including apoptosis, transcription, translation, metabolism, angiogenesis, and cell cycle progression. Every major node of this signaling network is activated in a wide range of human tumors. Mechanisms for the pathway activation include activation of receptor tyrosine kinases (RTKs) upstream of PI3K, mutation or amplification of PIK3CA encoding p110α catalytic subunit of PI3K, mutation or loss of PTEN tumor suppressor gene, and mutation or amplification of Akt1. Once the pathway is activated, signaling through Akt can stimulate a series of substrates including mTOR which is involved in protein synthesis. Thus, inhibition of this pathway is an attractive concept for cancer prevention and/or therapy. Currently some mTOR inhibitors are approved for several indications, and there are several novel PI3K/Akt/mTOR inhibitors in clinical trials.
MCE owns a unique collection of 616 compounds that can be used for PI3K/Akt/mTOR pathway research. PI3K/Akt/mTOR Compound Library also acts as a useful tool for anti-cancer drug discovery.
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Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P10323
-
Tumstatin (74-98), human
|
Integrin
FAK
mTOR
Apoptosis
|
Cancer
|
T7 peptide is an endothelial cell-specific inhibitor. T7 peptide interacts with αVβ3 integrin to inhibit the FAK, PI3-kinase, PKB/Akt, and mTOR signaling pathways in endothelial cells, ultimately suppressing protein synthesis and inducing apoptosis .
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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-N1050
-
-
-
- HY-N0281
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7,8-Dihydroxycoumarin
|
Structural Classification
Daphne
Classification of Application Fields
Thymelaeaceae
Source classification
Coumarins
Phenols
Polyphenols
Phenylpropanoids
Plants
Disease Research Fields
Cancer
|
EGFR
PKA
PKC
Autophagy
Apoptosis
AMPK
Akt
mTOR
Reactive Oxygen Species
Caspase
Bcl-2 Family
PARP
Parasite
|
Daphnetin (7,8-dihydroxycoumarin), one coumarin derivative can be found in plants of the Genus Daphne, is a potent, oral active protein kinase inhibitor, with IC50s of 7.67 μM, 9.33 μM and 25.01 μM for EGFR, PKA and PKC in vitro, respectively. Daphnetin triggers ROS-induced cell apoptosis and induces cytoprotective autophagy by modulating the AMPK/Akt/mTOR pathway. Daphnetin has anti-inflammation activitity and inhibits TNF-α, IL-1ß, ROS, and MDA production. Daphnetin has schizontocidal activity against malaria parasites. Daphnetin can be used for rheumatoid arthritis , cancer and anti-malarian research .
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-
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- HY-N10754
-
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- HY-N0281R
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Structural Classification
Daphne
Thymelaeaceae
Source classification
Coumarins
Phenols
Polyphenols
Phenylpropanoids
Plants
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EGFR
PKA
PKC
Autophagy
Apoptosis
AMPK
Akt
mTOR
Reactive Oxygen Species
Caspase
Bcl-2 Family
PARP
Parasite
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Daphnetin (Standard) is the analytical standard of Daphnetin. This product is intended for research and analytical applications. Daphnetin (7,8-dihydroxycoumarin), one coumarin derivative can be found in plants of the Genus Daphne, is a potent, oral active protein kinase inhibitor, with IC50s of 7.67 μM, 9.33 μM and 25.01 μM for EGFR, PKA and PKC in vitro, respectively. Daphnetin triggers ROS-induced cell apoptosis and induces cytoprotective autophagy by modulating the AMPK/Akt/mTOR pathway. Daphnetin has anti-inflammation activitity and inhibits TNF-α, IL-1 , ROS, and MDA production. Daphnetin has schizontocidal activity against malaria parasites. Daphnetin can be used for rheumatoid arthritis , cancer and anti-malarian research .
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