Search Result
Results for "
mTORC1
" in MedChemExpress (MCE) Product Catalog:
2
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-120904
-
|
AMPK
|
Metabolic Disease
|
AMPK-IN-1 is an activator of AMPK (EC50: 551 nM for isoform α2β2γ1). AMPK-IN-1 leads to eEF2 phosphorylation in a mTORC1-independent way [1] .
|
-
-
- HY-124798
-
|
mTOR
|
Neurological Disease
Inflammation/Immunology
Cancer
|
Rheb inhibitor NR1 is a Rheb inhibitor with an IC50 of 2.1 µM in the Rheb-IVK assay. Rheb inhibitor NR1 can directly bind Rheb in the switch II domain and selectively inhibit the activation of mechanistic target of rapamycin complex 1 (mTORC1). Rheb inhibitor NR1 inhibits the phosphorylation of mTORC1 driven T389pS6K1 and increases the phosphorylation of S473pAKT in a dose-dependent manner. Rheb inhibitor NR1 does not influence mTORC2 activity [1].
(Rheb-IVK: Rheb-dependent mTORC1 kinase activity)
|
-
-
- HY-134904
-
RM-006
|
mTOR
|
Cancer
|
RMC-6272 (RM-006) is a bi-steric mTORC1-selective inhibitor. RMC-6272 exhibits potent and selective (> 10-fold) inhibition of mTORC1 over mTORC2. RMC-6272 shows improved inhibition of mTORC1 in comparison to Rapamycin, and induces more cell death in TSC2 null tumors [1].
|
-
-
- HY-10219
-
Rapamycin
Maximum Cited Publications
850 Publications Verification
Sirolimus; AY-22989
|
mTOR
FKBP
Fungal
Autophagy
Endogenous Metabolite
Antibiotic
Bacterial
|
Cancer
|
Rapamycin (Sirolimus; AY 22989) is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1 [1]. Rapamycin is an autophagy activator, an immunosuppressant .
|
-
-
- HY-12652
-
|
mTOR
|
Cancer
|
AZD3147 is a potent, orally active, selective dual inhibitor of mTORC1 and mTORC2 with an IC50 value of 1.5 nM. AZD3147 also has a selective effect on PI3K [1].
|
-
-
- HY-10219S
-
Sirolimus-d3; AY-22989-d3
|
mTOR
FKBP
Autophagy
|
Cancer
|
Rapamycin-d3 is the deuterium labeled Rapamycin. Rapamycin is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1. Rapamycin is an autophagy activator, an immunosuppressant [1] .
|
-
-
- HY-132168
-
|
mTOR
|
Cancer
|
RMC-5552 is a potent and selective mTORC1 inhibitor. RMC-5552 inhibits phosphorylation of mTORC1 pS6K and p4EBP1 with IC50s of 0.14 nM and 0.48 nM, respectively. RMC-5552 shows much lower pAKT inhibition (IC50 of 19 nM), resulting in mTORC1/mTORC2 selectivity approaching 40-fold. RMC-5552 has anti-cancer activity [1].
|
-
-
- HY-155475
-
|
mTOR
|
Cardiovascular Disease
|
mTORC1-IN-2 (compound H3) is a NO donor compound that alleviates vasodilation and attenuates myocardial hypoxic injury. mTORC1-IN-2 upregulates TSC2-P expression and inhibits mTORC1 expression [1].
|
-
-
- HY-111065
-
|
mTOR
|
Cancer
|
OXA-01 is a potent mTORC1 and mTORC2 inhibitor, with IC50 values of 29 nM and 7 nM, respectively [1].
|
-
-
- HY-15281
-
|
mTOR
|
Cancer
|
QL-IX-55 is a selective ATP-competitive inhibitor of mTORC1/2 with IC50s of 50/50/10-50 nM for Human mTORC1/Yeast mTORC1/Yeast mTORC2, respectively.
|
-
-
- HY-14581
-
-
-
- HY-14530
-
AG 2037
|
Antifolate
|
Cancer
|
Pelitrexol (AG 2037) is an inhibitor of glycinamide ribonucleotide formyltransferase (GARFT), a purine biosynthetic enzyme. Pelitrexol also inhibits mTORC1 by reducing GTP-bound Rheb level, a mTORC1 obligate activator. Pelitrexol shows robust tumor growth suppression in mice [1].
|
-
-
- HY-10219R
-
|
mTOR
FKBP
Fungal
Autophagy
Endogenous Metabolite
Antibiotic
Bacterial
|
Cancer
|
Rapamycin (Standard) is the analytical standard of Rapamycin. This product is intended for research and analytical applications. Rapamycin (Sirolimus; AY 22989) is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1 [1]. Rapamycin is an autophagy activator, an immunosuppressant .
|
-
-
- HY-100026
-
PQR620
4 Publications Verification
|
mTOR
|
Cancer
|
PQR620 is an orally bioavailable and selective brain penetrant inhibitor of mTORC1/2 [1].
|
-
-
- HY-N2517
-
|
mTOR
|
Cancer
|
Dihydroevocarpine induces cytotoxicity in acute myeloid leukemia via suppressing the mTORC1/2 activity [1].
|
-
-
- HY-143510
-
|
mTOR
|
Cancer
|
RMC-4627 is a selective mTORC1 inhibitor that activates 4EBP1 and inhibits tumor growth.
|
-
-
- HY-125355
-
|
Apoptosis
|
Cancer
|
SEC induces activation of ANXA7 GTPase via the AMPK/mTORC1/STAT3 signaling pathway. SEC selectively promotes apoptosis in cancer cells, expressing a high level of ITGB4 by inducing ITGB4 nuclear translocation [1] .
|
-
-
- HY-N3628
-
-
-
- HY-107363
-
|
mTOR
|
Cancer
|
FT-1518 is a new generation selective, potent and oral bioavailable mTORC1 and mTORC2 inhibitor, and exhibits antitumor activity.
|
-
-
- HY-119665
-
|
AMPK
mTOR
|
Cancer
|
Asteltoxin is an inhibitor for extracellular vesicles (EV), which exhibits inhibitory effects towards mitochondrial ATP synthase and mTORC1 activation [1].
|
-
-
- HY-153789
-
|
Others
|
Cancer
|
PI5P4Kγ-IN-1 (compound 2) is a selective PI5P4Kγ inhibitor. PI5P4Kγ-IN-1 can be used to signal mTORC1 in MCF-7 breast cancer cells and further characterize PI5P4Kγ in the cells [1].
|
-
-
- HY-50710
-
|
mTOR
|
Cancer
|
KU-0063794 is a potent and specific mTOR inhibitor, inhibiting both the mTORC1 and mTORC2 complexes with IC50s of 10 nM.
|
-
-
- HY-W058849
-
|
AMPK
mTOR
Apoptosis
|
Cancer
|
MT 63-78 is a specific and potent direct AMPK activator with an EC50 of 25 μM. MT 63–78 also induces cell mitotic arrest and apoptosis. MT 63-78 blocks prostate cancer growth by inhibiting the lipogenesis and mTORC1 pathways. MT 63-78 has antitumor effects [1].
|
-
-
- HY-15247
-
AZD2014
|
mTOR
Autophagy
Apoptosis
|
Cancer
|
Vistusertib (AZD2014) is an ATP competitive mTOR inhibitor with an IC50 of 2.81 nM. AZD2014 inhibits both mTORC1 and mTORC2 complexes.
|
-
-
- HY-13806
-
XL388
3 Publications Verification
|
mTOR
Autophagy
|
Cancer
|
XL388 is a highly potent and ATP-competitive mTOR inhibitor with an IC50 of 9.9 nM. XL388 simultaneously inhibits both mTORC1 and mTORC2.
|
-
-
- HY-100222
-
CZ415
3 Publications Verification
|
mTOR
|
Cancer
|
CZ415 is a potent and highly selective mTOR inhibitor with a pIC50 of 8.07. CZ415 inhibits mTORC1 and mTORC2 protein complex.
|
-
-
- HY-15248
-
|
mTOR
Autophagy
|
Cancer
|
GDC-0349 is a potent and selective ATP-competitive mTOR inhibitor with a Ki of 3.8 nM. GDC-0349 inhibits of both mTORC1 and mTORC2 complexes.
|
-
-
- HY-16956
-
CC-223; ATG-008
|
mTOR
Apoptosis
|
Cancer
|
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.
|
-
-
- HY-P5984
-
|
mTOR
|
Others
|
Thioether-cyclized helix B peptide, CHBP can improve metabolic stability and renoprotective effect through inducing autophagy via inhibition of mTORC1 and activation of mTORC2 [1].
|
-
-
- HY-162147
-
|
mTOR
Autophagy
|
Inflammation/Immunology
|
Nur77 modulator 3 (9e) can bind to Nur77 and inhibit TGF-β1-induced α-SMA and COLA1 expression in a Nur77-dependent manner. Nur77 modulator 3 induces Nur77 expression and enhances autophagic flux by inhibiting the mTORC1 signaling pathway in vitro and in vivo. Nur77 modulator 3 blocks the progression of hepatic fibrosis [1].
|
-
-
- HY-114384
-
NV-5138
5 Publications Verification
|
mTOR
|
Neurological Disease
|
NV-5138, a leucine analog, is the first selective and orally active brain mTORC1 activator, binding to Sestrin2. NV-5138 is used for antidepressant studies [1] .
|
-
-
- HY-114384B
-
|
mTOR
|
Neurological Disease
|
NV-5138 hydrochloride, a leucine analog, is the first selective and orally active brain mTORC1 activator, binding to Sestrin2. NV-5138 hydrochloride is used for antidepressant studies [1] .
|
-
-
- HY-10422
-
|
mTOR
Autophagy
Apoptosis
|
Cancer
|
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 [1].
|
-
-
- HY-153493
-
-
-
- HY-B1787
-
|
mTOR
Drug Metabolite
|
Cancer
|
Sulindac sulfone is an mTORC1 pathway inhibitor and a metabolite of Sulindac. Sulindac sulfone inhibits colon cancer cell growth and induces cell cycle arrest. Sulindac sulfone is used in cancer research [1].
|
-
-
- HY-153493A
-
|
Small Interfering RNA (siRNA)
|
Metabolic Disease
|
PF-04523655 sodium is a siRNA directed against RTP801 gene. RTP801 sodium is an inhibitor of the mammalian target of rampamycin complex 1 (mTORC1) and downstream transcription factor HIF-1.
|
-
-
- HY-15901
-
|
mTOR
|
Cancer
|
LGB321 is an inhibitor of PIM2-dependent multiple myeloma cell lines, effectively inhibiting proliferation and key signaling pathways such as mTOR-C1 and phosphorylation of BAD [1].
|
-
-
- HY-134922
-
|
Influenza Virus
|
Infection
|
NS1-IN-1 (compound 3) is a potent NS1 inhibitor. NS1 is a major influenza A virus virulence factor that inhibits host gene expression. NS1-IN-1 decreases viral protein levels, contributing to the reduction of virus replication. NS1-IN-1 shows antiviral activity by repressing the activity of mTORC1 in a TSC1-TSC2-dependent manner [1].
|
-
-
- HY-10474
-
PP 242
|
mTOR
Autophagy
Mitophagy
Apoptosis
|
Cancer
|
Torkinib (PP 242) is a selective and ATP-competitive mTOR inhibitor with an IC50 of 8 nM [1]. PP242 inhibits both mTORC1 and mTORC2 with IC50s of 30 nM and 58 nM, respectively .
|
-
-
- HY-13003
-
|
mTOR
Autophagy
|
Cancer
|
Torin 1 is a potent inhibitor of mTOR with an IC50 of 3 nM. Torin 1 inhibits both mTORC1/2 complexes with IC50 values between 2 and 10 nM. Torin 1 is an effective inducer of autophagy.
|
-
-
- HY-18353
-
|
mTOR
|
Cancer
|
mTOR inhibitor-3 is a remarkably selective mTOR inhibitor with a Ki of 1.5 nM. mTOR inhibitor-3 suppresses mTORC1 and mTORC2 in cellular and in vivo pharmacokinetic (PK)/pharmacodynamic (PD) experiments.
|
-
-
- HY-16962
-
CC-115
2 Publications Verification
|
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.
|
-
-
- HY-16962A
-
|
DNA-PK
mTOR
|
Cancer
|
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.
|
-
-
- HY-128339
-
|
Autophagy
|
Cancer
|
Autogramin-1 potently inhibits autophagy induced by either starvation (IC50=0.17 μM) or mTORC1 inhibition (Rapamycin; IC50=0.44 μM) [1].
|
-
-
- HY-128340
-
|
Autophagy
|
Cancer
|
Autogramin-2 potently inhibits autophagy induced by either starvation (IC50=0.27 μM) or mTORC1 inhibition (Rapamycin; IC50=0.14 μM) [1].
|
-
-
- HY-12513
-
LY3023414
|
PI3K
DNA-PK
mTOR
Autophagy
|
Cancer
|
Samotolisib (LY3023414) potently and selectively inhibits class I PI3K isoforms, DNA-PK, and mTORC1/2 with IC50s of 6.07 nM, 77.6 nM, 38 nM, 23.8 nM, 4.24 nM and 165 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ, DNA-PK and mTOR, respectively. Samotolisib potently inhibits mTORC1/2 at low nanomolar concentrations [1] .
|
-
-
- 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 [1].
|
-
-
- HY-15880
-
|
Phosphatase
Apoptosis
Autophagy
|
Cancer
|
CCT007093 is an effective protein phosphatase 1D (PPM1D Wip1) inhibitor. Wip1 inhibition can activate the mTORC1 pathway and enhance hepatocyte proliferation after hepatectomy [1] .
|
-
-
- HY-15272
-
|
mTOR
|
Inflammation/Immunology
Cancer
|
WAY-600 is a potent, ATP-competitive, and selective mTOR inhibitor with an IC50 of 9 nM for recombinant mTOR enzyme. WAY-600 blocks mTOR complex 1/2 (mTORC1/2) assemble and activation.
|
-
-
- HY-W015309
-
|
iGluR
Tyrosinase
c-Met/HGFR
Glutaminase
Endogenous Metabolite
|
Neurological Disease
Metabolic Disease
Cancer
|
Decanoic acid is a key component of the medium-chain triglyceride (MCT) found in coconut oil. Decanoic acid is a brain-penetrant and non-competitive inhibitor of AMPA receptor showing antiseizure activity in rats. Decanoic acid reduces tyrosinase activity and inhibits melanosome maturation. Decanoic acid suppresses the phosphorylation of c-Met and induced apoptosis in hepatocellular carcinoma (HCC) cells by inhibiting the expression of various oncogenic proteins, which is promising for research in the field of mTORC1 signaling, HCC and epilepsy [1] .
|
-
- 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 [1] .
|
-
- HY-128892
-
EN6
3 Publications Verification
|
Autophagy
|
Neurological Disease
|
EN6 is a small-molecule in vivo autophagy activator that covalently targets cysteine 277 in the ATP6V1A subunit of the lysosomal v-ATPase. EN6-mediated modification of ATP6V1A uncouples v-ATPase from Rag, leading to inhibition of mTORC1 signalling, increased lysosomal acidification, and activation of autophagy. EN6 also scavenges TDP-43 aggregates (causative agents of frontotemporal dementia) in a lysosome-dependent manner [1].
|
-
- HY-W015309R
-
|
iGluR
Tyrosinase
c-Met/HGFR
Glutaminase
|
Neurological Disease
Metabolic Disease
Cancer
|
Decanoic acid (Standard) is the analytical standard of Decanoic acid. This product is intended for research and analytical applications. Decanoic acid is a key component of the medium-chain triglyceride (MCT) found in coconut oil. Decanoic acid is a brain-penetrant and non-competitive inhibitor of AMPA receptor showing antiseizure activity in rats. Decanoic acid reduces tyrosinase activity and inhibits melanosome maturation. Decanoic acid suppresses the phosphorylation of c-Met and induced apoptosis in hepatocellular carcinoma (HCC) cells by inhibiting the expression of various oncogenic proteins, which is promising for research in the field of mTORC1 signaling, HCC and epilepsy [1] .
|
-
- HY-10423
-
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 [1] .
|
-
- HY-15174
-
BEZ235 Tosylate; NVP-BEZ 235 Tosylate
|
PI3K
mTOR
Autophagy
|
Cancer
|
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.
|
-
- HY-114267
-
|
mTOR
|
Others
|
Cbz-B3A is a potent and selective inhibitor of mTORC1 signaling that appear to bind to ubiquilins 1, 2, and 4, and Cbz-B3A inhibits the phosphorylation of eIF4E-binding protein 1 (4EBP1).
|
-
- HY-N0112
-
Ampelopsin; Ampeloptin
|
mTOR
Influenza Virus
DNA/RNA Synthesis
Autophagy
|
Infection
Cancer
|
Dihydromyricetin is a potent inhibitor with an IC50 of 48 μM on dihydropyrimidinase. Dihydromyricetin can activate autophagy through inhibiting mTOR signaling. Dihydromyricetin suppresses the formation of mTOR complexes (mTORC1/2). Dihydromyricetin is also a potent influenza RNA-dependent RNA polymerase inhibitor with an IC50 of 22 μM.
|
-
- HY-119137
-
|
Autophagy
AMPK
|
Cancer
|
AMDE-1 is a potent autophagy inducer. AMDE-1 induces autophagy by the AMPK-mTORC1-ULK1 pathway and at the same time inhibited autophagy-mediated degradation by causing lysosome dysfunction. AMDE-1 can be used in research of cancer [1].
|
-
- HY-111370
-
|
mTOR
|
Cancer
|
mTOR inhibitor-2 is a highlt potent, selective and oral mTOR inhibitor with an IC50 of 7 nM. mTOR inhibitor-2 inhibits cellular phosphorylation of mTORC1 (pS6 and p4E-BP1) and mTORC2 (pAKT (S473)) substrates [1].
|
-
- HY-108900
-
|
Aminoacyl-tRNA Synthetase
Bacterial
|
Infection
Cancer
|
Leu-AMS (compound 6), a leucine analogue, is a potent inhibitor of leucyl-tRNA synthetase (LRS) with an IC50 of 22.34 nM, which inhibits the catalytic activity of LRS but did not affect the leucine-induced mTORC1 activation. Leu-AMS shows cytotoxicity in cancer cells and normal cells, and inhibits the growth of bacteria [1].
|
-
- HY-107365
-
|
PI3K
mTOR
|
Cancer
|
PQR530 is a potent, ATP-competitive, orally bioavailable and brain-penetrant dual pan-PI3K/mTORC1/2 inhibitor, with a subnanomolar Kd toward PI3Kα and mTOR (0.84 and 0.33 nM, respectively). Antitumor activity [1] .
|
-
- HY-10044
-
WYE-125132
|
mTOR
Apoptosis
|
Cancer
|
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.
|
-
- HY-10681
-
PKI-587; PF-05212384
|
PI3K
mTOR
|
Cancer
|
Gedatolisib (PKI-587) is a highly potent dual inhibitor of PI3Kα, PI3Kγ, and mTOR with IC50s of 0.4 nM, 5.4 nM and 1.6 nM, respectively [1]. Gedatolisib is equally effective in both complexes of mTOR, mTORC1 and mTORC2 .
|
-
- HY-126077
-
LXI-15029
|
mTOR
|
Inflammation/Immunology
Cancer
|
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 [1].
|
-
- HY-15271
-
WYE-687
3 Publications Verification
|
mTOR
PI3K
|
Cancer
|
WYE-687 is an ATP-competitive mTOR inhibitor with an IC50 of 7 nM. WYE-687 concurrently inhibits activation of mTORC1 and mTORC2. WYE-687 also inhibits PI3Kα and PI3Kγ with IC50s of 81 nM and 3.11 μM, respectively.
|
-
- HY-P5984A
-
|
mTOR
|
Others
|
Thioether-cyclized helix B peptide, CHBP (TFA) is the TFA form of Thioether-cyclized helix B peptide, CHBP (HY-P5984). Thioether-cyclized helix B peptide, CHBP (TFA) can improve metabolic stability and renoprotective effect through inducing autophagy via inhibition of mTORC1 and activation of mTORC2 [1].
|
-
- HY-15901A
-
|
Pim
mTOR
|
Cancer
|
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 [1].
|
-
- HY-158050
-
|
c-Fms
|
Cancer
|
PXB17 can inhibit CSF1R (IC50 = 1.7 nM) by blocking the activation of PI3K/ AKT/mTORC1 signaling. PXB17 is orally effective. PXB17 significantly inhibits the growth of CRC, improves PD-1 mAb efficacy and reduces tumor recurrence in CRC [1].
|
-
- HY-13002
-
|
mTOR
DNA-PK
Autophagy
Apoptosis
|
Cancer
|
Torin 2 is an mTOR inhibitor with EC50 of 0.25 nM for inhibiting cellular mTOR activity, and exhibits 800-fold selectivity over PI3K (EC50: 200 nM). Torin 2 also inhibits DNA-PK with an IC50 of 0.5 nM in the cell free assay. Torin 2 can suppress both mTORC1 and mTORC2.
|
-
- HY-15271A
-
|
mTOR
PI3K
|
Cancer
|
WYE-687 dihydrochloride is an ATP-competitive mTOR inhibitor with an IC50 of 7 nM [1]. WYE-687 dihydrochloride concurrently inhibits activation of mTORC1 and mTORC2 . WYE-687 also inhibits PI3Kα and PI3Kγ with IC50s of 81 nM and 3.11 μM, respectively [1].
|
-
- HY-N0112R
-
|
mTOR
Influenza Virus
DNA/RNA Synthesis
Autophagy
|
Infection
Cancer
|
Dihydromyricetin (Standard) is the analytical standard of Dihydromyricetin. This product is intended for research and analytical applications. Dihydromyricetin is a potent inhibitor with an IC50 of 48 μM on dihydropyrimidinase. Dihydromyricetin can activate autophagy through inhibiting mTOR signaling. Dihydromyricetin suppresses the formation of mTOR complexes (mTORC1/2). Dihydromyricetin is also a potent influenza RNA-dependent RNA polymerase inhibitor with an IC50 of 22 μM.
|
-
- HY-12034
-
|
mTOR
Autophagy
Apoptosis
|
Cancer
|
WYE-354 is an ATP-competitive mTOR inhibitor with an IC50 of 5 nM. WYE-354 also inhibits PI3Kα and PI3Kγ with IC50s of 1.89 μM and 7.37 μM, respectively. WYE-354 inhibits both mTORC1 and mTORC2. WYE-354 induces autophagy activation in vitro .
|
-
- HY-155542
-
|
ROR
|
Cancer
|
RORγ antagonist 1 (compound 22), a potent betulinic acid derivative, is an antagonist of RORγ (KD=0.18 μM). RORγ antagonist 1 exhibits anti-proliferative activity in HPAF-II pancreatic cancer xenograft model. RORγ antagonist 1 inhibits RAS/MAPK and AKT/mTORC1 pathway, and induces caspase-dependent apoptosis in pancreatic cancer cells [1].
|
-
- HY-16585
-
VS-5584
5 Publications Verification
SB2343
|
PI3K
mTOR
|
Cancer
|
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.
|
-
- HY-107758
-
|
Prolyl Endopeptidase (PREP)
|
Cancer
|
Y-29794 oxalate is a selective, orally active and blood-brain barrier permeable non-peptide prolyl endopeptidase inhibitor. Y-29794 oxalate blocks the IRS1-AKT-mTORC1 pathway and inhibits tumor growth. Y-29794 oxalate is also effective in inhibiting the progression of Aβ-like deposition in the hippocampus of aging-accelerated mice (SAM) [1] .
|
-
- HY-161509
-
|
mTOR
|
Cancer
|
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 [1].
|
-
- HY-10297
-
GSK2126458; GSK458
|
PI3K
mTOR
Autophagy
|
Cancer
|
Omipalisib (GSK2126458) is an orally active and highly selective inhibitor of PI3K with Kis 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. Omipalisib has anti-cancer activity [1] .
|
-
- HY-115570
-
GW108X
|
Kinesin
ULK
Autophagy
|
Cancer
|
GW406108X is a specific Kif15 (Kinesin-12) inhibitor with an IC50 of 0.82 uM in ATPase assays. GW406108X, a potent autophagy inhibitor, shows ATP competitive inhibition against ULK1 with a pIC50 of 6.37 (427 nM). GW406108X inhibits ULK1 kinase activity and blocks autophagic flux, without affecting the upstream signaling kinases mTORC1 and AMPK [1] .
|
-
- HY-10115
-
|
PI3K
mTOR
DNA-PK
Autophagy
Apoptosis
|
Cancer
|
PI-103 is a potent PI3K and mTOR inhibitor with IC50s of 8 nM, 88 nM, 48 nM, 150 nM, 20 nM, and 83 nM for p110α, p110β, p110δ, p110γ, mTORC1, and mTORC2. PI-103 also inhibits DNA-PK with an IC50 of 2 nM. PI-103 induces autophagy [1] .
|
-
- HY-10115A
-
|
PI3K
mTOR
DNA-PK
Autophagy
Apoptosis
|
Cancer
|
PI-103 Hydrochloride is a dual PI3K and mTOR inhibitor with IC50s of 8 nM, 88 nM, 48 nM, 150 nM, 20 nM, and 83 nM for p110α, p110β, p110δ, p110γ, mTORC1, and mTORC2. PI-103 Hydrochloride also inhibits DNA-PK with an IC50 of 2 nM. PI-103 Hydrochloride induces autophagy [1] .
|
-
- HY-12868
-
PQR309
|
PI3K
mTOR
|
Cancer
|
Bimiralisib (PQR309) is a potent, brain-penetrant, orally bioavailable, pan-class I PI3K/mTOR inhibitor with IC50s of 33 nM, 451 nM, 661 nM, 708 nM and 89 nM for PI3Kα, PI3Kδ, PI3Kβ, PI3Kγ and mTOR, respectively. Bimiralisib is an mTORC1 and mTORC2 inhibitor.
|
-
- HY-N0656A
-
|
mTOR
Bacterial
Autophagy
|
Cancer
|
(+)-Usnic acid is isolated from isolated from lichens, binds at the ATP-binding pocket of mTOR, and inhibits mTORC1/2 activity. (+)-Usnic acid inhibits the phosphorylation of mTOR downstream effectors: Akt (Ser473), 4EBP1, S6K, induces autophay, with anti-cancer activity [1]. (+)-Usnic acid possesses antimicrobial activity against a number of planktonic gram-positive bacteria, including Staphylococcus aureus, Enterococcus faecalis, and Enterococcus faecium .
|
-
- HY-50673
-
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.
|
-
- HY-10219S1
-
Sirolimus-13C,d3; AY-22989-13C,d3
|
Isotope-Labeled Compounds
|
Others
|
Rapamycin- 13C,d3 (Sirolimus- 13C,d3; AY-22989- 13C,d3) is the 13C and deuterium labeled Rapamycin (HY-10219) [1]. Rapamycin (Sirolimus; AY 22989) is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1 . Rapamycin is an autophagy activator, an immunosuppressant .
|
-
- HY-15113A
-
|
Prolyl Endopeptidase (PREP)
|
Neurological Disease
Cancer
|
Y-29794 tosylate is a selective, orally active inhibitor for non-peptide prolyl endopeptidase (PREP), with an IC50 of 3 nM and a Ki of 0.95 nM. Y-29794 tosylate enhances the effect of thyrotropin-releasing hormone (TRH) on the release of ACh in the rat hippocampus, exhibits potential neuroprotective efficacy. Y-29794 tosylate exhibits anticancer activity through inhibition of the IRS1-AKT-mTORC1 pathway. Y-29794 tosylate penetrates the brain-blood barrier (BBB) [1] .
|
-
- HY-15113
-
|
Prolyl Endopeptidase (PREP)
|
Neurological Disease
Cancer
|
Y-29794 is a selective, orally active inhibitor for non-peptide prolyl endopeptidase (PREP), with an IC50 of 3 nM and a Ki of 0.95 nM. Y-29794 enhances the effect of thyrotropin-releasing hormone (TRH) on the release of ACh in the rat hippocampus, exhibits potential neuroprotective efficacy. Y-29794 exhibits anticancer activity through inhibition of the IRS1-AKT-mTORC1 pathway. Y-29794 penetrates the brain-blood barrier (BBB) [1] .
|
-
- HY-N0656AR
-
|
mTOR
Bacterial
Autophagy
|
Cancer
|
(+)-Usnic acid (Standard) is the analytical standard of (+)-Usnic acid. This product is intended for research and analytical applications. (+)-Usnic acid is isolated from isolated from lichens, binds at the ATP-binding pocket of mTOR, and inhibits mTORC1/2 activity. (+)-Usnic acid inhibits the phosphorylation of mTOR downstream effectors: Akt (Ser473), 4EBP1, S6K, induces autophay, with anti-cancer activity [1]. (+)-Usnic acid possesses antimicrobial activity against a number of planktonic gram-positive bacteria, including Staphylococcus aureus, Enterococcus faecalis, and Enterococcus faecium .
|
-
- HY-15900
-
XL765; SAR245409
|
PI3K
mTOR
|
Cancer
|
Voxtalisib (XL765) is a potent PI3K inhibitor, which has a similar activity toward class I PI3K (IC50s=39, 113, 9 and 43 nM for p110α, p110β, p110γ and p110δ, respectively), also inhibits DNA-PK (IC50=150 nM) and mTOR (IC50=157 nM). Voxtalisib (XL765) inhibits mTORC1 and mTORC2 with IC50s of 160 and 910 nM, respectively.
|
-
- HY-18980
-
Mallotoxin; NSC 56346; NSC 94525
|
PKC
Autophagy
Apoptosis
HIV
RABV
|
Infection
Cancer
|
Rottlerin, a natural product purified from Mallotus Philippinensis, is a specific PKC inhibitor, with IC50 values for PKCδ of 3-6 μM, PKCα,β,γ of 30-42 μM, PKCε,η,ζ of 80-100 μM. Rottlerin acts as a direct mitochondrial uncoupler, and stimulates autophagy by targeting a signaling cascade upstream of mTORC1. Rottlerin induces apoptosis via caspase 3 activation [1] . Rottlerin inhibits HIV-1 integration and Rabies virus (RABV) infection .
|
-
- HY-134903
-
|
mTOR
|
Cancer
|
(32-Carbonyl)-RMC-5552 is a potent mTOR inhibitor. (32-Carbonyl)-RMC-5552 inhibits mTORC1 and mTORC2 substrate (p-P70S6K-(T389), p-4E-BP1-(T37/36), AND p-AKT1/2/3-(S473)) phosphorylation with pIC50s of > 9, >9 and between 8 and 9, respectively (patent WO2019212990A1, example 2) [1].
|
-
- HY-111373
-
|
mTOR
Autophagy
|
Cancer
|
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 [1] .
|
-
- HY-136265
-
|
Aminoacyl-tRNA Synthetase
|
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 [1] .
|
-
- HY-P2657
-
|
HIF/HIF Prolyl-Hydroxylase
Proton Pump
Endogenous Metabolite
|
Cancer
|
Verucopeptin is a potent HIF-1 (IC50=0.22 μM) inhibitor and decreases the expression of HIF-1 target genes and HIF-1α protein levels. Verucopeptin strongly inhibits v-ATPase activity by directly targeting the v-ATPase ATP6V1G subunit but not ATP1V1B2 or ATP6V1D. Verucopeptin exhibits antitumor activity against multidrug resistance (MDR) cancers and can be used for cancer research.
|
-
- HY-16724
-
1-Methyl-D-tryptophan; NLG-8189
|
Indoleamine 2,3-Dioxygenase (IDO)
|
Cancer
|
Indoximod (1-Methyl-D-tryptophan) is an orally active indoleamine 2,3-dioxygenase (IDO) pathway inhibitor. Indoximod acts as a Trp mimetic in regulating mTOR. Indoximod is an immunometabolic adjuvant used for the research of cancer [1] .
|
-
- HY-137458A
-
ARQ 751 trihydrochloride
|
Akt
|
Cancer
|
Vevorisertib (ARQ 751) trihydrochloride is a selective, allosteric, pan-AKT and AKT1-E17K mutant inhibitors. Vevorisertib trihydrochloride potently inhibit phosphorylation of AKT. Vevorisertib trihydrochloride has Kd values of 1.2 nM and 8.6 nM for AKT1 and AKT1-E17K, respectively. Vevorisertib trihydrochloride has IC50 values of 0.55, 0.81, and 1.3 nM for AKT1, AKT2, and AKT3, respectively. Vevorisertib trihydrochloride can be used for the research of cancer [1].
|
-
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P2657
-
|
HIF/HIF Prolyl-Hydroxylase
Proton Pump
Endogenous Metabolite
|
Cancer
|
Verucopeptin is a potent HIF-1 (IC50=0.22 μM) inhibitor and decreases the expression of HIF-1 target genes and HIF-1α protein levels. Verucopeptin strongly inhibits v-ATPase activity by directly targeting the v-ATPase ATP6V1G subunit but not ATP1V1B2 or ATP6V1D. Verucopeptin exhibits antitumor activity against multidrug resistance (MDR) cancers and can be used for cancer research.
|
-
- HY-P5984
-
|
mTOR
|
Others
|
Thioether-cyclized helix B peptide, CHBP can improve metabolic stability and renoprotective effect through inducing autophagy via inhibition of mTORC1 and activation of mTORC2 [1].
|
-
- HY-P5984A
-
|
mTOR
|
Others
|
Thioether-cyclized helix B peptide, CHBP (TFA) is the TFA form of Thioether-cyclized helix B peptide, CHBP (HY-P5984). Thioether-cyclized helix B peptide, CHBP (TFA) can improve metabolic stability and renoprotective effect through inducing autophagy via inhibition of mTORC1 and activation of mTORC2 [1].
|
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-10219
-
-
-
- HY-10219R
-
-
-
- HY-N2517
-
-
-
- HY-N3628
-
-
-
- HY-W015309
-
-
-
- HY-N0112
-
-
-
- HY-N0656A
-
|
Structural Classification
other families
Classification of Application Fields
Ketones, Aldehydes, Acids
Plants
Lichen
Disease Research Fields
Cancer
|
mTOR
Bacterial
Autophagy
|
(+)-Usnic acid is isolated from isolated from lichens, binds at the ATP-binding pocket of mTOR, and inhibits mTORC1/2 activity. (+)-Usnic acid inhibits the phosphorylation of mTOR downstream effectors: Akt (Ser473), 4EBP1, S6K, induces autophay, with anti-cancer activity [1]. (+)-Usnic acid possesses antimicrobial activity against a number of planktonic gram-positive bacteria, including Staphylococcus aureus, Enterococcus faecalis, and Enterococcus faecium .
|
-
-
- HY-W015309R
-
|
Structural Classification
Microorganisms
Ketones, Aldehydes, Acids
Source classification
Endogenous metabolite
|
iGluR
Tyrosinase
c-Met/HGFR
Glutaminase
|
Decanoic acid (Standard) is the analytical standard of Decanoic acid. This product is intended for research and analytical applications. Decanoic acid is a key component of the medium-chain triglyceride (MCT) found in coconut oil. Decanoic acid is a brain-penetrant and non-competitive inhibitor of AMPA receptor showing antiseizure activity in rats. Decanoic acid reduces tyrosinase activity and inhibits melanosome maturation. Decanoic acid suppresses the phosphorylation of c-Met and induced apoptosis in hepatocellular carcinoma (HCC) cells by inhibiting the expression of various oncogenic proteins, which is promising for research in the field of mTORC1 signaling, HCC and epilepsy [1] .
|
-
-
- HY-N0112R
-
-
-
- HY-N0656AR
-
|
Structural Classification
other families
Ketones, Aldehydes, Acids
Plants
Lichen
|
mTOR
Bacterial
Autophagy
|
(+)-Usnic acid (Standard) is the analytical standard of (+)-Usnic acid. This product is intended for research and analytical applications. (+)-Usnic acid is isolated from isolated from lichens, binds at the ATP-binding pocket of mTOR, and inhibits mTORC1/2 activity. (+)-Usnic acid inhibits the phosphorylation of mTOR downstream effectors: Akt (Ser473), 4EBP1, S6K, induces autophay, with anti-cancer activity [1]. (+)-Usnic acid possesses antimicrobial activity against a number of planktonic gram-positive bacteria, including Staphylococcus aureus, Enterococcus faecalis, and Enterococcus faecium .
|
-
-
- HY-18980
-
Mallotoxin; NSC 56346; NSC 94525
|
Structural Classification
Chalcones
Flavonoids
Classification of Application Fields
Source classification
Phenols
Polyphenols
Euphorbiaceae
Plants
Disease Research Fields
Mallotus philippensis
Cancer
|
PKC
Autophagy
Apoptosis
HIV
RABV
|
Rottlerin, a natural product purified from Mallotus Philippinensis, is a specific PKC inhibitor, with IC50 values for PKCδ of 3-6 μM, PKCα,β,γ of 30-42 μM, PKCε,η,ζ of 80-100 μM. Rottlerin acts as a direct mitochondrial uncoupler, and stimulates autophagy by targeting a signaling cascade upstream of mTORC1. Rottlerin induces apoptosis via caspase 3 activation [1] . Rottlerin inhibits HIV-1 integration and Rabies virus (RABV) infection .
|
-
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-10219S
-
|
Rapamycin-d3 is the deuterium labeled Rapamycin. Rapamycin is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1. Rapamycin is an autophagy activator, an immunosuppressant [1] .
|
-
-
- HY-10219S1
-
|
Rapamycin- 13C,d3 (Sirolimus- 13C,d3; AY-22989- 13C,d3) is the 13C and deuterium labeled Rapamycin (HY-10219) [1]. Rapamycin (Sirolimus; AY 22989) is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1 . Rapamycin is an autophagy activator, an immunosuppressant .
|
-
Cat. No. |
Product Name |
|
Classification |
-
- HY-153493
-
|
|
siRNAs
|
PF-04523655 is a siRNA directed against RTP801 gene. RTP801 is an inhibitor of the mammalian target of rampamycin complex 1 (mTORC1) and downstream transcription factor HIF-1.
|
-
- HY-153493A
-
|
|
siRNAs
|
PF-04523655 sodium is a siRNA directed against RTP801 gene. RTP801 sodium is an inhibitor of the mammalian target of rampamycin complex 1 (mTORC1) and downstream transcription factor HIF-1.
|
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