mTORC1 Inhibitor

JPS004 is a PROTAC degrader targeting HDAC1, HDAC2 and HDAC3. JPS004 induces extensive transcriptomic changes in human colon cancer cell line HCT116, including downregulation of HDAC complex components and cell cycle regulatory machinery, modulation of the AKT/mTOR signaling pathway, and upregulation of FOXO-mediated apoptosis and autophagy related genes. JPS004 can be used in colon cancer-related research.

PPM-18 (NSC 73233) is a Vitamin K (HY-B2172) analog. PPM-18 prevents LPS-induced IκBα degradation, thereby inhibiting NF-κB activation and nuclear translocation of NF-κB. PPM-18 inhibits LPS-induced nitrite production and iNOS expression. PPM-18 inhibits HDAC6. PPM-18 induces ROS accumulation, activates AMPK, inhibits the mTORC1 and PI3K/AKT pathways, initiates Autophagy, and induces Apoptosis. PPM-18 suppresses seizures in zebrafish and mouse epilepsy models. PPM-18 prevents LPS-induced lethal toxicity and delayed hypotension. PPM-18 exhibits anticancer activity against leukemia and bladder cancer. PPM-18 can be used in research related to septic shock, bladder cancer and atherosclerosis.

CIDD-0067106 is a selective mTORC1 pathway inhibitor targeting androgen receptor-positive (AR+) triple-negative breast cancer (TNBC). CIDD-0067106 demonstrates potent inhibition of AR+ TNBC cell lines with an GI₅₀ value of 0.8 μM. CIDD-0067106 is promising for research of AR+ TNBC.

mTORC1-IN-3 is a potent and selective mTORC1 inhibitor with an IC₅₀ of 26.38 μM . mTORC1-IN-3 selectively inhibits the phosphorylation of mTORC1 substrates and does not without affect the phosphorylation of mTORC2 substrate. mTORC1-IN-3 can reduce cellular lipid accumulation and induce autophagy. mTORC1-IN-3 can be used for the researches of cancer, immunology, metabolic and neurological disease, such as diabetes and Alzheimer’s disease.

eALM1137 is a mTOR inhibitor with an IC₅₀ of 4.8 nM. eALM1137 mediates dual inhibition of the mTORC1 and mTORC2 signaling pathways, and inhibits DNA-PK (IC₅₀=77 nM). eALM1137 exhibits antiproliferative and cytostatic activities, and induces G1 cell cycle arrest. eALM1137 is applicable to the research of glioblastoma multiforme.

M-1111 is a Rapa-Link inhibitor. M-1111 is covalently linked by Rapamycin (HY-10219) and an inhibitor of the active site mTOR. M-1111 has strong inhibitory activity on the mTORC1 signaling pathway (pS6 and p4E-BP1). M-1111 has nanomolar-level inhibitory activity against various cancer cells. M-1111 completely inhibits p4E-BP1 without inhibiting pAkt S473. M-1111 can be used for research on liver cancer, kidney cancer, and colorectal cancer.

Nur77 modulator 3 is a Nur77 modulator. Nur77 modulator 3 induces Nur77 expression, inhibits hepatic stellate cells (HSCs) activation, and reduces extracellular matrix (ECM) deposition. Nur77 modulator 3 enhances Nur77-denpendent autophagic flux and significantly inhibits the mTORC1 signaling pathway. Nur77 modulator 3 ameliorates HSCs activation, inflammation and hepatic fibrosis in vivo.

NV-5440 (Compound I-120) is an mTORC1 inhibitor and glucose transporter inhibitor. NV-5440 targets GLUT-1, -2, -3, and -4, and shows no activity against GLUT-5. NV-5440 inhibits glucose uptake.

Rapamycin-¹³C,d₃-1 (Sirolimus-¹³C,d₃-1) is the deuterated, ¹³C-labeled Rapamycin (HY-10219). Rapamycin (Sirolimus; AY 22989) is a potent and specific blood-brain barrier-transmissible mTOR inhibitor with an IC₅₀ of 0.1 nM in HEK293 cells. Rapamycin is a molecular glue that binds FKBP12 and mTOR proteins together, thereby inhibiting mTOR kinase activity. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1. Rapamycin is an autophagy activator, an immunosuppressant.

Sapanisertib (INK-128; MLN0128; TAK-228) Standard is the analytical standard of Sapanisertib (HY-13328). This product is intended for research and analytical applications. Sapanisertib (INK-128; MLN0128; TAK-228) is an orally active dual mTORC1/mTORC2 inhibitor. Sapanisertib directly and simultaneously inhibits mTORC1/2 activity through competitive binding with ATP, thereby comprehensively blocking downstream processes such as protein and lipid synthesis and cytoskeletal reorganization, consequently suppressing tumor cell proliferation and promoting apoptosis. Sapanisertib is applicable to research on melanoma, ovarian cancer, pulmonary fibrosis, and hematological malignancies.

(S)-2-Amino-5,5,5-trifluoropentanoic acid ((S)-5,5,5-Trifluoronorvaline; H-Nva (5,5,5-triF)-OH) is a selective Sestrin-GATOR2 modulator that indirectly inhibits mTORC1 activity via a competitive binding mechanism. (S)-2-Amino-5,5,5-trifluoropentanoic acid can be used in research on cancer, metabolic diseases, neurodegenerative diseases, and muscle atrophy.\n

Nuvisertib (Standard) (TP-3654 (Standard)) is the analytical standard of Nuvisertib (HY-101126). This product is intended for research and analytical applications. Nuvisertib (TP-3654) is an orally active second-generation pan-PIM kinase inhibitor with K_i values of 5 nM, 239 nM, and 42 nM against PIM-1, PIM-2, and PIM-3, respectively. Nuvisertib inhibits JAK-independent inflammatory and survival signaling pathways, reduces the production of proinflammatory cytokines, restores apoptotic sensitivity, inhibits mTORC1, MYC, and TGF-β signaling pathways, and decreases the expression of fibrosis markers. Nuvisertib selectively impairs the transport function of ABCG2, resensitizes multidrug-resistant cancer cells to cytotoxic drugs, and overcomes JAK2 inhibitor resistance. Nuvisertib can be used in research related to myelofibrosis, renal cell carcinoma, multidrug-resistant cancer, advanced solid tumors, urothelial carcinoma, and prostate adenocarcinoma.

Endoxifen Z-isomer methanesulfonate is an orally active selective PKCβ1 inhibitor with an IC₅₀ of 360 nM against human PKCβ1. It also acts as an estrogen receptor modulator and antiestrogen. Endoxifen Z-isomer methanesulfonate binds to and blocks ERα, ERβ and PKCβ1, inhibits estrogen and PI3K/AKT/mTORC1 signaling pathways, suppresses the expression of genes associated with cell cycle, cell proliferation and extracellular matrix remodeling, and induces apoptosis, reactive oxygen species (ROS) production and hypoxic features. Endoxifen Z-isomer methanesulfonate inhibits tumor growth in breast tumor and glioblastoma models, reduces bone turnover and blood lipid levels, and does not require metabolism via CYP2D6. It can be used in research related to ER⁺ breast cancer, invasive breast cancer, glioblastoma multiforme, type I bipolar disorder, desmoid tumor, gynecological malignancies, melanoma and hormone receptor-positive solid tumors.

Nuvisertib hydrochloride (TP-3654 hydrochloride) is an orally active second-generation pan-PIM kinase inhibitor with K_i values of 5 nM, 239 nM, and 42 nM against PIM-1, PIM-2, and PIM-3, respectively. Nuvisertib hydrochloride inhibits JAK-independent inflammatory and survival signaling pathways, reduces the production of proinflammatory cytokines, restores apoptotic sensitivity, inhibits mTORC1, MYC, and TGF-β signaling pathways, and decreases the expression of fibrosis markers. Nuvisertib hydrochloride selectively impairs the transport function of ABCG2, resensitizes multidrug-resistant cancer cells to cytotoxic drugs, and overcomes JAK2 inhibitor resistance. Nuvisertib hydrochloride can be used in research related to myelofibrosis, renal cell carcinoma, multidrug-resistant cancer, advanced solid tumors, urothelial carcinoma, and prostate adenocarcinoma.

Sapanisertib (INK-128; MLN0128; TAK-228) phosphate is an orally active dual mTORC1/mTORC2 inhibitor. Sapanisertib phosphate directly and simultaneously inhibits mTORC1/2 activity through competitive binding with ATP, thereby comprehensively blocking downstream processes such as protein and lipid synthesis and cytoskeletal reorganization, consequently suppressing tumor cell proliferation and promoting apoptosis. Sapanisertib phosphate is applicable to research on melanoma, ovarian cancer, pulmonary fibrosis, and hematological malignancies.