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| Cat. No. | Product Name | ||
|---|---|---|---|
| L2191 | 抗乳腺癌化合物库 | 1965 compounds | |
| A unique collection of 1965 compounds with anti-breast cancer therapeutic activity or targeting breast cancer’s major signaling pathways, can be used for anti-breast cancer drug discovery and mechanism study； | |||
| Cat. No. | Product Name | Target | Signaling Pathways |
|---|---|---|---|
| T36310 | AKT-IN-6 | Akt | PI3K/Akt/mTOR signaling; Cytoskeletal Signaling |
| AKT-IN-6 has an inhibitory effect on ATK. Akt is an important component of cellular signaling for growth factors, cytokines, and other cell stimuli. Abnormal Akt activation has been associated with the development of type 2 diabetes mellitus and cancer. | |||
| T5S2178 | Fargesin | Adrenergic Receptor | Neuroscience; GPCR/G Protein |
| 1. Fargesin as a potential β1AR antagonist through cAMP/PKA pathway could protect against myocardial ischemia/reperfusion injury in rats. 2. Fargesin improves dyslipidemia and hyperglycemia by activating Akt and AMPK in WAT. | |||
| T8656 | CAY10404 | COX; Akt; Apoptosis | Immunology/Inflammation; Cytoskeletal Signaling; Apoptosis; Neuroscience; PI3K/Akt/mTOR signaling |
| CAY10404 is a potent and highly selective inhibitor of COX-2 and COX-1. It is also a potent inhibitor of PKB/Akt and MAPK signalling pathways and induces apoptosis in NSCLC cells, with analgesic, anti-inflammatory and anti-cancer activities. | |||
| T5S1331 | Herbacetin | Akt; c-Met/HGFR | Tyrosine Kinase/Adaptors; Cytoskeletal Signaling; PI3K/Akt/mTOR signaling |
| 1. Herbacetin induces apoptosis in HepG2 cells, by ROS and PI3K/Akt pathway. 2. Herbacetin suppresses the HGF-induced motility of human breast cancer MDA-MB-231 cells by inhibiting c-Met and Akt phosphorylation. | |||
| T3729 | Ethyl gallate | NF-κB; MMP; Akt; Antibacterial | Cytoskeletal Signaling; PI3K/Akt/mTOR signaling; Proteases/Proteasome; Microbiology/Virology; NF-κB |
| Ethyl gallate obviously decreases cell proliferation in MDA-MB-231 and MCF-7 cells in a dose- and time-dependent manner, exhibits cytotoxicity in a dose-dependent manner. Ethyl gallate can inhibit the abilities of invasion of breast cancer in vitro by inh | |||
| T5S0055 | Chelidonine | Apoptosis; Influenza Virus; Others | Microbiology/Virology; Apoptosis; Others |
| 1. Chelidonine isolated from Chelidonium majus efficiently induced apoptosis in HeLa cells through possible alteration of p38-p53 and AKT/PI3 kinase signalling pathways. 2. Chelidonine is a promising model compound for overcoming MDR and for enhancing cyt | |||
| T14214 | AMG 511 | PI3K | PI3K/Akt/mTOR signaling |
| AMG 511 is a potent and orally available pan inhibitor of class I PI3Ks(Kis of 4 nM, 6 nM, 2 nM and 1 nM for PI3Kα, β, δ and γ, respectively). It exhibits anti-tumor activity in mouse glioblastoma xenograft model[1]. AMG 511 significantly suppresses PI3K | |||
| T4S1419 | (±)-Praeruptorin A | Calcium Channel; p38 MAPK; Akt | MAPK; Metabolism; Cytoskeletal Signaling; Membrane transporter/Ion channel; PI3K/Akt/mTOR signaling |
| 1. Praeruptorin A could exhibit its anti-osteoclastogenic activity by inhibiting p38/Akt-c-Fos-NFATc1 signaling and PLCγ-independent Ca(2+) oscillation 2. Praeruptorin A has the potential to inhibit migration/fusion of preosteoclasts in vitro and bone ero | |||
| T6S0659 | Rhynchophylline | Calcium Channel; NF-κB | Metabolism; NF-κB; Membrane transporter/Ion channel |
| 1. Rhynchophylline can protect against ischemic damage, probably via regulating the Akt/mTOR pathway. 2. Rhynchophylline can protect against glutamate-induced neuronal death, can inhibit MA impairment in cultured neurons in vitro. 3. Rhynchophylline and i | |||
| T4444 | A-674563 HCl (552325-73-2(free base)) | PKA; Akt; ERK; PKC; CDK | MAPK; Cell Cycle/Checkpoint; Cytoskeletal Signaling; Chromatin/Epigenetic; Tyrosine Kinase/Adaptors; PI3K/Akt/mTOR signaling |
| A-674563 is an orally available, ATP-competitive, and reversible inhibitor of Akt (Ki: 11 nM for Akt1) [1]. It exhibits inhibitory activity against PKA and Cdk2 (IC50: 16/46 nM) but is 10- to >1, 800-fold selective for Akt1 versus additional kinases in th | |||
| T1952 | MK-2206 dihydrochloride | Apoptosis; Akt; Autophagy | Apoptosis; Autophagy; Cytoskeletal Signaling; PI3K/Akt/mTOR signaling |
| MK-2206 dihydrochloride 是具有口服活性的，高效选择性的变构Akt抑制剂，对 Akt1、Akt2 和 Akt3 的IC50分别为 8、12 和 65 nM。它具有抗癌活性。 | |||
| T4S0498 | Glaucocalyxin A | PI3K; Caspase; Apoptosis; Akt | PI3K/Akt/mTOR signaling; Cytoskeletal Signaling; Apoptosis; Proteases/Proteasome |
| 1. Glaucocalyxin A-SBE-β-CD could be useful with a better solubility and sustained function in drug delivery. 2. Glaucocalyxin A activates caspase-3, decreases BAD phosphorylation, and reduces the expression of X-linked inhibitor of apoptosis protein. 3. | |||
| T2966 | Beta-Sitosterol | Endogenous Metabolite; Lipase; Apoptosis | Metabolism; Apoptosis |
| β-Sitosterol has recently been shown to induce G2/M arrest, endoreduplication, and apoptosis through the Bcl-2 and PI3K/Akt signaling pathways. β-Sitosterol, a main dietary phytosterol found in plants, may have the potential for prevention and therapy for | |||
| T6S0653 | Linarin | TNF; AChE | Neuroscience; Apoptosis |
| 1. Linarin (acacetin-7-O-β-d-rutinoside) shows selective dose dependent inhibitory effect on acetylcholinesterase. 2. Linarin alleviates GalN/LPS-induced liver injury by suppressing TNF-α-mediated apoptotic pathways. 3. Linarin prevents A beta-induced neu | |||
| T6S2099 | Geraniin | TNF; Antioxidant | oxidation-reduction; Apoptosis |
| 1. Geraniin has a protective effect against OVX-induced rat osteoporosis. 2. Geraniin has cytotoxic activity towards cancer cells in vitro and in vivo. 3. Geraniin exerts inhibitory effects on osteoclast differentiation in vitro and suppresses Ti particle | |||
| T3923 | Calycosin | Tyrosinase; Apoptosis | Proteases/Proteasome; Apoptosis |
| Calycosin acts as a selective estrogen receptor modulator. Calycosin induces apoptosis in human ovarian cancer SKOV3 cells by activating caspases and Bcl-2 family proteins. Calycosin suppresses breast cancer cell growth via ERβ-dependent regulation of IGF | |||
| T6S0525 | Farrerol | ERK; p38 MAPK; Akt | Cytoskeletal Signaling; MAPK; PI3K/Akt/mTOR signaling |
| 1. Farrerol has antioxidative activity.2. Farrerol modulates TAP and BNBD5 gene expression in mammary gland, enhances bMEC defense against S. aureus infection and could be useful in protection against bovine mastitis. 3. Farrerol inactivates KEAP-1 or act | |||
| T6S1315 | Oroxylin A | Autophagy; HIF/HIF Prolyl-Hydroxylase; Virus Protease | Microbiology/Virology; Metabolism; Autophagy; Chromatin/Epigenetic |
| 1. Oroxylin A has various anti-tumor effects including apoptosis, cell cycle arrest, drug-resistant reversion. 2. Oroxylin A possesses abilities of inhibiting the ATRA-induced IL-6 production via modulation of LAP/LIP/CHOP in leukemia cell lines, which co | |||
| T6S1699 | Shogaol | Autophagy; Lipoxygenase | Autophagy; Metabolism |
| 1. 6-Shogaol has antipyretic and analgesic effects in addition to inhibitory effect on lipoxygenase activity. 2. 6-shogaol has anti-inflammatory property, reduces the inflammatory response and protected the femoral cartilage from damage produced in a CFA | |||
| T2S0410 | Euphorbia factor L1 | Apoptosis; P-gp | Membrane transporter/Ion channel; Neuroscience; Apoptosis |
| 1. Euphorbia factor L1 can enhance the ATP hydrolysis activity of ABCB1 stimulated by verapamil. 2. Euphorbia factor L1 inhibits the efflux of ABCB1 in KBv200 and MCF-7/adr cells, does not downregulate their expression either in mRNA or protein level. | |||
| T3211 | Midostaurin | PKC; Others | Chromatin/Epigenetic; Others; Cytoskeletal Signaling |
| PKC412(Midostaurin; CGP41231; CGP41251) is a broad spectrum protein kinase inhibitor. Midostaurin inhibits protein kinase C alpha (PKCalpha), vascular endothelial growth factor receptor 2 (VEGFR2), c-kit, platelet-derived growth factor receptor (PDGFR) an | |||
| T4S21320 | ISOGINKGETIN | Others; MMP | Others; Proteases/Proteasome |
| 1. Isoginkgetin, a compound derived from the leaves of Ginkgo biloba, to up-regulate adiponectin secretion with potency comparable to that of rosiglitazone, a known modulator of adiponectin production. 2. Isoginkgetin has anti-tumor activity, the mechanis | |||
| T5S1097 | Neferine | Apoptosis; NF-κB; Autophagy | NF-κB; Autophagy; Apoptosis |
| 1. Neferine has anti-tumor activities , Metabolic activation mediated by CYP3A4 and GSH depletion enhanced Neferine-induced cytotoxicity. 2. Neferine can be helpful to increase the efficacy of DOX and to achieve anticancer synergism by curbing the toxicit | |||
| T6S1740 | Nardosinone | Others | Others |
| 1. Nardosinone has inhibitory effect on Ang II-induced hypertrophy in H9c2 cells, might be mediated by targeting PI3K/Akt and MEK/ERK signaling pathways. 2. Nardosinone could protect against the neuronal injury exposed to OGD, which may be relevant to the | |||
| T5S1982 | Periplocin | Others; Apoptosis | Others; Apoptosis |
| 1. Periplocin has anti-cancer effects on lung cancer cells, induces apoptosis and inhibits growth of cancer cells by the beta-catenin/Tcf signaling pathway. 2. Periplocin is used for treatment of rheumatoid arthritis, reinforcement of bones and tendons, p | |||
| T2940 | 6-Hydroxyflavone | GABA Receptor | Neuroscience; Membrane transporter/Ion channel |
| 6-Hydroxyflavone is a noncompetitive inhibitors of cytochrome P450 2C9. It is a flavone, a type of chemical compound. It is reported in leaves of Barleria prionitis Linn. (a common Acanthaceae from India). 6-Hydroxyflavone may have a potential as a therap | |||
| T3S0209 | Vincristine | NF-κB; mTOR; JNK; ERK; p38 MAPK; Akt | Cytoskeletal Signaling; NF-κB; PI3K/Akt/mTOR signaling; MAPK |
| Vincristine binds to tubulin and inhibits the formation of microtubules, thereby inhibiting mitosis of the cancer cell. Vincristine can be used as a microtubule-destabilizing agent for research on the treatment of hematologic cancers, such as leukemia and | |||
| T3895 | Polyphyllin I | Autophagy; JNK; mTOR; PDK; Akt; Apoptosis | PI3K/Akt/mTOR signaling; Cytoskeletal Signaling; Autophagy; Apoptosis; MAPK |
| Polyphyllin D induces apoptosis via the mitochondrial apoptotic pathway as evidenced by decreased Bcl-2 expression levels, disruption of MMP and increased Bax, cytochrome C, and cleaved-caspase-3 levels. Polyphyllin D has an anti-angiogenic effect. Polyph | |||
| T6S1559 | Aurantio-obtusin | Others | Others |
| 1. Biotransformation of glucoAurantio-obtusin towards Aurantio-obtusin increased the toxicity of irinotecan through increased inhibition of SN-38 glucuronidation. 2. Aurantio-obtusin, stimulated chemotactic migration of MC3T3-E1 osteoblast cells in a conc | |||
| T3826 | Polygalasaponin F | TLR; PI3K; NF-κB; Akt | Immunology/Inflammation; NF-κB; Cytoskeletal Signaling; PI3K/Akt/mTOR signaling |
| Polygalasaponin F has anti-neuroinflammatory activity, can inhibit the release of inflammatory cytokines TNF-α and NO induced by lipopolysaccharides (LPS) and reduce the expression of inducible nitric oxide synthases. Polygalasaponin F can significantly i | |||
| T2S2215 | Crebanine | Apoptosis; Akt; Others | PI3K/Akt/mTOR signaling; Others; Cytoskeletal Signaling; Apoptosis |
| 1. Crebanine iv 5mg/kg can eonvert BaCl_2-induced arrhythmia into sinus rhythm in rats, and can significantly increase the tolerant dose of aconitine to produce ventrieular fibrillation(VF) and cardiac arrest (CA) in rata. 2. Crebanine can also decrease t | |||
| T10274 | AKT-IN-2 | Akt | Cytoskeletal Signaling; PI3K/Akt/mTOR signaling |
| AKT-IN-2 is a selective, and orally bioavailable AKT inhibitor (IC50: 5 nM for AKT1). | |||
| T60564 | PI3K/Akt/mTOR-IN-2 | ||
| PI3K/Akt/mTOR-IN-2 is an inhibitor of PI3K/AKT/mTOR pathway. PI3K/Akt/mTOR-IN-2 can induce cancer cell cycle arrest and apoptosis. PI3K/Akt/mTOR-IN-2 shows anti-cancer effects and selectivity against MDA-MB-231 cells with IC 50 value of 2.29 μM [1]. | |||
| T35489 | 1-O-Octadecyl-2-O-methyl-sn-glycerol | ||
| 1-O-Octadecyl-2-O-methyl-sn-glycerol is a metabolite of a phosphotidylinositol ether lipid analog (PIA). PIAs are known to target the pleckstrin homology domain of the serine/threonine kinase Akt and to induce apoptosis in cancer cell lines with high levels of endogenous Akt activity. | |||
| T35490 | 2-Amino-5-bromo-6-chloropyrazine | ||
| 2-Amino-5-bromo-6-chloropyrazine is a heterocyclic building block.1,2It has been used in the synthesis of Akt inhibitors. 1.Kettle, J.G., Brown, S., Crafter, C., et al.Diverse heterocyclic scaffolds as allosteric inhibitors of AKTJ. Med. Chem.55(3)1261-1273(2012) 2.Goel, R., Luxami, V., and Paul, K.Recent advances in development of imidazo[1,2-a]pyrazines: Synthesis, reactivity and their biological applicationsOrg. Biomol. Chem.13(12)3525-3555(2015) | |||
| T62013 | PI3Kδ-IN-10 | ||
| PI3Kδ-IN-10 is a highly potent and orally active PI3Kδ inhibitor (IC50= 2 nM). In hepatocellular carcinoma models, PI3Kδ-IN-10 robustly suppresses the downstream AKT pathway to induce subsequent apoptosis. | |||
| T29543 | ACAF4 | ||
| ACAF4 is a neurotrophic agent which significantly increases survival in PC12 neuronal cells and enhances the effect of nerve growth factor (NGF). ACAF4 induces neurite outgrowth, and modulates ERK1/2 and AKT signaling pathways. | |||
| TN6419 | Chamaejasmine | ||
| Chamaejasmine could be a candidate drug for osteosarcoma and breast cancer chemoprevention, induces apoptosis in MG63 and HEp-2 cells by Akt inactivation and dephosphorylation of BAD. It inhibits Bcl-2 expression and induces Bax expression to desintegrate | |||
| T70926 | BRN-103 | ||
| BRN-103 was found to suppress the VEGF-induced phosphorylation of VEGF receptor 2 (VEGR2) and the activations of AKT and eNOS. Taken together, these results suggest that BRN-103 inhibits VEGF-mediated angiogenesis signaling in human endothelial cells. | |||
| T63967 | Multi-kinase-IN-2 | ||
| Multi-kinase-IN-2 is an orally active inhibitor of angiokinases. multi-kinase-IN-2 significantly inhibits the activity of angiokinases such as VEGFR-1/2/3, PDGFRα/β, FGFR-1, LYN and c-KIT kinases. -IN-2 significantly attenuates phosphorylation of AKT and ERK proteins, induces apoptosis and has anticancer effects. | |||
| T61522 | Nrf2/HO-1 activator 2 | ||
| Nrf2/HO-1 activator 2 (compound 13m), difluoro-substituted derivative, is a potent Nrf2/HO-1 activator. Nrf2/HO-1 activator 2 has neuroprotective and antioxidant effects through the Nrf2/HO-1 pathway mediated by phosphorylation of ERK1/2, JNK, or Akt in PC12 cells. Nrf2/HO-1 activator 2 can be used in the research of Parkinson's disease (PD) [1]. | |||
| TN5100 | Taspine | MAPK; ERK; Akt; BCL; EGFR; VEGFR | MAPK; Tyrosine Kinase/Adaptors; PI3K/Akt/mTOR signaling; Cytoskeletal Signaling; JAK/STAT signaling; Angiogenesis; Apoptosis |
| Taspine shows antitumor activity by modulating the EGFR signaling pathway of Erk1/2 and Akt in vitro and in vivo, it can inhibit growth and induce apoptosis of HUVEC in a dose-dependent manner, it has shown meaningful angiogenesis activity. Taspine exhibi | |||
| T69990 | Ruboxistaurin mesylate monohydrate | ||
| Ruboxistaurin mesylate monohydrate is a PKC beta inhibitor potentially for the treatment of diabetic nephropathy and diabetic macular edema. Ruboxistaurin attenuates diabetic nephropathy via modulation of TGF-β1/Smad and GRAP pathways. Ruboxistaurin reduces oxidative stress and attenuates left ventricular hypertrophy and dysfunction in rats with streptozotocin-induced diabetes. Ruboxistaurin inhibits retinal neovascularization via suppression of phosphorylation of ERK1/2 and Akt. | |||
| T3689L | Ruboxistaurin mesylate | ||
| Ruboxistaurin is a PKC beta inhibitor. Ruboxistaurin reduces oxidative stress and attenuates left ventricular hypertrophy and dysfunction in rats with streptozotocin-induced diabetes. Ruboxistaurin attenuates diabetic nephropathy via modulation of TGF-β1/ | |||
| T35855 | AAA | ||
| AAA is an antagonist of G protein-coupled receptor 75 (GPR75).1It increases basal GPR75 protein levels and inhibits 20-HETE-induced reductions in GPR75 protein levels in PC3 cells. AAA (5 and 10 μM) also reduces 20-HETE-induced phosphorylation of EGFR, NF-κB, and Akt in, and cell migration of, PC3 cells.In vivo, AAA (10 mg/kg per day) reduces systolic blood pressure, albuminuria, renal angiotensin II levels, and cardiac hypertrophy in a Cyp1a1-Ren-2 transgenic rat model of malignant hypertension... | |||
| T68980 | MRK003 | ||
| MRK003 is a γ-secretase inhibitor exhibits promising in vitro pre-clinical activity in multiple myeloma and non-Hodgkin's lymphoma. MRK003 treatment induced caspase-dependent apoptosis and inhibited proliferation of MM and NHL cell lines and patient cells. Examination of signaling events after treatment showed time-dependent decrease in levels of the notch intracellular domain, Hes1 and c-Myc. MRK003 downregulated cyclin D1, Bcl-Xl and Xiap levels in NHL cells and p21, Bcl-2 and Bcl-Xl in MM cel... | |||
| TN4168 | Grifolin | Others | Others |
| Grifolin has anti-cancer effects, it induces apoptosis and promotes cell cycle arrest in the A2780 human ovarian cancer cell line via inactivation of the ERK1/2 and Akt pathways; it enhances the differentiation and proliferation of oligodendrocyte precurs | |||
| TN4046 | Excisanin A | PARP; PI3K; Caspase; GSK-3; JNK; Prostaglandin Receptor; Akt; NF-κB; MMP; FAK; Wnt/beta-catenin | DNA Damage/DNA Repair; Apoptosis; GPCR/G Protein; Stem Cells; Chromatin/Epigenetic; NF-κB; Immunology/Inflammation; Cytoskeletal Signaling; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors; Proteases/Proteasome; MAPK; Angiogenesis |
| ExcisaninA may be a potent inhibitor of AKT signaling pathway in tumor cells, it can inhibit invasion by suppressing MMP-2 and MMP-9 expression, it may be a potential anti-metastatic chemotherapeutic agent for the treatment of breast cancer. Excisanin A s | |||
| T63939 | JBJ-09-063 | ||
| JBJ-09-063 is a mutation-selective variant EGFR inhibitor that acts on EGFR L858R (IC50: 0.147 nM), EGFR L858R/T790M (IC50: 0.063 nM), EGFR L858R/T790M/C797S (IC50: 0.083 nM) and EGFRLT/L747S (IC50: 0.396 nM). JBJ-09-063 is effective in both EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models.JBJ-09-063 is effective in reducing EGFR, Akt and ERK1/2 phosphorylation.JBJ-09-063 can be used to study EGFR mutant lung cancer. | |||
| T4S0083 | Protostemonine | Others | Others |
| 1. Protostemonine has anti-inflammatory activity, it effectively attenuates LPS-induced inflammatory responses in vitro and in vivo; the beneficial effects are associated with the decreased phosphorylation of MAPK and AKT and the reduced expression of pro | |||
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