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AKT-IN-1

" in MedChemExpress (MCE) Product Catalog:

75

阻害剤およびアゴニスト

1

生化学アッセイ試薬

5

ペプチド

2

阻害性抗体

14

天然物

4

同位体標識化合物

1

オリゴヌクレオチド

製品番号 製品名 Target 研究分野 構造式
  • HY-10071
    Y-27632
    Maximum Cited Publications
    533 Publications Verification

    		 ROCK NADPH Oxidase mTOR Reactive Oxygen Species (ROS) NF-κB Apoptosis Akt Autophagy PAK Ras Cancer
    Y-27632 is a ROCK inhibitor with Ki values of 220 nM and 300 nM for ROCK1 and ROCK2, respectively. Y-27632 exerts anti-inflammatory and immunomodulatory effects in systemic lupus erythematosus models by inhibiting the ROCK/NF-κB pathway. Y-27632 enhances autophagy by inhibiting the AKT/mTOR pathway, thereby inducing apoptosis apoptosis in oral squamous cell carcinoma. Y-27632 induces the formation of tunneling nanotubes in ARPE-19 cells and significantly enhances mitochondrial transfer through these channels. Y-27632 promotes neurite outgrowth in PC12 cells by activating the Rac1/NOX1/ROS/AKT/PAK1 signaling cascade [1] .
    Y-27632
  • HY-15431
    Capivasertib
    80+ Cited Publications

    AZD5363

    		 Akt Autophagy Cancer
    Capivasertib (AZD5363) is an orally active and potent pan-AKT kinase inhibitor with IC50 of 3, 7 and 7 nM for Akt1,Akt2 and Akt3, respectively.
    Capivasertib
  • HY-15186
    Ipatasertib
    55+ Cited Publications

    GDC-0068; RG7440

    		 Organoid Akt Apoptosis Cancer
    Ipatasertib (GDC-0068) is an orally active, highly selective and ATP-competitive pan-Akt inhibitor with IC50 values of 5, 18, 8 nM for Akt1/2/3, respectively. Ipatasertib synchronously activates FoxO3a and NF-κB through inhibition of Akt leading to p53-independent activation of PUMA. Ipatasertib also induces apoptosis in cancer cells and inhibits tumor growth in xenograft mouse models [1] .
    Ipatasertib
  • HY-13685
    Miltefosine
    10+ Cited Publications

    HePC; Hexadecyl phosphocholINe

    		 Akt HIV Parasite Infection Cancer
    Miltefosine is a broad spectrum antimicrobial, anti-leishmanial, phospholipid agent acting by inhibiting the PI3K/Akt activity . Miltefosine is an inhibitor of CTP-phosphocholine cytidyltransferase (CCT) .
    Miltefosine
  • HY-15965
    Uprosertib
    15+ Cited Publications

    GSK2141795

    		 Akt Cancer
    Uprosertib (GSK2141795) is a potent and selective pan-Akt inhibitor with IC50 values of 180/328/38 nM for Akt1/Akt2/Akt3, respectively.
    Uprosertib
  • HY-15727
    Afuresertib
    15+ Cited Publications

    GSK2110183; LAE002

    		 Akt PKC ROCK Cancer
    Afuresertib (GSK2110183) is an orally bioavailable, selective, ATP-competitive and potent pan-Akt kinase inhibitor with Kis of 0.08/2/2.6 nM for Akt1/Akt2/Akt3, respectively [1] .
    Afuresertib
  • HY-100018
    BAY1125976
    3 Publications Verification

    		 Akt Cancer
    BAY1125976, a chemical probe, is a selective allosteric Akt1/Akt2 inhibitor; inhibits Akt1 and Akt2 activity with IC50 values of 5.2 nM and 18 nM at 10 μM ATP, respectively.
    BAY1125976
  • HY-122913
    Borussertib

    		Akt Cancer
    Borussertib, a chemical probe, is a covalent-allosteric and first-in-class inhibitor of protein kinase Akt, with an IC50 of 0.8 nM and a Ki of 2.2 nM for Akt wt .
    Borussertib
  • HY-P0119
    Lixisenatide
    2 Publications Verification

    		 GLP Receptor Akt MEK Apoptosis Reactive Oxygen Species (ROS) MMP Cardiovascular Disease Neurological Disease Metabolic Disease Inflammation/Immunology
    Lixisenatide is a glucagon-like peptide-1 (GLP-1) receptor agonist. Lixisenatide inhibits the inflammatory response through down regulation of pro-inflammatory cytokines, and suppresses of the Akt-MEK1/2 signaling pathway. Lixisenatide can inhibit oxidative stress, mitochondrial dysfunction and apoptosis. Lixisenatide can be used for the researches of inflammation, metabolic disease, neurological disease and cardiovascular disease, such as rheumatoid arthritis, diabetes, Alzheimer's disease and atherosclerosis [1] .
    Lixisenatide
  • HY-16071
    AT13148
    2 Publications Verification

    		 Akt PKA ROCK Ribosomal S6 Kinase (RSK) Cancer
    AT13148 is an orally active and ATP-competitive, multi-AGC kinase inhibitor with IC50s of 38 nM/402 nM/50 nM, 8 nM, 3 nM, and 6 nM/4 nM for Akt1/2/3, p70S6K, PKA, and ROCKI/II, respectively.
    AT13148
  • HY-13425
    Deguelin
    Maximum Cited Publications
    15 Publications Verification

    (-)-DeguelIN; (-)-cis-DeguelIN

    		 Akt Autophagy Apoptosis Cancer
    Deguelin, a naturally occurring rotenoid, acts as a chemopreventive agent by blocking multiple pathways like PI3K-Akt, IKK-NF-κB, and MAPK-mTOR-survivin-mediated apoptosis. Deguelin binding to Hsp90 leads to a decreased expression of numerous oncogenic proteins, including MEK1/2, Akt, HIF1α, COX-2, and NF-κB.
    Deguelin
  • HY-N1181
    Tamarixetin
    2 Publications Verification

    4'-O-Methyl QuercetIN

    		 Endogenous Metabolite ClpP Bacterial Apoptosis Akt Interleukin Related COX JNK p38 MAPK Reactive Oxygen Species (ROS) Infection Cardiovascular Disease Inflammation/Immunology Cancer
    Tamarixetin (4'-O-Methyl Quercetin) is an orally active natural flavonoid derivative of quercetin and caseinolytic protease p (ClpP) inhibitor with anti-inflammatory, antioxidant and antitumor effects. Tamarixetin inhibits the hydrolytic activity of ClpP to the fluorescent substrate Suc-LY-AMC with an IC50 of 49.73 μM, which can be used for the study of Staphylococcus aureus infection. Tamarixetin inhibits tumor cell growth, induces apoptosis, and cell cycle arrest. Tamarixetin prevents cardiac hypertrophy by inhibiting the NFAT and AKT pathways .
    Tamarixetin
  • HY-N2292
    Kinsenoside
    4 Publications Verification

    		 Keap1-Nrf2 Apoptosis Inflammation/Immunology
    Kinsenoside is the main active ingredient of the genus plant, and has various biological activities. Kinsenoside and Nrf2 depend on the protection of nuclear cells (NPCs), which significantly reduces their ability to survive. Kinsenoside Active NPC Medium AKT-ERK1/2-Nrf2 Signal passage, Prevent physical decline, aging, harmonious physical function impairment. Kinsenoside can improve the puncture guide model for intermediate vertebral wall discharge (IDD).
    Kinsenoside
  • HY-12494
    LDC1267
    5+ Cited Publications

    		 TAM Receptor FLT3 Neurological Disease Cancer
    LDC1267 is a AXL/TAM/FLT3 inhibitor with IC50 values of 42 nM, 130 nM, and 63 nM against AXL, MERTK, and TYRO3, respectively. LDC1267 blocks GAS6-induced AXL phosphorylation and the downstream AKT/ERK1/2 signaling pathway. LDC1267 inhibits cancer cell proliferation, colony formation, and glioblastoma cell invasion, without causing obvious impairment of cytotoxic autophagic flux. LDC1267 exerts a synergistic effect when used in combination with Imatinib (HY-15463) in chronic myeloid leukemia models. LDC1267 can be widely applied in studies related to glioblastoma and chronic myeloid leukemia [1] .
    LDC1267
  • HY-144806
    PI3K/AKT-IN-1
    10+ Cited Publications

    		 PI3K Akt Apoptosis Cancer
    PI3K/AKT-IN-1 is an effective PI3K/AKT dual inhibitor (IC50 of 6.99, 4.01 and 3.36 μM for PI3Kγ, PI3Kδ and AKT, respectively). PI3K/AKT-IN-1 has anticancer activity and acts by inhibiting PI3K/AKT axis and inducing caspase 3 dependent apoptosis [1].
    PI3K/AKT-IN-1
  • HY-18296
    AKT-IN-1
    5 Publications Verification

    		 Akt Cancer
    AKT-IN-1 is an allosteric AKT inhibitor with an IC50 of 1.042 μM.
    AKT-IN-1
  • HY-P99274
    Xentuzumab
    1 Publications Verification

    BI 836845; Anti-Human IGF1 and IGF2 RecombINant Antibody

    		 IGF-1R Cancer
    Xentuzumab (Anti-Human IGF1 and IGF2 Recombinant Antibody; BI836845) is a recombinant a human monoclonal antibody that targets IGF ligands IGF1 and IGF2. Xentuzumab inhibits both of IGF1 and IGF2 growth-promoting signalling and suppresses AKT activation .
    Xentuzumab
  • HY-107597
    Halicin
    2 Publications Verification

    SU3327

    		 JNK Metabolic Disease Inflammation/Immunology
    Halicin (SU3327) is a potent, selective and substrate-competitive JNK inhibitor with an IC50 of 0.7 μM. Halicin also inhibits protein-protein interactions between JNK and JNK Interacting Protein (JIP) with an IC50 of 239 nM. Halicin shows less active against p38α and Akt kinase .
    Halicin
  • HY-N7110
    6-Hydroxyflavone
    2 Publications Verification

    		 Akt ERK JNK GABA Receptor Neurological Disease Metabolic Disease Inflammation/Immunology
    6-Hydroxyflavone is an orally effective flavonoid compound. 6-Hydroxyflavone can inhibit LPS (HY-D1056) -induced NO production and has anti-inflammatory effects. 6-Hydroxyflavone promotes osteoblast differentiation by activating AKT, ERK 1/2 and JNK signaling pathways. 6-Hydroxyflavone has an inhibitory effect on bovine hemoglobin (BHb) glycosylation. 6-Hydroxyflavone has a kidney protective effect. In addition, 6-Hydroxyflavone enhances GABA-induced current through the Benzodiazepine sites of γ-aminobutyric acid (GABAA) receptors. 6-Hydroxyflavone shows a clear preference for α2 - and α3 - subtypes, which play an anti-anxiety role [1] .
    6-Hydroxyflavone
  • HY-N0616
    Trifolirhizin

    		Tyrosinase TNF Receptor Bacterial Apoptosis Autophagy AMPK mTOR ERK NF-κB Infection Metabolic Disease Inflammation/Immunology Cancer
    Trifolirhizin is a pterocarpan flavonoid found in the roots of Sophora flavescens. Trifolirhizin is a tyrosinase inhibitor with an IC50 value of 506.77 μM. Trifolirhizin reduces intracellular melanin production and modulates multiple signaling pathways including NFκB-MAPK, AMPK/mTOR, PI3K/Akt, MAPK-NFATc1 and EGFR-MAPK. Trifolirhizin targets biological molecules including PTK6 and COX-2, inhibits the activities of hyaluronidase, collagenase and elastase, induces apoptosis, autophagy and cell cycle arrest, and suppresses the proliferation, migration and invasion of cancer cells. Trifolirhizin exerts diverse pharmacological effects including anti-inflammatory, anti-asthmatic, bone-protective, renoprotective, antibacterial, antifungal, hepatoprotective, antiplatelet, estrogenic and wound-healing activities. Trifolirhizin can be used to investigate a broad range of malignant, inflammatory, metabolic and infectious disorders [1] .
    Trifolirhizin
  • HY-40351
    4-Chloro-7H-pyrrolo[2,3-d]pyrimidine

    		Drug Intermediate Others
    4-Chloro-7H-pyrrolo[2,3-d]pyrimidine is a nitrogen-containing heterocyclic organic synthesis intermediate that can be used for the synthesis of JAK and PKB/Akt inhibitors .
    4-Chloro-7H-pyrrolo[2,3-d]pyrimidine
  • HY-15727A
    Afuresertib hydrochloride
    15+ Cited Publications

    GSK2110183 hydrochloride; LAE002 hydrochloride

    		 Akt PKC ROCK Cancer
    Afuresertib hydrochloride (GSK 2110183 hydrochloride) is an orally bioavailable, selective, ATP-competitive and potent pan-Akt kinase inhibitor with Kis of 0.08/2/2.6 nM for Akt1/Akt2/Akt3 respectively [1] .
    Afuresertib hydrochloride
  • HY-N0479
    Licarin B
    1 Publications Verification

    (-)-LicarIN B

    		 PPAR GLUT Metabolic Disease
    Licarin B, a nitric oxide production inhibitor extracted from the component of the seeds of Myristica fragrans, improves insulin sensitivity via PPARγ and activation of GLUT4 in the IRS-1/PI3K/AKT pathway .
    Licarin B
  • HY-12059
    AT7867
    5 Publications Verification

    		 Akt PKA Ribosomal S6 Kinase (RSK) Cancer
    AT7867 is a potent ATP-competitive inhibitor of Akt1/Akt2/Akt3 and p70S6K/PKA with IC50s of 32 nM/17 nM/47 nM and 85 nM/20 nM, respectively.
    AT7867
  • HY-118020A
    Loliolide

    Loliolid; Digiprolactone

    		 Endogenous Metabolite Caspase PI3K Apoptosis Akt Sirtuin Reactive Oxygen Species (ROS) NF-κB MMP Neurological Disease Cancer
    Loliolide (Loliolid) is a β-carotene metabolite. Loliolide reduces caspase 3, 8, 9 expression, enhances PI3K, AKT, SIRT1, inhibits ROS, apoptosis, and blocks NF-κB p65 nuclear translocation. Loliolide protects mitochondria, reduces oxidative stress, and increases cell viability in neuroblastoma cells. Loliolide can be used for the research of UV-induced skin damage and Parkinson’s disease [1] .
    Loliolide
  • HY-N3312
    Matairesinol

    		p38 MAPK JNK NF-κB Metabolic Disease Inflammation/Immunology Cancer
    Matairesinol is an orally active bioactive compound with anti-inflammatory, antioxidant and anticancer activities. Matairesinol inhibits the phosphorylation of MAPK, JNK and NF-κB, downregulates RANKL-induced NFATc1 expression and activity, and suppresses the activation of the PI3K/AKT/FOXO1 pathway. Matairesinol can be used in research related to sepsis-mediated brain injury, osteoporosis, heart failure, atopic dermatitis and cancer [1] .
    Matairesinol
  • HY-N7676
    Marein
    3 Publications Verification

    		 AMPK HDAC Cardiovascular Disease Neurological Disease Metabolic Disease
    Marein has the neuroprotective effect due to a reduction of damage to mitochondria function and activation of the AMPK signal pathway. Marein improves insulin resistance induced by high glucose in HepG2 cells through CaMKK/AMPK/GLUT1 to promote glucose uptake, through IRS/Akt/GSK-3β to increase glycogen synthesis, and through Akt/FoxO1 to decrease gluconeogenesis. Marein is a HDAC inhibitor with an IC50 of 100 μM. Marein has beneficial antioxidative, antihypertensive, antihyperlipidemic and antidiabetic effects [1] .
    Marein
  • HY-P0119A
    Lixisenatide acetate
    2 Publications Verification

    		 GLP Receptor Akt MEK Reactive Oxygen Species (ROS) Apoptosis MMP Cardiovascular Disease Neurological Disease Metabolic Disease Inflammation/Immunology
    Lixisenatide acetate is a glucagon-like peptide-1 (GLP-1) receptor agonist. Lixisenatide acetate inhibits the inflammatory response through down regulation of pro-inflammatory cytokines, and suppresses of the Akt-MEK1/2 signaling pathway. Lixisenatide acetate can inhibit oxidative stress, mitochondrial dysfunction and apoptosis. Lixisenatide acetate can be used for the researches of inflammation, metabolic disease, neurological disease and cardiovascular disease, such as rheumatoid arthritis, diabetes, Alzheimer's disease and atherosclerosis [1] .
    Lixisenatide acetate
  • HY-12059A
    AT7867 dihydrochloride
    5 Publications Verification

    		 Akt PKA Ribosomal S6 Kinase (RSK) Cancer
    AT7867 dihydrochloride is a potent ATP-competitive inhibitor of Akt1/Akt2/Akt3 and p70S6K/PKA with IC50s of 32 nM/17 nM/47 nM and 85 nM/20 nM, respectively.
    AT7867 dihydrochloride
  • HY-121012
    (rac)-AG-205

    		NF-κB Akt Endocrinology
    (rac)-AG-205 is a potent inhibitor of progesterone receptor membrane component 1 (Pgrmc1) that induces genes involved in sterol synthesis, including the INSIG1 protein, which forms a complex with PGRMC1. (rac)-AG-205 prevents neuronal resistance to hypoxic ischaemia by blocking NF-kB signalling and activation of the BDNF/PI3K/AKT pathway .
    (rac)-AG-205
  • HY-16461
    Solenopsin

    (-)-SolenopsIN A

    		 Akt Ribosomal S6 Kinase (RSK) PI3K PDK-1 FOXO Mitophagy Reactive Oxygen Species (ROS) Mitochondrial Metabolism Cardiovascular Disease
    Solenopsin ((-)-Solenopsin A) is an ATP-competitive and selective Akt-1 inhibitor with an IC50 of 5-10 μM, and also acts as an RSK1 inhibitor. Solenopsin inhibits the activities of PDK1 in lipid rafts, downregulates PI3K, blocks PI3K-dependent generation of 3-phosphoinositides, and suppresses the phosphorylation of FOXO1a. Solenopsin induces Mitophagy and ROS production, reduces mitochondrial oxygen consumption, and exhibits antiproliferative and antiangiogenic activities. Solenopsin can be used in research related to hyperproliferative skin diseases and malignant diseases [1] .
    Solenopsin
  • HY-10071A
    Y-27632 hydrochloride hydrate
    395+ Cited Publications

    		 ROCK NF-κB Apoptosis Autophagy Akt mTOR NADPH Oxidase Reactive Oxygen Species (ROS) PAK Ras Neurological Disease Inflammation/Immunology Cancer
    Y-27632 hydrochloride hydrate is a ROCK inhibitor with Ki values of 220 nM and 300 nM for ROCK1 and ROCK2, respectively. Y-27632 hydrochloride hydrate exerts anti-inflammatory and immunomodulatory effects in systemic lupus erythematosus models by inhibiting the ROCK/NF-κB pathway. Y-27632 hydrochloride hydrate enhances autophagy by inhibiting the AKT/mTOR pathway, thereby inducing apoptosis apoptosis in oral squamous cell carcinoma. Y-27632 hydrochloride hydrate induces the formation of tunneling nanotubes in ARPE-19 cells and significantly enhances mitochondrial transfer through these channels. Y-27632 hydrochloride hydrate promotes neurite outgrowth in PC12 cells by activating the Rac1/NOX1/ROS/AKT/PAK1 signaling cascade [1] .
    Y-27632 hydrochloride hydrate
  • HY-131055
    Mytoxin B

    		ADC Payload PI3K Apoptosis Cancer
    Mytoxin B is an ADC cytotoxin. Mytoxin B is a satratoxin-type trichothecene macrolide and is similar to the effect of LY294002 (HY-10108). Mytoxin B induces cell apoptosis via PI3K/Akt pathway .
    Mytoxin B
  • HY-15431R
    Capivasertib (Standard)

    AZD5363 (Standard)

    		 Akt Autophagy Reference Standards Cancer
    Capivasertib (Standard) is the analytical standard of Capivasertib. This product is intended for research and analytical applications. Capivasertib (AZD5363) is an orally active and potent pan-AKT kinase inhibitor with IC50 of 3, 7 and 7 nM for Akt1,Akt2 and Akt3, respectively.
    Capivasertib (Standard)
  • HY-13685R
    Miltefosine (Standard)

    HePC (Standard); Hexadecyl phosphocholINe (Standard)

    		 Akt HIV Parasite Reference Standards Infection Cancer
    Miltefosine (Standard) is the analytical standard of Miltefosine. This product is intended for research and analytical applications. Miltefosine is a broad spectrum antimicrobial, anti-leishmanial, phospholipid agent acting by inhibiting the PI3K/Akt activity . Miltefosine is an inhibitor of CTP-phosphocholine cytidyltransferase (CCT) .
    Miltefosine (Standard)
  • HY-13425R
    Deguelin (Standard)

    (-)-DeguelIN (Standard); (-)-cis-DeguelIN (Standard)

    		 Akt Autophagy Apoptosis Reference Standards Cancer
    Deguelin (Standard) is the analytical standard of Deguelin. This product is intended for research and analytical applications. Deguelin, a naturally occurring rotenoid, acts as a chemopreventive agent by blocking multiple pathways like PI3K-Akt, IKK-NF-κB, and MAPK-mTOR-survivin-mediated apoptosis. Deguelin binding to Hsp90 leads to a decreased expression of numerous oncogenic proteins, including MEK1/2, Akt, HIF1α, COX-2, and NF-κB.
    Deguelin (Standard)
  • HY-15113A
    Y-29794 tosylate

    		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] .
    Y-29794 tosylate
  • HY-N1181R
    Tamarixetin (Standard)

    4'-O-Methyl QuercetIN (Standard)

    		 Reference Standards Endogenous Metabolite ClpP Bacterial Apoptosis Akt Interleukin Related COX JNK p38 MAPK Reactive Oxygen Species (ROS) Infection Cardiovascular Disease Inflammation/Immunology Cancer
    Tamarixetin (Standard) is the analytical standard of Tamarixetin. This product is intended for research and analytical applications. Tamarixetin (4'-O-Methyl Quercetin) is an orally active natural flavonoid derivative of quercetin and caseinolytic protease p (ClpP) inhibitor with anti-inflammatory, antioxidant and antitumor effects. Tamarixetin inhibits the hydrolytic activity of ClpP to the fluorescent substrate Suc-LY-AMC with an IC50 of 49.73 μM, which can be used for the study of Staphylococcus aureus infection. Tamarixetin inhibits tumor cell growth, induces apoptosis, and cell cycle arrest. Tamarixetin prevents cardiac hypertrophy by inhibiting the NFAT and AKT pathways .
    Tamarixetin (Standard)
  • HY-15965A
    Uprosertib hydrochloride

    GSK2141795 hydrochloride

    		 Akt Cancer
    Uprosertib hydrochloride (GSK2141795 hydrochloride) is a potent and selective pan-Akt inhibitor with IC50 values of 180/328/38 nM for Akt1/Akt2/Akt3, respectively.
    Uprosertib hydrochloride
  • HY-122959
    Kihadanin B

    		Akt PPAR Metabolic Disease
    Kihadanin B is a citrus limonoid that can be purified from the peels of immature Citrus unshiu. Kihadanin B suppresses adipogenesis through repression of the Akt-FOXO1-PPARγ axis in 3T3-L1 adipocytes [1].
    Kihadanin B
  • HY-149989
    Ack1 inhibitor 1

    		Ack1 Akt Cancer
    Ack1 inhibitor 1 is a potent, selective, and orally active inhibitor of ACK1 kinase with an IC50 value of 2.1 nM. Ack1 inhibitor 1 inhibits the phosphorylation of ACK1 and activation of downstream AKT. Ack1 inhibitor 1 has anti-tumor activity [1].
    Ack1 inhibitor 1
  • HY-N9968
    Cucurbitacin C

    		Akt Apoptosis Cancer
    Cucurbitacin C is a triterpenoid calabinoid that can be isolated from Cucurbitaceae plants. Cucurbitacin C has anti-cancer activity in vivo and in vitro. Cucurbitacin C can induce cell cycle arrest in G1 or G2/M phase and apoptosis by inhibiting Akt signaling .
    Cucurbitacin C
  • HY-155542
    RORγ antagonist 1

    		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].
    RORγ antagonist 1
  • HY-175848
    NSC 850745

    		c-Met/HGFR STAT Apoptosis Akt VEGFR Bcl-2 Family MDM-2/p53 Caspase Cancer
    NSC 850745 is a selective and potent c-Met/STAT3 inhibitor with IC50 values of 210 and 670 nM. NSC 850745 can inhibit cell proliferation, induce G2/M phase arrest and induce apoptosis. NSC 850745 can downregulate AKT-1, VEGF and Bcl-2 expression and upregulate p53, Bax and caspase expression. NSC 850745 can be used for the research of cancer, such as leukemia and colon cancer [1].
    NSC 850745
  • HY-P991243
    MP-RM-1

    		EGFR Akt Cancer
    MP-RM-1 is an antibody-based, non-competitive ErbB-3 inhibitor with a Kd value of 32.7 nM. MP-RM-1 inhibits both ligand-dependent and ligand-independent ErbB-3 activation, blocks ErbB-2/ErbB-3 heterodimerization, induces ErbB-3 internalization and degradation, and suppresses the phosphorylation of downstream Akt. MP-RM-1 exerts its antagonistic effect through a non-competitive mechanism. MP-RM-1 inhibits tumor growth in melanoma and prostate cancer xenograft models in nude mice and reduces the proliferative activity of tumor cells [1].
    MP-RM-1
  • HY-145244
    APN/AKT-IN-1

    		Akt Cancer
    APN/AKT-IN-1 is a potent and dual inhibitor of APN and AKT with IC50s of 0.21 and 0.27 μM, respectively. APN/AKT-IN-1 can effectively inhibit the phosphorylation of GSK3β, the intracellular substrate of AKT [1].
    APN/AKT-IN-1
  • HY-161891
    EGFR/Akt-IN-1

    		EGFR Akt Cancer
    EGFR/Akt-IN-1 (compound 17) is a potent inhibitor of EGFR/Akt, with the IC50s of 12.89 μM and 10.88 μM in A549 cells, respectively. EGFR/Akt-IN-1 arrestes the cell cycle at the S phase [1].
    EGFR/Akt-IN-1
  • HY-161861
    VEGFR-2/AKT-IN-1

    		VEGFR Akt Cancer
    VEGFR-2/AKT-IN-1 (compound 17) is a dual inhibitor of VEGFR-2 and AKT, with the IC50s of 0.164 μM and 0.452 μM, respectively. VEGFR-2/AKT-IN-1 has antitumor activity [1].
    VEGFR-2/AKT-IN-1
  • HY-173007
    ALK/PI3K/AKT-IN-1

    		Akt PI3K Anaplastic lymphoma kinase (ALK) CDK Apoptosis Mitochondrial Metabolism Cancer
    ALK/PI3K/AKT-IN-1 (Compound 45) inhibits the proliferation of cancer cell A549, H1975 and PC9 with an IC50 of 0.44, 0.83 and 1.51 μM. ALK/PI3K/AKT-IN-1 increases the expression of p21 and p27, inhibits the activity of CDK2 and p-Rb, arrests the cell cycle at G1 phase. ALK/PI3K/AKT-IN-1 inhibits the ALK/PI3K/AKT signaling pathway, promotes the depolarization of mitochondrial membrane potential, and inducing apoptosis in A549 cell. ALK/PI3K/AKT-IN-1 inhibits the formation and growth of A549 cell spheroids [1].
    ALK/PI3K/AKT-IN-1
  • HY-161351
    STAT3/AKT-IN-1

    		Akt STAT Apoptosis Cancer
    STAT3/AKT-IN-1 is a dual inhibitor for the signal transducer and activator of transcription 3 (STAT3) and protein kinase B (AKT) signalling pathway, exhibits antitumor activity against gastric cancer and induces cell apoptosis in SGC-7901 cells [1].
    STAT3/AKT-IN-1

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