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EGFR activator
Isoprocurcumenol is a guaiane-type sesquiterpene isolated from *Curcuma comosa* with notable bioactivity in epidermal growth factor receptor (EGFR) signaling. It activates EGFR and enhances downstream phosphorylation of ERK and AKT, key mediators of cell survival and proliferation pathways. As a result, isoprocurcumenol promotes keratinocyte proliferation, suggesting potential applications in skin regeneration, wound healing, and dermatological research. -
BMP receptor agonist
SY-LB-35 is a potent agonist of bone morphogenetic protein (BMP) receptors, capable of activating both canonical and non-canonical signaling pathways. In the C2C12 myoblast cell line, SY-LB-35 significantly enhances cell proliferation and viability, promoting cell cycle progression by increasing the proportion of cells in the S and G2/M phases. Mechanistically, it activates the canonical Smad pathway as well as non-canonical PI3K/Akt, ERK, p38, and JNK signaling cascades. These properties make SY-LB-35 a valuable tool for studying BMP-related cellular processes and a potential therapeutic candidate for tissue regeneration and muscle repair. -
PROTAC AKT degrader
INY-05-040 is a potent and selective PROTAC degrader targeting all three isoforms of AKT (AKT1, AKT2, and AKT3). It induces rapid proteasomal degradation of AKT, effectively inhibiting downstream signaling pathways such as PI3K/AKT/mTOR, which are critical for cancer cell survival and proliferation. INY-05-040 demonstrates broad antiproliferative activity across 288 cancer cell lines, highlighting its potential as a powerful therapeutic agent for targeting AKT-driven malignancies. -
HDAC inhibitor
Marein is a natural compound with multifaceted pharmacological properties, including HDAC inhibition with an IC₅₀ of 100 μM. It exerts neuroprotective effects by preserving mitochondrial function and activating the AMPK signaling pathway. In HepG2 cells, Marein improves high glucose–induced insulin resistance by enhancing glucose uptake via the CaMKK/AMPK/GLUT1 pathway, promoting glycogen synthesis through the IRS/Akt/GSK-3β pathway, and suppressing gluconeogenesis via the Akt/FoxO1 axis. Additionally, Marein possesses antioxidative, antihypertensive, antihyperlipidemic, and antidiabetic properties, making it a promising candidate for metabolic and neurodegenerative disease research. -
FFAR3 agonist
AR420626 is a selective agonist of free fatty acid receptor 3 (FFAR3, also known as GPR41), with an IC₅₀ of 117 nM. It demonstrates anti-inflammatory, antitumor, and antidiabetic activities. AR420626 improves neurogenic diarrhea by modulating neural pathways mediated by nicotinic acetylcholine receptors (nAChRs). In cancer models, it suppresses the growth of HepG2 xenografts and inhibits hepatoma cell proliferation through apoptosis induction. Additionally, AR420626 mitigates allergic asthma and eczema and enhances glucose uptake by activating FFAR3-mediated Ca²⁺ signaling, offering potential therapeutic benefits in metabolic disorders such as diabetes. -
PIK3CG PROTAC degrader
ARM165 is a heterobifunctional PROTAC molecule that targets and degrades PIK3CG (PI3Kγ), effectively inhibiting the PI3Kγ-Akt signaling pathway. It exhibits potent antileukemic activity, suppressing the proliferation of acute myeloid leukemia (AML) cells with an IC₅₀ of less than 1 μM. ARM165 is a promising tool for investigating PI3Kγ-driven signaling and developing targeted therapies for leukemia. -
AKT PROTAC degrader
MS15 TFA is a potent and selective PROTAC degrader targeting AKT isoforms. It inhibits the activity of AKT1, AKT2, and AKT3 with IC₅₀ values of 798 nM, 90 nM, and 544 nM, respectively. MS15 TFA serves as a valuable tool for studying AKT signaling and its role in cancer and metabolic diseases. -
PROTAC PIKfyve degrade
PIK5-12d is a potent PROTAC degrader targeting PIKfyve, with a DC₅₀ of 1.48 nM. It induces extensive cytoplasmic vacuolization, disrupts autophagic flux, and inhibits proliferation in multiple prostate cancer cell lines. PIK5-12d exhibits notable anti-tumor activity, supporting its use in cancer research. -
PROTAC Akt Degrader
INY-03-041 is a potent and highly selective PROTAC-based pan-AKT degrader that targets AKT1, AKT2, and AKT3 with IC₅₀ values of 2.0 nM, 6.8 nM, and 3.5 nM, respectively. It is composed of the ATP-competitive AKT inhibitor GDC-0068 linked to the cereblon ligand lenalidomide, making it a valuable tool for studying AKT signaling and targeted cancer therapy. -
PI3K Activator
UCL-TRO-1938 is a potent allosteric activator of phosphoinositide 3-kinase alpha (PI3Kα), exhibiting an EC50 value of approximately 60 μM. This compound promotes cell proliferation and demonstrates cardioprotective effects against ischemia-reperfusion injury. Additionally, UCL-TRO-1938 enhances nerve regeneration following nerve crush, making it a valuable tool in neuroprotection and regenerative medicine research. -
PI3Kα Inhibitor
Tersolisib is a selective allosteric inhibitor of PI3Kα, specifically designed to target mutant forms of the enzyme. This compound exhibits significant anti-tumor activity, demonstrating robust and durable regression in various cancer models. Tersolisib is valuable in cancer research, particularly for studies focusing on PI3K pathway alterations and their therapeutic implications. -
PI3K/Akt/mTOR Inhibitor
Veratramine is a selective inhibitor of the PI3K/Akt/mTOR signaling pathway and serves as a modulator of SIGMAR1. This compound facilitates autophagic apoptosis in tumor cells, effectively induces G0/G1 cell cycle arrest, and diminishes epithelial-mesenchymal transition (EMT) markers, thereby reducing tumor migration. Additionally, Veratramine exhibits neuroprotective effects by inhibiting SIGMAR1 interactions with NMDAR and the phosphorylation of NMDAR Ser896, resulting in reduced neurological damage in neuropathy models. Its diverse biological activities make it suitable for research on liver cancer, osteosarcoma, and diabetic peripheral neuropathy. -
PI3Kα Inhibitor
BBO-10203 is a potent PI3Kα inhibitor that selectively and covalently binds to Cys242 in the RAS-Binding Domain. It inhibits both the GTP-bound and GDP-bound states of KRASG12C with an IC50 of 0.031 nM and an EC50 of 0.02 nM. By disrupting the interaction between RAS isoforms and PI3Kα, BBO-10203 effectively reduces pERK expression, suppresses cell growth, and induces G1 arrest and apoptosis. This compound is valuable for research into breast cancer, colorectal cancer, and non-small cell lung cancer. -
PI3K/Akt/CREB Activator
PI3K/Akt/CREB activator 1 is a potent, orally active compound that stimulates the PI3K/Akt/CREB signaling pathway. This activator promotes neuronal proliferation, induces differentiation of Neuro-2a cells into neuron-like cells, and facilitates the axon-dendrite polarization in primary hippocampal neurons by upregulating brain-derived neurotrophic factor. It is particularly relevant for research into vascular dementia (VaD). -
PI3K/AKT Inhibitor
PI3K/AKT-IN-1 is a potent dual inhibitor of the PI3K/AKT signaling pathway, exhibiting IC50 values of 6.99 μM for PI3Kγ, 4.01 μM for PI3Kδ, and 3.36 μM for AKT. This compound demonstrates significant anticancer activity by disrupting the PI3K/AKT axis, leading to the induction of caspase-3 dependent apoptosis. It serves as a valuable tool for research in cancer biology and therapeutic development targeting the PI3K/AKT pathway. -
PI3K/MDK Inhibitor
iMDK is a potent inhibitor of phosphoinositide 3-kinase (PI3K) and midkine (MDK), a growth factor associated with tumorigenesis. This compound has demonstrated the ability to effectively suppress non-small cell lung cancer (NSCLC) growth, particularly in combination with MEK inhibitors, while exhibiting minimal toxicity to normal cells and healthy mouse models. iMDK is a valuable tool for researchers studying cancer biology and potential therapeutic strategies targeting the PI3K/MDK signaling pathway. -
PI3Ka Inhibitor
Zovegalisib is an orally active allosteric inhibitor that selectively targets mutant forms of PI3Kα, exhibiting significant anti-tumor activity. This compound has demonstrated efficacy in inhibiting tumor growth in PIK3CA-mutant xenograft mouse models while exhibiting minimal effects on insulin levels. It is valuable for research into targeted cancer therapies and the exploration of PI3K signaling pathways. -
AKT PROTAC Degrader
MS21 is a potent AKT PROTAC degrader designed to selectively target and degrade AKT proteins. This compound effectively inhibits mutations within the PI3K/PTEN pathway, leading to suppressed tumor cell proliferation and induction of cell cycle arrest. MS21 demonstrates significant anti-tumor activity, making it a valuable tool for cancer research and therapeutic development. -
PROTAC AKT Degrader
MS170 is a highly selective PROTAC degrader targeting the AKT isoforms. With a DC50 value of 32 nM, MS170 effectively depletes total AKT (T-AKT) in cellular assays. It demonstrates strong binding affinity for AKT1, AKT2, and AKT3, with dissociation constants (Kd) of 1.3 nM, 77 nM, and 6.5 nM, respectively. This compound is suitable for research applications investigating AKT-related signaling pathways and therapeutic interventions in cancer biology. -
Endogenous Metabolite
Ergothioneine is an endogenous metabolite that acts as a potent antioxidant. It functions primarily as a specific inhibitor of p38 MAPK and Akt, which are critical signaling pathways involved in cellular stress responses. Ergothioneine is utilized in research focused on neuroprotection, cell apoptosis, and oxidative stress, making it a valuable compound for investigations into cellular resilience and health. -
Secondary Metabolite
Atranorin is a secondary metabolite derived from lichens that acts as an AKT inhibitor. This compound demonstrates a wide range of biological activities, including antibacterial, anti-inflammatory, antioxidant, anti-glycation, analgesic, and anti-tumor effects. Notably, Atranorin has IC50 values of 117 μM for scavenging DPPH free radicals and less than 10 μM for ABTS radicals, highlighting its potent antioxidant capacity. Additionally, Atranorin promotes wound healing and can be utilized in research focused on myelodysplastic syndromes, tumors, and various inflammatory conditions. -
CDK Inhibitor
Aloisine A is a potent cyclin-dependent kinase (CDK) inhibitor, exhibiting IC50 values of 0.15 μM for CDK1/cyclin B, 0.12 μM for CDK2/cyclin A, 0.4 μM for CDK2/cyclin E, and 0.16 μM for CDK5/p35. In addition to its CDK inhibitory effects, Aloisine A also inhibits GSK-3α and GSK-3β with IC50 values of 0.5 μM and 1.5 μM, respectively. Notably, it enhances the activity of wild-type and mutant CFTR with submicromolar affinity through a cAMP-independent mechanism, making it a valuable tool for research related to cystic fibrosis and CFTR-related disorders. -
CDK Inhibitor
NSC693868 is a selective inhibitor of cyclin-dependent kinases CDK1 and CDK5, demonstrating IC50 values of 600 nM and 400 nM, respectively. This compound also exhibits weaker inhibition of GSK3β with an IC50 of 1 µM and does not affect CDC25 activity. NSC693868 is employed in research to elucidate the functions of CDK1 and CDK5 within various cellular signaling pathways. -
GSK-3α/β Inhibitor
(E/Z)-BIO-acetoxime is a potent and selective inhibitor of GSK-3α/β, exhibiting an IC50 of 10 nM. This compound demonstrates exceptional selectivity with over 200-fold preference against CDK5/p25, CDK2/cyclin A, and CDK1/cyclin B, with IC50 values of 2.4, 4.3, and 63 μM, respectively. Its strong inhibitory activity makes it a valuable tool for research focused on signaling pathways involved in cell proliferation, differentiation, and apoptosis. -
Anti-Insect Agent
Methyl Eugenol is an anti-insect agent primarily effective against the oriental fruit fly (Bactrocera dorsalis). In addition to its insecticidal properties, Methyl Eugenol exhibits anti-cancer and anti-inflammatory activities, making it a versatile compound for biological research. It has been shown to induce autophagy in cells and can be utilized in studies related to intestinal ischemia/reperfusion injury. -
Iron Chelator
Deferoxamine (Deferoxamine B) is an iron chelator (binds to Fe(III) and many other metal cations), is widely used to reduce iron accumulation and deposition in tissues. Deferoxamine upregulates HIF-1α levels with good antioxidant activity. Deferoxamine also shows anti-proliferative activity, can induce apoptosis and autophagy in cancer cells. Deferoxamine can be used in studies of diabetes, neurodegenerative diseases as well as anti-cancer and anti-COVID-19. -
AMPK Agonist
10-Gingerol is an AMPK agonist derived from ginger oleoresin, exhibiting notable anti-inflammatory, antioxidant, and anti-proliferative properties. It effectively suppresses neointimal hyperplasia and inhibits the proliferation of vascular smooth muscle cells. Demonstrating significant radical scavenging activities, 10-Gingerol has IC50 values of 10.47 μM against DPPH, 1.68 μM against superoxide, and 1.35 μM against hydroxyl radicals. This compound also inhibits MDA-MB-231 tumor cell line proliferation with an IC50 of 12.1 μM, while targeting the PI3K/Akt signaling pathway to suppress proliferation, migration, invasion, and promote apoptosis. It holds potential for research applications in ulcerative colitis. -
PPAR Activator
Bilobetin acts as a PPARα activator, enhancing lipid metabolism and insulin sensitivity. It effectively reduces blood lipid levels by promoting hepatic lipid uptake and oxidation, while decreasing triglyceride secretion and accumulation in tissues. Additionally, Bilobetin stimulates the phosphorylation and nuclear translocation of PPARα, resulting in increased cAMP levels and PKA activity. This compound is significant for research in metabolic disorders, particularly those related to insulin resistance and lipid regulation. -
Glycosaminoglycan
Hyaluronic acid sodium, also known as sodium hyaluronate, is a glycosaminoglycan that plays a crucial role in the extracellular matrix (ECM). This biopolymer is involved in key biological activities such as cell proliferation, tissue remodeling, and angiogenesis, particularly in the context of digestive cancers. Hyaluronic acid sodium is implicated in tumor cell growth and migration, and it activates the PI3K-Akt signaling pathway. This reagent can also be utilized in research related to joint diseases, wound healing, and as a drug delivery system to enhance the efficacy of therapeutics in cancer research. -
MELK Inhibitor
HTH-01-091 is a selective inhibitor of maternal embryonic leucine zipper kinase (MELK), exhibiting an IC50 of 10.5 nM. In addition to its primary target, HTH-01-091 also demonstrates inhibitory activity against PIM1/2/3, RIPK2, DYRK3, smMLCK, and CLK2. This compound is valuable for research applications focused on breast cancer and elucidating the role of MELK in tumorigenesis. -
mTORC1 Inhibitor
RMC-4745 is a selective dual-site inhibitor of mTORC1 with a 35-fold higher affinity for mTORC1 compared to mTORC2. It effectively inhibits the proliferation of MCF-7 breast cancer cells and induces apoptosis by upregulating Caspase-3/7 activity. Notably, RMC-4745 does not lead to the upregulation of HER3 due to its selective inhibition of mTORC2. This compound is valuable for research focused on breast cancer and the mechanisms underlying mTOR signaling. -
Akt Allosteric Inhibitor
AKT-IN-28 is an allosteric inhibitor of Akt, a key protein involved in cell survival and metabolism. It exhibits a binding affinity with a Kd of 2.07 μM and demonstrates the ability to significantly inhibit Akt activity. This compound induces apoptosis, arrests the cell cycle in the G2/M phase, and suppresses proliferation, migration, and metabolic processes in KRAS mutant colorectal cancer cells, making it a valuable tool for cancer research applications focused on targeting the Akt pathway. -
MEK/PI3K Inhibitor
ST-168 is an orally bioavailable inhibitor of MEK and PI3K, exhibiting IC50 values of 182 nM for MEK1 and showing varying potency against PI3K isoforms with values of 69.2 nM, 41.7 nM, 1482 nM, and 2293 nM for PI3Kα, PI3Kδ, PI3Kβ, and PI3Kγ, respectively. It effectively inhibits ERK1/2 and AKT phosphorylation, inducing apoptosis in cancer cells within a 3D tumor sphere model. In vivo studies demonstrate its substantial antitumor efficacy in A375 melanoma mouse models. Additionally, ST-168 displays an improved ocular safety profile compared to conventional MEK inhibitors, evidenced by reduced caspase activation and apoptosis levels, making it a valuable tool for melanoma research. -
Akt1/Akt2 Inhibitor
Akt1/Akt2-IN-2 is an allosteric dual inhibitor targeting Akt1 and Akt2, exhibiting IC50 values of 138 nM and 212 nM, respectively. This compound enhances caspase-3 activity and effectively reduces the viability of various tumor cell lines. Its application in cancer research highlights its potential for investigating therapeutic strategies that disrupt Akt-mediated signaling pathways. -
ENO1 Inhibitor/AMPK Activator.
SU212 acts as an ENO1 inhibitor and AMPK activator, selectively inducing oxidative phosphorylation while reducing glycolysis and glucose uptake in tumor cells. This compound binds directly to ENO1, promoting apoptosis and ENO1 degradation through proteasomal and autophagic pathways, without affecting normal cells. Additionally, SU212 leads to mitotic arrest and apoptosis in triple-negative breast cancer (TNBC) cells, showcasing significant anti-tumor activity in vitro. It inhibits tumor growth and metastasis in various in vivo models, including syngeneic, xenograft, and diabetic mice, and has demonstrated an excellent safety profile, making it a valuable tool for research in TNBC, diabetes, and fatty liver disease. -
Akt Inhibitor
2-Chlorophenoxazine is an Akt inhibitor with an IC50 value of 2-5 μM in vitro. This compound has been shown to induce apoptosis in various cancer cell lines. It is a valuable tool for research into cancerpathways and therapeutic strategies targeting Akt signaling. -
CIP2A and p-Akt Inhibitor
PP2A Cancerous-IN-1 is a strong and potent CIP2A (Cancerous inhibitor of PP2A) and p-Akt inhibitor. PP2A Cancerous-IN-1 shows the most potent antiproliferative activities. PP2A Cancerous-IN-1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. -
AKT Inhibitor
AKT-IN-14 free base is a highly potent inhibitor of the AKT family of serine/threonine kinases, demonstrating IC50 values of less than 0.01 nM, 1.06 nM, and 0.66 nM for AKT1, AKT2, and AKT3, respectively. This compound is valuable for research applications focused on cancer biology, particularly in studies investigating the role of AKT signaling in tumor progression and therapeutic resistance. -
Akt Substrate
AKTide-2T is a selective substrate for AKT, demonstrating competitive inhibition of histone H2B phosphorylation with a Ki of 12 nM. This peptide mimics the optimal phosphorylation sequence of Akt, effectively serving as an inhibitory agent due to the absence of Thr at the S22 position in the wildtype sequence. It is a valuable tool for studying AKT signaling pathways and their implications in various biological processes. -
PI4KIIIβ Inhibitor
PI4KIII beta inhibitor 4 is a highly selective inhibitor of PI4KIIIβ, exhibiting an IC50 of 0.005 μM. This compound effectively induces apoptosis in tumor cells, mediates cell cycle arrest, and promotes autophagy through inhibition of the PI3K/AKT signaling pathway. Its key biological activities make it a valuable tool for cancer research and therapeutic investigations. -
mTOR Inhibitor
Ovalitenone is a flavonoid compound known to inhibit the mTOR signaling pathway. This compound demonstrates significant anti-cancer activity, as it effectively reduces anchorage-independent growth and suppresses the migration and invasion of cancer cells without inducing cytotoxicity in lung cancer cell lines H460 and A549. Ovalitenone modulates epithelial-mesenchymal transition (EMT) by decreasing N-cadherin, snail, and slug levels while promoting E-cadherin expression. Additionally, it inhibits signaling pathways associated with focal adhesion kinase (FAK), ATP-dependent tyrosine kinase (AKT), and cell division cycle 42 (Cdc42), making it a valuable reagent for cancer research applications. -
Akt Inhibitor
DETD-35 is a potent inhibitor of the Akt signaling pathway, with additional effects on MEK-ERK and STAT3 pathways. It induces apoptosis in cancer cells and decreases their resistance to Vemurafenib. DETD-35 demonstrates effective inhibitory activity against various melanoma cell lines, with IC50 values of 2.5 to 6.0 μM across wild-type and mutant strains. This compound is a valuable tool for investigating mechanisms of anti-melanoma therapies. -
PI3K/AKT Pathways Inhibitor
Isocucurbitacin B selectively inhibits the PI3K/AKT signaling pathways, along with the MAPK and STAT3 pathways, demonstrating notable anti-cancer properties. This natural terpenoid, derived from Pedicellus melo, effectively suppresses cancer cell proliferation, migration, and invasion. Additionally, Isocucurbitacin B induces apoptosis and facilitates G2/M phase cell cycle arrest, while altering intracellular cholesterol and pH levels, and elevating intracellular calcium levels. It serves as a valuable reagent for research applications in cancer biology, particularly in the study of glioma. -
Akt Inhibitor
AM-9635 is a selective Akt inhibitor that targets the PI3Kδ pathway. It demonstrates significant in vitro and in vivo efficacy, effectively inhibiting PI3Kδ-dependent B cell receptor-mediated AKT phosphorylation. This compound has been shown to suppress the production of specific IgG and IgM antibodies in a rat model immunized with Aplysia leocyanin (KLH), making it useful for research applications in immunology and cancer biology. -
Akt Inhibitor
CCT129254 is a selective inhibitor of the Akt pathway, targeting the serine/threonine kinase Akt. This compound demonstrates significant reduction in melanoma cell motility in vivo, highlighting its potential utility in cancer research. CCT129254 may serve as a valuable tool for studying the role of Akt in tumor progression and therapeutic resistance. -
TrkA/Akt Inhibitor
HS-345 is a selective inhibitor of the TrkA/Akt signaling pathway, demonstrating significant anti-cancer effects in pancreatic cancer models. It inhibits the growth and proliferation of pancreatic cancer cells while inducing apoptosis. Moreover, HS-345 disrupts angiogenesis by downregulating the expression of HIF-1α and VEGF. This compound shows potential as a valuable tool for research into pancreatic cancer therapies. -
PI3K Inhibitor
PI3K-IN-7 is a selective inhibitor of phosphoinositide 3-kinase (PI3K) that effectively inhibits the phosphorylation of AKT, thereby disrupting downstream signaling pathways essential for cell survival. This compound promotes apoptosis in tumor cells while exhibiting low toxicity towards normal cells. PI3K-IN-7 is suitable for research applications focused on acute and chronic leukemia, multiple myeloma, and lymphoma. -
Akt Inhibitor
Uprosertib hydrochloride is a potent and selective pan-Akt inhibitor, characterized by IC50 values of 180 nM for Akt1, 328 nM for Akt2, and 38 nM for Akt3. This compound effectively modulates Akt signaling pathways, which are crucial in regulating cell growth, proliferation, and survival. Uprosertib hydrochloride is widely utilized in cancer research and therapeutic studies to explore potential treatments targeting the Akt pathway. -
PI3Kα/c-Met Inhibitor
DFX117 is a selective, orally active inhibitor targeting PI3Kα and c-Met tyrosine kinase. This compound effectively inhibits the PI3K/Akt/mTOR pathway, demonstrating significant antiproliferative activity against cancer cell lines such as NCI-H1975, NCI-H1993, and HCC827, with IC50 values ranging from 0.02 to 0.08 µM. DFX117 induces cell cycle arrest at the G0/G1 phase and promotes apoptosis in A549 and NCI-H1975 cells. Additionally, DFX117 exhibits notable antitumor efficacy in murine models, making it a valuable tool for cancer research.

