Catalog No.
Product Name
Application
Product Information
Citations
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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. -
PI3K/mTOR Inhibitor
FD274 is a potent dual inhibitor of PI3K and mTOR, exhibiting IC50 values of 0.65 nM for PI3Kα, 1.57 nM for PI3Kβ, 0.65 nM for PI3Kγ, 0.42 nM for PI3Kδ, and 2.03 nM for mTOR. This compound demonstrates significant anti-proliferative effects on acute myeloid leukemia (AML) cell lines, specifically HL-60 and MOLM-16, inducing G1 phase cell cycle arrest and promoting apoptosis. In vivo studies reveal dose-dependent inhibition of tumor growth in HL-60 xenograft models, making FD274 a valuable tool for research into acute myeloid leukemia therapies. -
PARP/PI3K Inhibitor
PARP/PI3K-IN-1 is a potent inhibitor of both PARP and PI3K, exhibiting pIC50 values of 8.22 for PARP-1, 8.44 for PARP-2, and varying activity against PI3K isoforms with values of 8.25 for PI3Kα, 6.54 for PI3Kβ, 8.13 for PI3Kδ, and 6.08 for PI3Kγ. This compound demonstrates significant anticancer activity and is suitable for research applications targeting a variety of oncological disorders. Its dual inhibition may provide insights into therapeutic strategies for cancer treatment. -
PI3Kδ Inhibitor
PI3Kδ-IN-16 is a highly selective inhibitor of the PI3Kδ isoform, displaying an impressive IC50 value of 0.9 nM. This compound exhibits significant anti-proliferative effects on SU-DHL-6 cells, leading to cell cycle arrest and the induction of apoptosis. PI3Kδ-IN-16 demonstrates substantial selectivity for PI3Kδ over other isoforms, with a kinase activity that is approximately 378-fold greater than PI3Kα, 412-fold greater than PI3Kβ, and 10-fold greater than PI3Kγ. It is a valuable tool for research into hematologic malignancies and the therapeutic targeting of PI3Kδ. -
NF-κB Inhibitor/Nrf2/AMPK Activator
Panduratin A is a potent inhibitor of the NF-κB signaling pathway, recognized for its significant anti-inflammatory and antioxidant properties. It demonstrates protective effects against nephrotoxicity induced by Colistin, primarily by mitigating oxidative stress and enhancing mitochondrial function. Additionally, Panduratin A activates autophagy through an AMPK-dependent mechanism and exhibits potential anti-tuberculosis and antiviral activities by inhibiting the methyltransferase of SARS-CoV-2. These diverse biological activities make Panduratin A a valuable tool in various areas of research, including inflammation, cellular stress responses, and infectious diseases. -
PI3Kα/mTOR Inhibitor
PWT-33597 free base is a dual inhibitor targeting PI3Kα and mTOR, effectively disrupting downstream signaling pathways associated with cell growth and metabolism. This compound induces apoptosis in tumor cells and demonstrates significant inhibitory effects on tumor proliferation. PWT-33597 free base is applicable in research focused on various tumors, including renal cell carcinoma, making it a valuable tool for cancer studies. -
HSP90/mTOR Inhibitor
HSP90/mTOR-IN-1 is a potent inhibitor targeting both Hsp90 and mTOR, exhibiting IC50 values of 69 nM and 29 nM, respectively. This compound effectively suppresses the proliferation of SW780 cells by over-activating the PI3K/AKT/mTOR signaling pathway. In addition to inducing apoptosis and autophagy through selective inhibition, HSP90/mTOR-IN-1 demonstrates significant in vivo anti-tumor activity. It serves as a valuable reagent for research applications focused on bladder cancer. -
PI3Kα/mTOR Inhibitor
PWT-33597 is a potent dual inhibitor of PI3Kα and mTOR, effectively disrupting downstream signaling pathways associated with cell growth and survival. This reagent induces apoptosis in tumor cells and demonstrates significant anti-tumor activity. PWT-33597 is a valuable tool for research into various malignancies, including renal cell carcinoma, providing insights into tumor biology and therapeutic strategies. -
PI3Kα Inhibitor
PI3Kα-IN-6 is a selective inhibitor of the phosphoinositide 3-kinase alpha (PI3Kα) pathway. This compound demonstrates significant anticancer activity by promoting the generation of reactive oxygen species (ROS), leading to a decrease in mitochondrial membrane potential (MMP) and subsequently inducing apoptosis in cancer cells. PI3Kα-IN-6 is valuable for research focused on cancer therapeutics and the exploration of PI3K signaling in cell survival and proliferation. -
mTOR Inhibitor
MT-44 is a potent and selective inhibitor of the mechanistic target of rapamycin (mTOR), exhibiting an IC50 of 49.4 nM. It effectively inhibits cancer cell proliferation, migration, and invasion, while inducing apoptosis and increasing reactive oxygen species (ROS) production. MT-44 also causes G2/M phase cell cycle arrest and activates the cGAS/STING signaling pathway. This compound is valuable for cancer research, particularly in the study of triple-negative breast cancer. -
PI3K Inhibitor
Copanlisib dihydrochloride is a potent, selective pan-class I PI3K inhibitor that acts through ATP-competitive mechanisms. It exhibits remarkable inhibitory activity with IC50 values of 0.5 nM, 0.7 nM, 3.7 nM, and 6.4 nM for PI3Kα, PI3Kδ, PI3Kβ, and PI3Kγ, respectively, demonstrating over 2,000-fold selectivity against other lipid and protein kinases, except for mTOR. This compound has been shown to possess significant antitumor activity, making it a valuable reagent for cancer research and therapeutic development focusing on the PI3K pathway. -
PI4KIIα Inhibitor
PI-273 is a selective inhibitor of phosphatidylinositol 4-kinase II alpha (PI4KIIα), with an IC50 value of 0.47 μM. This compound demonstrates efficacy in inhibiting breast cancer cell proliferation, disrupting the cell cycle, and inducing apoptosis. PI-273 serves as a valuable tool for investigating the role of PI4KIIα in cancer biology and developing targeted therapeutic strategies. -
MARK/SIK/AMPK Inhibitor
MRT199665 is a potent, ATP-competitive inhibitor targeting MARK, SIK, and AMPK pathways, exhibiting IC50 values of 2 nM for MARK1, 10 nM for AMPKα1, and 110 nM for SIK1. This compound induces apoptosis in MEF2C-activated human acute myeloid leukemia (AML) cells by effectively inhibiting the phosphorylation of the SIK substrate CRTC3 at S370. MRT199665 serves as a valuable tool for investigating the roles of MARK, SIK, and AMPK in cellular signaling and cancer biology. - Lipoteichoic acid is an orally active compound with anti-inflammatory and antitumor properties. It is a key immune molecule found in Gram-positive bacteria that activates the complement system by upregulating C3 and inhibiting CD55. Lipoteichoic acid modulates macrophage autophagy via the PI3K/Akt/mTOR pathway, induces lung injury in mouse models, and inhibits melanin production.
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DK/PI3K/BRD4 Inhibitor
SRX3177 is a potent triple inhibitor targeting CDK4/6, PI3K, and BRD4, with IC50 values of <2.5 nM for CDK4, 3.3 nM for CDK6, 79 nM for PI3Kα, 83 nM for PI3Kδ, 3.18 μM for PI3Kγ, and 33 nM and 89 nM for BRD4 BD1 and BD2, respectively. It exhibits broad cytotoxic activity against cancer cells while sparing normal epithelial cells, highlighting its potential as a targeted cancer therapeutic with reduced toxicity. - 6-Demethoxytangeretin is a flavonoid compound isolated from *Citrus reticulata* with demonstrated anti-inflammatory and anti-allergic properties. It inhibits IL-6 production and the expression of related genes in human mast cells by modulating the ALK and MAPK signaling pathways. Additionally, 6-Demethoxytangeretin enhances CRE-mediated transcription in hippocampal neurons, indicating potential neuroregulatory effects.
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fMLP inhibitor
Larixol is an fMLP inhibitor that also suppresses key signaling pathways involved in immune regulation, including Src kinase, ERK1/2, p38, and AKT phosphorylation. It disrupts the interaction between the βγ subunit of the fMLP receptor Gi protein and downstream effectors, thereby inhibiting fMLP-induced respiratory burst. Larixol effectively inhibits fMLP (0.1 μM)-induced superoxide anion production (IC50: 1.98 μM), cathepsin G release (IC50: 2.76 μM), and neutrophil chemotaxis. It mitigates neutrophil hyperactivation and helps reduce inflammation and tissue damage. Additionally, Larixol derivatives have shown inhibitory activity against TRPC6 functional mutants associated with focal segmental glomerulosclerosis (FSGS). - Hirsutenone is a bioactive diarylheptanoid derived from *Alnus* species, known for its anti-inflammatory, anti-tumor-promoting, and anti-atopic dermatitis properties. It attenuates adipogenesis by directly binding to PI3K and ERK1 in a non-ATP competitive manner. Hirsutenone is a valuable compound for research related to obesity and metabolic disorders.
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PI3K/Akt/mTOR inhibitor
PI3K/Akt/mTOR-IN-2 is an inhibitor of the PI3K/AKT/mTOR signaling pathway with demonstrated anticancer activity. It selectively inhibits the proliferation of MDA-MB-231 cells with an IC50 of 2.29 μM and induces cell cycle arrest and apoptosis, making it a promising candidate for cancer research. -
PGAM1 inhibitor
HKB99 is an allosteric inhibitor of phosphoglycerate mutase 1 (PGAM1) that induces apoptosis and suppresses cell migration by inhibiting the formation of invasive pseudopodia. It increases oxidative stress, activates the JNK/c-Jun pathway, and downregulates AKT and ERK signaling. HKB99 is a promising compound for the study of non-small cell lung cancer (NSCLC). -
ALK/ROS1 inhibitor
Iruplinalkib (WX-0593) is an orally active and selective ALK/ROS1 inhibitor that effectively blocks tyrosine autophosphorylation of ALK, mutant ALK, and EGFR, with IC50 values ranging from 5.38 to 16.74 nM. Additionally, it inhibits the transport activity of MATE1, MATE2K, P-gp, and BCRP. Iruplinalkib is under investigation for the treatment of non-small cell lung cancer (NSCLC). -
Endoplasmic Reticulum Stress Inhibitor
Tauroursodeoxycholate (Tauroursodeoxycholic acid; TDUCA) dihydrate is an inhibitor of endoplasmic reticulum (ER) stress that significantly downregulates pro-apoptotic molecules, including caspase-3 and caspase-12. Additionally, it suppresses ERK signaling, contributing to its cytoprotective and anti-apoptotic effects. -
TrkA agonist
Gambogic amide is a potent and selective TrkA agonist that induces tyrosine phosphorylation of TrkA and activates downstream signaling pathways, including Akt and MAPK. It specifically binds to the cytoplasmic juxtamembrane domain of TrkA, promoting receptor dimerization and activation. Gambogic amide exhibits neuroprotective effects by preventing glutamate-induced neuronal cell death and demonstrates improved efficacy in a transient middle cerebral artery occlusion (MCAO) model of stroke, supporting its potential use in research on neurodegenerative diseases and stroke. -
mGluR5 allosteric modulator
CDPPB is a selective, orally active allosteric modulator of the metabotropic glutamate receptor 5 (mGluR5). It enhances AKT and ERK1/2 signaling and upregulates BDNF mRNA expression. CDPPB also inhibits caspase-3 activation and mitigates mitochondrial dysfunction, demonstrating therapeutic potential in improving cognitive impairment, depression, and Huntington’s disease. -
EGFR/PI3K Inhibitor
MTX-531 is an orally active small molecule that inhibits EGFR (IC50 = 14.7 nM) and multiple PI3K isoforms, with IC50 values of 6.4 nM (PI3Kα), 233 nM (PI3Kβ), 8.3 nM (PI3Kγ), and 1.1 nM (PI3Kδ), demonstrating potent antitumor activity. Additionally, MTX-531 functions as a weak PPARγ agonist (IC50 = 2.5 µM), which may mitigate PI3K inhibitor-induced hyperglycemia. -
Hsp90/HSV inhibitor
AT-533 is a potent inhibitor of heat shock protein 90 (Hsp90) and herpes simplex virus (HSV), exhibiting strong antitumor and antiviral activities. It suppresses tumor growth and angiogenesis by disrupting the HIF-1α/VEGF/VEGFR-2 signaling axis, a critical pathway in tumor vascularization and progression. Additionally, AT-533 inhibits key downstream signaling cascades, including Akt/mTOR/p70S6K, ERK1/2, and FAK pathways. In endothelial cells, specifically human umbilical vein endothelial cells (HUVECs), AT-533 effectively inhibits tube formation, cell migration, and invasion, highlighting its anti-angiogenic properties. These combined effects position AT-533 as a promising candidate for cancer therapy and angiogenesis-related disease research. -
Anticholinergic agent
Penehyclidine hydrochloride (also known as Penequinine hydrochloride) is a selective anticholinergic agent that acts as an antagonist of muscarinic M1 and M3 receptors. It exerts anti-inflammatory effects by modulating immune signaling in lung tissue, notably through activation of the NF-κB pathway and inhibition of pro-inflammatory cytokine release. In preclinical studies, Penehyclidine hydrochloride has been shown to alleviate pulmonary inflammation in rat models of chronic obstructive pulmonary disease (COPD), particularly under conditions of mechanical ventilation. These properties suggest its potential utility in managing respiratory inflammatory conditions and improving outcomes in mechanically ventilated patients with COPD. - Deltonin is a steroidal saponin isolated from *Dioscorea zingiberensis*, exhibiting notable antitumor activity. It exerts its effects by inhibiting the activation of key survival and proliferation pathways, specifically ERK1/2 and AKT signaling. Through this dual inhibition, Deltonin suppresses tumor cell growth and promotes apoptosis, making it a promising candidate for further investigation in cancer research and therapeutic development.
- 6-Hydroxyflavone is an orally active flavonoid with diverse pharmacological properties. It exhibits anti-inflammatory activity by inhibiting lipopolysaccharide (LPS)-induced nitric oxide (NO) production and also promotes osteoblast differentiation through activation of the AKT, ERK1/2, and JNK signaling pathways, supporting its role in bone health. Additionally, 6-Hydroxyflavone inhibits the glycosylation of bovine hemoglobin (BHb), suggesting potential in managing glycation-related complications. It demonstrates kidney-protective effects and modulates GABAergic neurotransmission by enhancing GABA-induced currents via the benzodiazepine binding sites on GABAA receptors
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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. -
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.
