pi3k-in-6

PI3K-IN-6 is an oral active and highly selective inhibitor of phosphoinositide 3-kinase (PI3K) β/δ(IC50 values of 7.8 nM/5.3 nM , respectively).

PI3K-IN-60 (Compound 34) is a selective PI3Kγ inhibitor for studying autoimmune diseases and cancers such as multiple sclerosis, breast cancer, and pancreatic ductal adenocarcinoma.

4-Vinylcyclohexene Dioxide (VCD) is an industrial epoxy resin intermediate and metabolite that exhibits a highly selective destructive effect on oocytes in primordial and primary follicles; it is used as a key inducer for establishing animal models of premature ovarian failure and premenopause. 4-Vinylcyclohexene Dioxide exerts its ovarian toxicity by activating caspase-dependent apoptotic pathways and can induce apoptosis in ovarian granulosa cells by upregulating reactive oxygen species and activating the PI3K/Akt/mTOR signaling pathway. It is used in reproductive toxicology and endocrine regulation research.

Luteolin-7-rutinoside is a natural product that alleviates LPS-induced acute liver injury by inhibiting the PI3K/AKT/AMPK/NF-κB signaling pathways and suppressing TNF-α, IL-6, and IL-1β.

Rhodiolin, a natural product from Rhodiola rosea, blocks glycolysis of glucose 6-phosphate isomerase (GPI) in human papillary thyroid cancer (PTC), inhibits phosphorylation of the PI3K/AKT/mTOR signaling pathway and induces apoptosis of PTC cells.

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), exhibiting anti-tumor activity in a mouse glioblastoma xenograft model[1]. AMG 511 significantly suppresses PI3K signaling as indicated by a decrease in p-Akt (Ser473).

Dehydroxy-oridonin-vinyl ester (Compound 6k) is an anticancer agent. It exhibits exceptionally potent antiproliferative activity against SU-DHL-6 cells, with an IC₅₀ value of 0.12 μM. Dehydroxy-oridonin-vinyl ester induces apoptosis by inhibiting the activation of the PI3K/Akt signaling pathway, without affecting cell cycle progression. Dehydroxy-oridonin-vinyl is applicable in lymphoma research.

PI3K/Akt/mTOR-IN-6 (Compound JW4) is an orally active inhibitor of the PI3K/Akt/mTOR pathway. It induces apoptosis through the mitochondrial pathway and demonstrates significant anti-non-small cell lung cancer activity.

TBK1/IKKε-IN-4, a 6-aminopyrazolopyrimidine derivative, serves as a potent, selective inhibitor for TBK1 and IKKε, demonstrating IC50 values of 13 nM and 59 nM, respectively. This compound exhibits significantly reduced activity, by 100- to 1000-fold, against other protein kinases, such as PDK1, PI3K family members, and mTOR[1].

PI3K-IN-26 is an effective PI3K inhibitor. PI3K-IN-26 inhibits the proliferation of SU-DHL-6 cells, IC50= 36 nM.

HDAC-IN-43 is a potent HDAC 1/3/6 inhibitor with IC50 values of 82 nM for HDAC 1, 45 nM for HDAC 3, and 24 nM for HDAC 6, and a weak PI3K/mTOR inhibitor with IC50 values of 3.6 μM for PI3K and 3.7 μM for mTOR, exhibiting a broad-spectrum anti-proliferative effect.

PI3K-IN-37 (Example 84.1) is an inhibitor of PI3K α (IC50: 6 nM), PI3K β (IC50: 8 nM), and PI3K δ (IC50: 4 nM), and also inhibits mTOR with an IC50 of 4 nM.

PI3K/mTOR Inhibitor-6 (Compound 19c) is a potent dual PI3K/mTOR inhibitor, exhibiting greater stability than gedatolisib in artificial gastric fluid. At 10 μM, PI3K/mTOR Inhibitor-6 significantly inhibits the PI3K/Akt/mTOR signaling pathway and has shown potential for cancer research.

1. Oroxylin A (Baicalein 6-methyl ether) 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 could providing a therapeutic strategy for RAS. 3. Oroxylin A inhibits UCP2s triggers the MPTP opening, and promotes the apoptosis in CaCo-2 cells; uncoupling protein 2 plays a key role in mitochondrial apoptotic pathway. 4. Oroxylin A inhibits N1ICD translocating to the nucleus and binding to epithelial-mesenchymal transition-related transcription factor Snail, thus suppressing the invasion and migration of MCF-7 cells. 5. Oroxylin A improves the sensitivity of K562/ADM cells by increasing apoptosis in leukemic cells and decreasing the expression of CXCR4 and PI3K/Akt/NF-κB pathway, and probably served as a most promising agent for CML treatment.

1. 6-Shogaol (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 monoarthritic model of the knee joint of rats. 3. 6-Shogaol inhibits the growth of human cancer cells and induces apoptosis in COLO 25 cells through modulation of mitochondrial functions regulated by reactive oxygen species (ROS). 4. 6-Shogaol effectively inhibit invasion and metastasis of hepatocellular carcinoma through diverse molecular mechanisms, including inhibition of the MAPK and PI3k/Akt pathways and NF-κB and STAT3 activities to suppress expression of MMP-2/-9 and uPA and block angiogenesis, could further regulate urokinase-type plasminogen activity.

6-O-Isobutyrylbritannilactone is a natural sesquiterpene and melanogenesis inhibitor capable of suppressing IBMX-induced melanogenesis in B16F10 cells. It modulates ERK, CREB, and PI3K/AKT pathways while reducing pigmentation in zebrafish embryos.

PI3Kδ-IN-17 (Compound S5) is a potent PI3K δ inhibitor with an IC50 value of 2.82 nM, significantly inhibiting SU-DHL-6 cell proliferation with an IC50 of 0.035 μM [1].

Anticancer agent 109 (compound 6-15) acts as an inhibitor targeting the Gas6-Axl axis, demonstrating significant anti-cancer properties. This compound suppresses the expression of Gas6, Axl, p-PI3K, and p-AKT in cancer cells, thereby inducing G1 phase arrest and promoting apoptosis of cancer cells. Additionally, Anticancer agent 109 effectively inhibits tumor growth in nude mouse tumor-bearing models [1].

Compound 19, also known as Antidiabetic agent 6, is an antidiabetic compound. It stimulates the translocation of GLUT4 by activating the PI3K/AKT-dependent signaling pathway. Furthermore, this compound reduces blood glucose levels in diabetic rats induced by streptozotocin.

Citronellol-d3 ((±)-Citronelloll-d3) is the deuterium-labeled form of Citronellol. Citronellol ((±)-Citronellol) acts as an orally effective apoptosis inducer. It can prevent oxidative stress, mitochondrial dysfunction, and apoptosis in the Parkinson's disease model of SH-SY5Y cells induced by 6-OHDA through the regulation of ROS-NO, MAPK/ERK, and PI3K/Akt signaling pathways. Additionally, Citronellol induces necroptosis in human lung cancer cells via the TNF-α pathway and reactive oxygen species (ROS) accumulation. It modulates the autophagy pathway by reducing LC-3 and p62 levels, inhibiting oxidative stress and neuroinflammation, thus offering neuroprotective effects in rat models of Parkinson's disease. Furthermore, Citronellol exhibits antifungal activity against Trichophyton rubrum by inhibiting ergosterol synthesis.

Shogaol (Standard) is a reference standard for research and analysis in studies involving Shogaol. 1. 6-Shogaol (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 monoarthritic model of the knee joint of rats. 3. 6-Shogaol inhibits the growth of human cancer cells and induces apoptosis in COLO 25 cells through modulation of mitochondrial functions regulated by reactive oxygen species (ROS). 4. 6-Shogaol effectively inhibit invasion and metastasis of hepatocellular carcinoma through diverse molecular mechanisms, including inhibition of the MAPK and PI3k/Akt pathways and NF-κB and STAT3 activities to suppress expression of MMP-2/-9 and uPA and block angiogenesis, could further regulate urokinase-type plasminogen activity.

Pectolinarin (Standard) is a reference standard for research and analysis in studies involving Pectolinarin. Pectolinarin is a Cirsium isolate with anti-inflammatory activity.

Oroxylin A (Standard) is a reference standard for research and analysis in studies involving Oroxylin A. 1. Oroxylin A (Baicalein 6-methyl ether) 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 could providing a therapeutic strategy for RAS. 3. Oroxylin A inhibits UCP2s triggers the MPTP opening, and promotes the apoptosis in CaCo-2 cells; uncoupling protein 2 plays a key role in mitochondrial apoptotic pathway. 4. Oroxylin A inhibits N1ICD translocating to the nucleus and binding to epithelial-mesenchymal transition-related transcription factor Snail, thus suppressing the invasion and migration of MCF-7 cells. 5. Oroxylin A improves the sensitivity of K562/ADM cells by increasing apoptosis in leukemic cells and decreasing the expression of CXCR4 and PI3K/Akt/NF-κB pathway, and probably served as a most promising agent for CML treatment.

Oldenlandoside I ((E)-6-O-p-coumaroyl scandoside methyl ester) is a natural product isolated from Hedyotis diffusa exhibiting potential antiproliferative activity. It induces apoptosis in SKM-1 cells in combination with p-coumaric acid, associated with caspase activation and inhibition of PI3K/Akt pathway proteins.