PI3K Inhibitor

PI3K-IN-7 (Compound C96) is a PI3K inhibitor. PI3K-IN-7 inhibits phosphorylation of AKT and the activation of an AKT downstream protein. PI3K-IN-7 induces apoptosis of the tumor cells. PI3K-IN-7 has low toxicity for normal cells. PI3K-IN-7 can be used for research of acute and chronic leukemia, multiple myeloma, lymphoma.

GNE-477 (Standard) is the analytical standard of GNE-477 (HY-11042). This product is intended for research and analytical applications. GNE-477 is a potent and efficacious dual PI3K (IC₅₀=4 nM)/mTOR(K_i=21 nM) inhibitor.

Iridin (Standard) is the analytical standard of Iridin. This product is intended for research and analytical applications. Iridin is an orally active natural isoflavone. Iridin inhibits the PI3K/AKT and PKM2 signaling pathways, and downregulates the JAK/STAT and NF-κB pathways. Iridin induces Fas-mediated extrinsic apoptosis, G2/M cell cycle arrest, and inhibits cell proliferation. Iridin reduces inflammation, inhibits ROS production, suppresses glycolysis, and also exhibits antioxidant and antidiabetic activities. Iridin can be used in research related to gastric cancer and acute lung injury.

Tianeptine sodium salt (Standard) is the analytical standard of Tianeptine sodium salt (HY-90003A). This product is intended for research and analytical applications. Tianeptine sodium salt is an atypical antidepressant. Tianeptine sodium salt is a moderate-intensity agonist of the μ-opioid receptor (MOR), and to a lesser extent, is an agonist of the δ-opioid receptor (DOR). Tianeptine sodium salt is a glutamate modulator that can enhance AMPA receptor and antagonize NMDA receptor. Tianeptine sodium salt increases sensitivity of the α1 adrenergic receptor, which only manifests in chronic treatment. Tianeptine sodium salt exerts neuroprotective effects under stress/inflammation-induced conditions, exhibiting anti-inflammatory and antioxidant properties. Tianeptine sodium salt inhibits MMP-9 by suppressing the PI3K/Akt-mediated NF-κB pathway. Tianeptine sodium salt can be used to alleviate symptoms of depression and anxiety, but does not cause sedative effects.

GSK2636771 (Standard) is the analytical standard of GSK2636771. This product is intended for research and analytical applications. GSK2636771 is a potent, selective and orally bioavailable inhibitor of PI3Kβ with a Ki of 0.89 nM and an IC50 of 5.2 nM, showing 900-fold selectivity over p110α and p110γ, and 10-fold selectivity over p110δ isoforms.

GNE-493 (Standard) is the analytical standard of GNE-493 (HY-10811). This product is intended for research and analytical applications. GNE-493 is a potent, selective, and orally available dual pan-PI3-K_inase/mTOR inhibitor with IC₅₀s of 3.4 nM, 12 nM, 16 nM, 16 nM and 32 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ and mTOR.

PK_i-402 (Standard) is the analytical standard of PK_i-402 (HY-10683). This product is intended for research and analytical applications. PK_i-402 is a selective, reversible, ATP-competitive inhibitor of PI3K, including PI3K-α mutants, and mTOR (IC₅₀=2, 3, 7,14 and 16 nM for PI3Kα, mTOR, PI3Kβ, PI3Kδ and PI3Kγ).

Eganelisib (Standard) is the analytical standard of Eganelisib (HY-100716). This product is intended for research and analytical applications. Eganelisib (IPI549) is a potent and selective PI3Kγ inhibitor with an IC50 of 16 nM. Eganelisib shows >100-fold selectivity over other lipid and protein kinases.

AS-605240 (Standard) is the analytical standard of AS-605240 (HY-10109). This product is intended for research and analytical applications. AS-605240 is a specific and orally active inhibitor of the PI3Kγ, with an IC50 of 8 nM, and a Ki of 7.8 nM.

Autophinib (Standard) is the analytical standard of Autophinib (HY-101920). This product is intended for research and analytical applications. Autophinib is a potent, selective autophagy inhibitor with IC₅₀s of 90 nM and 40 nM for starvation- and Rapamycin-induced autophagy, respectively. Autophinib is also an ATP competitive Vacuolar Protein Sorting 34 (VPS34) inhibitor with an IC₅₀ of 19 nM. Autophinib inhibits autophagy induced by starvation or Rapamycin by targeting VPS34.

Alisol B acetate is a Triterpenoids product that can be isolated from the tubers of Alisma plantago-aquatica Linn..

WJD008 is a potent dual phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitor with antiproliferative and anticlonogenic activity in tumor cells and transformed cells with PIK3CA mutant. WJD008 inhibits kinase activity of PI3K α and mTOR and abrogates insulin-like growth factor-I-activated PI3K-Akt-mTOR signaling cascade. WJD008 is promising for research of cancers.

PQR530 (Standard) is the analytical standard of PQR530 (HY-107365). This product is intended for research and analytical applications. PQR530 is a potent, ATP-competitive, orally bioavailable and brain-penetrant dual pan-PI3K/mTORC1/2 inhibitor, with a subnanomolar K_d toward PI3Kα and mTOR (0.84 and 0.33 nM, respectively). Antitumor activity.

BrAC-GGFG-Aminal-PI3K/mTOR-IN-21 is a conjugate of PI3K/mTOR-IN-21 (HY-185456) and Linker.

Daphnoretin (Dephnoretin; Thymelol) (Standard) is the analytical standard of Daphnoretin (HY-N0699). This product is used for research and analytical applications. Daphnoretin is a protein kinase C (PKC) activator that can inhibit the expression of hepatitis B virus (HBV) surface antigen (HBsAg) and has antiviral activity. Daphnoretin exerts its anti-tumor effect by inhibiting the activation of the PI3K/AKT signaling pathway, triggering the mitochondrial apoptosis pathway. Daphnoretin alleviates chondrocyte apoptosis and inflammatory responses by inhibiting endoplasmic reticulum stress and the activation of the NLRP3 inflammasome. Daphnoretin can regulate the differentiation and maturation of dendritic cells, by down-regulating the phosphorylation level of JNK, inhibiting its immune stimulating function, thereby playing a protective role in skin transplant rejection reactions.

LX2343 (Standard) is the analytical standard of LX2343 (HY-111383). This product is intended for research and analytical applications. LX2343 is a BACE1 enzyme inhibitor with an IC₅₀ value of 11.43±0.36 μM. LX2343 acts as a non-ATP competitive PI3K inhibitor with an IC₅₀ of 15.99±3.23 μM. LX2343 stimulates autophagy in its promotion of Aβ clearance.

Pictilisib (dimethanesulfonate) (Standard) is the analytical standard of Pictilisib (dimethanesulfonate). This product is intended for research and analytical applications. Pictilisib dimethanesulfonate (GDC-0941 dimethanesulfonate) is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold).

(R)-GSK-F1 is the R-type isomer of GSK-F1 (HY-100603). GSK-F1 (Compound F1) is an orally active PI4KA inhibitor with pIC₅₀ values of 8.0, 5.9, 5.8, 5.9, 5.9 and 6.4 against PI4KA, PI4KB, PI3KA, PI3KB, PI3KG and PI3KD, respectively. GSK-F1 can be used for HCV infection research.

Schisantherin B (Gomisin-B) (Standard) is the analytical standard of Schisantherin B. This product is intended for research and analytical applications. Schisantherin B is a lignan compound and one of the active components of Schisandra chinensis. Schisantherin B activates the PI3K/AKT signaling pathway, restores the activity of GSK3β, and reduces the hyperphosphorylation of tau protein in hippocampal and cerebral cortical tissues. Schisantherin B upregulates the level of GLT-1, decreases the expression of pro-inflammatory cytokines TNF-α/IL-1β/IL-6, upregulates the expression of IL-10, and inhibits cell apoptosis. Schisantherin B is applicable to the research of spinal cord injury, Alzheimer's disease and depression.

NSC781406 (Standard) is the analytical standard of NSC781406 (HY-100470). This product is intended for research and analytical applications. NSC781406 is a highly potent PI3K and mTOR inhibitor with an IC50 of 2 nM for PI3Kα.