PI3K Inhibitor

PI3K-IN-41 (compound 2) is a photocaged compound, as well as a photocaged PI3K inhibitor (IC₅₀=18.92 nM) with anticancer properties. PI3K-IN-41 has potential to be used in precisely controlled cancer therapeutics. PI3K-IN-41 exhibits potent PI3K ihibition upon UV light irradiation, and enhances antitumor effect.

Sinigrin (Standard) (Allyl-glucosinolate (Standard)) is the analytical standard of Sinigrin (HY-N0404). This product is intended for research and analytical applications. Sinigrin (Allyl-glucosinolate) is an orally active glucosinolate found in cruciferous plants. Sinigrin possesses multiple activities such as anti-cancer, antibacterial, antifungal, anti-inflammatory, antioxidant, and inhibition of fat synthesis. Sinigrin can be used in the research of tumors, inflammatory, and metabolic diseases.

LAS195319 is an orally active and potent inhibitor against PI3Kδ with an IC₅₀ value of 0.5 nM. LAS195319 is also a highly selective inhibitor against an extensive panel of proteins, lipid kinases and GPCRs. LAS195319 causes an inhibition of neutrophil and eosinophil infiltration. LAS195319 is promising for research of respiratory diseases such as asthma and chronic obstructive pulmonary disease (COPD).

Anticancer agent 190 (compound 3e) is an inhibitor targeting KSP (Kinesin) and PI3Kδ with activity against breast cancer.

D-Allose-¹³C-2 is the ¹³C labeled D-Allose (HY-128741). D-Allose exhibits antitumor activity against various cancer cells. D-Allose scavenges reactive oxygen species (ROS) and reduces oxidative stress damage. D-Allose exhibits anti-inflammatory and neuroprotective through inhibition of TLR4/PI3K/AKT signaling pathway. D-Allose exhibits antihypertensive, cryoprotective, and anti-osteoporotic activities.

FD2157 is a photosensitive PI3K inhibitor, with IC₅₀s of 43 nM, 83 nM, 84 nM, 14 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ respectively. FD2157 potently inhibits cancer cell proliferation and induces cell apoptosis when exposed to 365 nm UV light.

Multi-target kinase inhibitor 4 (Compound 2) is a PI3K/DNA-PK inhibitor and potent chemosensitizer that can increase the amount of DNA double strand breaks induced by Doxorubicin (HY-15142A). Multi-target kinase inhibitor 4, is an efficient inhibitor of multidrug resistance (MDR) that exhibits inhibitory activity toward P-glycoprotein-mediated drug efflux. Multi-target kinase inhibitor 4 can be loaded into PEG-coated LNPs.

Calebin A is a PI3K/Akt/mTOR, MAPK, and NF-κB inhibitor with oral effectiveness. Calebin A can block the autophagy-repressive, inhibiting apoptosis. Calebin A has anti-tumor activity by epigenetic regulation. Calebin A suppresses adipogenesis, modulates thermogenesis, and enriches gut probiotics. Calebin A can be used in research on osteoarthritis, Alzheimer's disease, type 2 diabetes, malignant peripheral nerve sheath tumors, and colorectal cancer.

PI3Kγ inhibitor 6 (compound 9) is a PI3Kγ inhibitor. PI3Kγ inhibitor 6 can be used for the research of inflammatory and autoimmune diseases.

Polygalasaponin F (Standard) is the analytical standard of Polygalasaponin F. This product is intended for research and analytical applications. Polygalasaponin F is an orally active triterpenoid saponin monomer. Polygalasaponin F downregulates the expression of Bax, p53, caspase-3, NF-κB p65 and MEK1; restores and upregulates the expression of Bcl-2; activates the PI3K/Akt signaling pathway; inhibits the phosphorylation of p38 MAPK, nuclear translocation of NF-κB, TLR4-mediated signaling pathway, mitophagy (Mitophagy) and ROS production; enhances cell viability and suppresses apoptosis (Apoptosis). Polygalasaponin F maintains mitochondrial function, alleviates Ca²⁺ overload, upregulates pCREB and BDNF, preserves cell viability and inhibits the release of inflammatory cytokines. Polygalasaponin F alleviates lung injury induced by influenza A H1N1 and cerebral ischemia-reperfusion injury. Polygalasaponin F is applicable to researches related to Parkinson's disease, cerebral ischemia, pneumonia induced by influenza A H1N1, stroke and Alzheimer's disease.

Taxamairin B is a potent anti-inflammatory agent. Taxamairin B decreases proinflammatory cytokines (TNF-α, IL-1β and IL-6) expression and the production of NO and ROS in LPS-induced RAW264.7 cells. Taxamairin B exhibits significant protective effects in LPS-induced acute lung injury in mice.

NVP-BBD130 is a potent, stable, ATP-competitive and orally active dual PI3K and mTOR inhibitor. NVP-BBD130 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

A2073 is a flavagline derivative that potently inhibits the proliferation of erythroleukemia cells by causing cell cycle arrest and suppressing the MAPK, NF-κB, and PI3K signaling pathways. A2073 formes stable interactions with cell cycle-related proteins (CDK1, CCNA2, PRIM1). A2073 exhibits significant anti-proliferative activity against tumor cells while maintaining a favorable toxicity profile in a zebrafish xenograft tumor model. A2073 can be used for the study of acute erythroleukemia.

EGFR-IN-214 is an orally active EGFR inhibitor with an EC₅₀ of 3.353 μM. EGFR-IN-214 blocks the downstream PI3K/Akt signaling pathway, induces intracellular ROS accumulation and Caspase-dependent apoptosis. EGFR-IN-214 exhibits antiproliferative activity in cancer cells and inhibits tumor growth in xenograft models. EGFR-IN-214 can be used in studies related to hepatocellular carcinoma.