PI3K (Phosphoinositide 3-kinase), via phosphorylation of the inositol lipid phosphatidylinositol 4,5-bisphosphate (PI(4,5)P2), forms the second messenger molecule phosphatidylinositol (3,4,5)-trisphosphate (PI(3,4,5)P3) which recruits and activates pleckstrin homology domain containing proteins, leading to downstream signalling events crucial for proliferation, survival and migration. The four distinct catalytic isoforms of class I PI3K enzymes are PI3K, PI3K, PI3K, and PI3K.
Three main classes of PI3K enzymes exist, with class IA being strongly linked to cancer. Catalytic subunits (p110α, p110β, or p110δ; encoded by PIK3CA, PIK3CB, and PIK3CD genes, respectively) and regulatory subunits (p85) make up heterodimeric lipid kinases known as class IA PI3K.
The PI3K pathway is crucial for the progression of the cell cycle, cell growth and survival, actin rearrangement and migration, and intracellular vesicular transport, among many other biological processes.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V2337 | AS041164 | 6318-41-8 | AS041164 is a novel and potent inhibitor of PI3K with selectivity for the class IB isoform PI3Kγ (IC50 = 70 nM) |
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V69215 | ATM Inhibitor-3 | 2769140-52-3 | ATM Inhibitor -3 (Compound 34) is a potent and specific ATM inhibitor (antagonist) with IC50 of 0.71 nM. |
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V69210 | ATM Inhibitor-4 | 2769140-74-9 | ATM Inhibitor -4 (Compound 39) is a potent and specific ATM inhibitor (antagonist) with IC50 of 0.32 nM. |
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V0124 | AZD-6482 (KIN-193) | 1173900-33-8 | AZD6482(KIN193) is a novel, potent, selective and ATP competitive PI3Kβ (phosphatidylinositol-3-kinase) inhibitor with potential anticancer activity. |
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V0152 | AZD8186 | 1627494-13-6 | AZD8186 (also known as AZD) is a novel, potent and selective inhibitor of PI3Kβ (phosphatidylinositol 3-kinase β) with potential anticancer activity. |
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V2544 | AZD8835 | 1620576-64-8 | AZD8835 is a novel, selective, and orally bioavailable inhibitor of the class I (PI3K) catalytic subunit alpha (PIK3CA) PI3Kα and PI3Kδ with IC50s of 6.2 and 5.7 nM, respectively with potential antineoplastic activity. |
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V103657 | BBO-10203 | 2971769-60-3 | BBO-10203 (Compound 758) binds to the RBD region of PI3Kα and inhibits the binding of K-, H-, and N-Ras to PI3Kα. |
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V4264 | BGT226 (NVP-BGT226) | 915020-55-2 | BGT226 (also known as NVP-BGT226) is a novel dual class PI3K(phosphatidylinositol 3-kinase)/mammalian target of rapamycin (mTOR) inhibitorwith IC50 of 4 nM/63 nM/38 nM. |
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V0131 | BGT226 (NVP-BGT226) | 1245537-68-1 | BGT226 maleate (also known as NVP-BGT226 maleate) is a novel and potent dual inhibitor of class I PI3K (phosphatidylinositol 3-kinase)/mammalian target of rapamycin (mTOR) with potential anticancer activity. |
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V17019 | Brevianamide F | 38136-70-8 | Brevianamide F (Cyclo(L-Pro-L-Trp)) is a mycotoxin extracted from Colletotrichum gloeosporioides with anti-bacterial effect. |
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V0139 | CAY10505 | 1218777-13-9 | CAY10505, the dehydroxylated form of AS-252424, is a novel,potent and selective inhibitor ofPI3Kγ (phosphoinositide 3-kinase) with a potential toimprove hypertension-associated vascular endothelial dysfunction. |
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V0138 | CH5132799 | 1007207-67-1 | CH5132799 is a novel and potent class I PI3K (phosphoinositide 3-kinase) inhibitor with potential anticancer activity. |
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V97408 | CHF-6523 | 2500579-21-3 | CHF-6523 is an orally active PI3Kδ inhibitor being investigated in the field of chronic obstructive pulmonary disease (COPD). |
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V18587 | CNX-1351 | 1276105-89-5 | CNX-1351 (CNX1351; CNX 1351) is a novel, potent, covalent and selective inhibitor of PI3Kα with anticancer activity. |
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V69216 | CXJ-2 | 2919976-92-2 | CXJ-2 is a cyclic peptide that displays moderate affinity for elastin-derived peptide (EDP). |
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V2542 | CZ415 | 1429639-50-8 | CZ415 is a potent, cell-permeable (Kd app = 6.9 nM), and ATP-competitive mTOR inhibitor with high selectivity over any other kinase (IC50 = 14.5 nM IC50 for pS6RP and 14.8 nM for pAKT) and very good pharmacokinetic properties which include moderate clearance and good oral bioavailability. |
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V0145 | CZC24832 | 1159824-67-5 | CZC24832 is a novel, potent and highly selectiveinhibitor of PI3Kγ (phosphoinostide 3-kinase γ)with apotential for treatment for inflammatory and autoimmune diseases (e. |
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V102553 | D-106669 | 938444-93-0 | D-106669 (Compound 150) is a potent inhibitor of PI3Kα with IC50 of 0.129 μM. |
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V105563 | Dactolisib hydrochloride | 2319647-83-9 | Dactolisib (BEZ235) hydrochloride is an orally active bi-pan class I PI3K and mTOR inhibitor with IC50 of 4 nM/5 nM/7 nM/75 nM and 20.7 nM for p110α/γ/δ/β and mTOR, respectively. |
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V69206 | DS-7423 | 1222104-37-1 | DS-7423 is a dual (bifunctional) inhibitor of PI3K and mTOR, with IC50s of 15.6 nM and 34.9 nM for PI3Kα and mTOR, respectively. |
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