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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V0122 | PIK-90 | 677338-12-4 | PIK-90 is a novel and potent PI3Kα/γ/δ inhibitor with potential anticancer activity. |
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V0120 | PIK-93 | 593960-11-3 | PIK-93, aphenylthiazole analog,is a novel, potent, and selective PI4K (PI4KIIIβ) inhibitor with antiviral effects (antienterovirus activity). |
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V0150 | Pilaralisib (XL147; SAR245408) | 934526-89-3 | Pilaralisib (formerly XL-147; SAR-245408) is a novel, potent, orally bioavailable, ATP-competitive, selective and reversible inhibitor of class I PI3K (phosphatidylinositol 3-kinase) with potential anticancer activity. |
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V0112 | Pilaralisib analog (XL147 analog, SAR245408 analog) | 956958-53-5 | Pilaralisib analog (XL-147 analog, SAR-245408) is novel, selective, potent, orally bioavailableand reversible small moleculeinhibitor of Class 1 PI3K (phosphatidylinositol 3 kinase) family of kinases with potential anticancer activity. |
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V81151 | PITCOIN4 | PITCOIN4 is a selective class IIPI3K-C2α inhibitor. | |
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V69187 | PKI-179 hydrochloride | 1463510-35-1 | PKI-179 HCl is a potent and orally bioactive dual PI3K/mTOR inhibitor (antagonist) with IC50s of 8 nM and 24 nM for PI3K-α, PI3K-β, PI3K-γ, PI3K-δ and mTOR, respectively. |
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V0141 | PKI-402 | 1173204-81-3 | PKI-402 is a novel, potent, dual and pan-inhibitor of PI3K/mTOR (phosphatidylinositol 3-kinase/mammalian target of rapamycin)with potential anticancer activity. |
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V0147 | Quercetin (Sophoretin; NSC 9221; Kvercetin) | 117-39-5 | Quercetin (Sophoretin; NSC-9221; Kvercetin) is a natural flavonoid isolated from various vegetables, fruits and wine. |
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V1988 | Quercetin Dihydrate | 6151-25-3 | Quercetin, a naturally occuring polyphenolic flavonoid found in a wide variety of plant-based foods, such as apples, onions, berries, and red wine, is utilized in many different cultures for their nervous system and anticancer effects. |
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V69188 | CYH33 methanesulfonate | 1494684-33-1 | CYH33 methanesulfonate is an orally bioactive, selective PI3Kα inhibitor (antagonist) with IC50s of 5.9 nM/598 nM/78.7 nM/225 nM for α/β/δ/γ isoforms respectively. |
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V69212 | RLY-2608 | 2733573-94-7 | RLY-2608 is the first selective allosteric inhibitor of PI3Ka. |
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V69199 | Roginolisib hemifumarate (MSC2360844 hemifumarate; IOA-244 hemifumarate) | 1621688-31-0 | Roginolisib (MSC2360844) hemifumarate is a potent, orally bioactive and selective PI3Kδ inhibitor (antagonist) with IC50 of 145 nM. |
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V2545 | Samotolisib (LY3023414; GTPL8918) | 1386874-06-1 | Samotolisib (LY3023414; GTPL8918)is an orally bioactive, selective and ATP competitive inhibitor of the class I PI3K isoforms, mTOR and DNA-PK withIC50s of 6.07 nM, 77.6 nM, 38 nM, 23.8 nM, 4.24 nM and 165 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ, DNA-PK and mTOR, respectively. |
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V4833 | SAR-405 | 1523406-39-4 | SAR405 (SAR-405) is a novel, potent and selective PIK3C3/Vps34inhibitor (IC50 = 1.2 nM) with anticancer activity. |
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V5889 | SAR260301 | 1260612-13-2 | SAR260301 is potent, orally bioavailable and selective Class I phosphatidylinositol-3-kinase (PI3K)β specific inhibitor with an IC50 of 52 nM for PI3Kβ. |
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V3970 | SELETALISIB | 1362850-20-1 | Seletalisib (formerlyknown as UCB-5857) is a novel, potent, ATP-competitive, and selective, small-molecule inhibitor of PI3Kδwith an IC50 value of 12 nM. |
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V2969 | SF2523 | 1174428-47-7 | SF2523 (SF-2523; SF 2523) is a novel, selective and potent dual inhibitor of PI3K-BRD4 with potentialanticancer activities. |
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V69195 | SN32976 | 1246202-11-8 | SN32976 is a potent and specific class I PI3K and mTOR inhibitor (antagonist) with IC50s of 15.1 nM, 461 nM, 110 nM, 134 nM and 194 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ and mTOR, respectively. |
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V4886 | Sonolisib (PX866) | 502632-66-8 | Sonolisib (also known as PX-866), a wortmannin analog, is a novel, an oral, irreversible, and pan-isoform small-molecule inhibitor ofphosphoinositide 3-kinase/PI3K(IC50=0.1 nM (p110α), 1.0 nM (p120γ), 2.9 nM (p110δ)) with with potential antineoplastic activity. |
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V69204 | STX-478 | 2883540-92-7 | STX-478 (Compound 80) is an orally bioactive, BBB (blood-brain barrier) permeable (penetrable), mutation-selective allosteric PI3Kα inhibitor. |
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