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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V4531 | Taselisib (GDC0032) | 1282512-48-4 | Taselisib (formerly also known as GDC-0032 or RG-7606), an imidazobenzoxazepin compound, is a novel and potent β-sparing small molecule inhibitor ofPI3KwithKivalues of 0.29 nM, 0.91 nM, 0.97 nM for PI3Kα, PI3Kβ and PI3Kγ, respectively. |
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V3107 | Tenalisib | 1639417-53-0 | Tenalisib (also known as RP6530) is a new, potent and selective dualPI3Kδ/γinhibitor with anticancer activity. |
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V3108 | Tenalisib R Enantiomer | 1639417-54-1 | Tenalisib R Enantiomer is the R-isomer of Tenalisib (also known as RP-6530). |
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V0129 | TG100-115 | 677297-51-7 | TG100-115 is a novel, potent and selective PI3Kγ/δ inhibitor with potential cardioprotecting effects. |
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V0142 | TG100713 | 925705-73-3 | TG100713 is a novel and potent pan-PI3K(phosphatidylinositol 3-kinase)inhibitor with potential anti-inflammatory activity. |
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V0109 | TGX-221 | 663619-89-4 | TGX-221 is a novel, potent, selective, and cell membrane permeable inhibitor of the PI3K p110β catalytic subunit with potential anticancer activity. |
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V69203 | UCL-TRO-1938 | 2919575-27-0 | UCL-TRO-1938 is a potent allosteric activator of PI3Kα with EC50 of approximately 60 μM. |
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V0556 | Umbralisib (TGR1202; RP-5264) | 1532533-67-7 | Umbralisib (formerly TGR-1202; RP-5264; TGR1202; RP5264;Ukoniq) is a novel, highly specific, orally bioavailable and potentPI3Kδinhibitor approved in 2021 by FDA to treat marginal zone lymphoma and follicular lymphoma. |
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V4754 | Umbralisib HCl | 1532533-78-0 | Umbralisib HCl (also known as TGR-1202; RP5264; trade nameUkoniq), the hydrochloride salt ofUmbralisib, is an orally bioavailable PI3Kδinhibitor that has gained FDAapproval in 2021for treating marginal zone lymphoma and follicular lymphoma. |
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V0106 | Voxtalisib (XL-765, SAR-245409) | 934493-76-2 | Voxtalisib (also known as SAR245409, XL765) is a potent, orally bioavailable small molecule and dual inhibitor of mTOR/PI3K (mammalian target of rapamycin/phosphatidylinositol 3 kinase) with anticancer activity. |
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V0119 | Voxtalisib Analog (SAR245409 Analog, XL765 Analog) | 1349796-36-6 | Voxtalisib analogue (also known as PI3K-IN-1, SAR-245409Analog, XL-765Analog), aVoxtalisib derivative,is a novel, potent and orally bioavailable dual inhibitor of mTOR/PI3K with potential anticancer activity. |
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V0985 | VPS34 inhibitor 1 | 1383716-46-8 | VPS34 inhibitor 1 (also known as Vps34-IN1, Compound 19, PIK-III analogue) is a potent and selective inhibitor of VPS34 the potential to serve as a chemical tool to modulate autophagy in Vivo. |
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V69209 | Vps34-IN-3 | 2770104-92-0 | Vps34-IN-3 is an orally bioactive and selective VPS34 kinase inhibitor. |
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V28052 | VPS34-IN1 | 1383716-33-3 | VPS34-IN1 (VPS34-IN-1) is a novel and potent Vps34 (vacuolar protein sorting 34) inhibitor with potential antitumor activity. |
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V4832 | VPS34-IN2 | 1383716-40-2 | VPS34-IN2 (PIK-III; Vps34-PIK-III) is a novel, potent and selective inhibitor ofVPS34 (IC50 = 18 nM) with the ability to modulate autophagy in Vivo. |
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V0143 | VS-5584 (SB-2343) | 1246560-33-7 | VS-5584 (also known as SB2343), a purine analog, is a novel, potent and selective small-molecule dual inhibitor of both mammalian target of rapamycin (mTOR) kinase and all class I phosphoinostide 3-kinase (PI3K) isoforms with potential anticancer activity. |
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V0111 | Wortmannin (SL-2052; KY-12420) | 19545-26-7 | Wortmannin (SL2052; KY12420),a steroid metabolite of the fungi Penicillium funiculosum, is the first described, potentselective and irreversible PI3K inhibitor with potential anticancer activity. |
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V0137 | YM201636 | 371942-69-7 | YM201636, apyridofuropyrimidine compound, is a novel, potent and selective PIKfyve (phosphatidylinositol‑3‑phosphate 5‑kinase) inhibitor with potential anti-retroviral replication and anticancer activity, as silencing of PIKfyve which is the sole enzyme for PtdIns(3,5)P(2) biosynthesis that controls proper endosome dynamics, can inhibit retroviral replication. |
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V0113 | ZSTK474 | 475110-96-4 | ZSTK474 is a novel, potent and ATP-competitive pan-PI3K inhibitor (class I) with potential anticancer activity. |
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V37833 | α-Linolenic acid | 463-40-1 | α-Linolenic acid is extracted from perilla and is an essential fatty acid that cannot be synthesized by the human body. |
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