PI3K

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Product Name
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  1. SUMO inhibitor

    2-D08 is a cell permeable, mechanistically unique inhibitor of protein sumoylation. It is also inhibits Axl, IRAK4, ROS1, MLK4, GSK3β, RET, KDR and PI3Kα with IC50 values of 0.49, 3.9, 5.3, 9.8, 11, 11, 17 and 35 nM respectively in biochemical assays.
  2. PI3Kβ inhibitor

    SAR260301 is potent and selective Class I phosphatidylinositol-3-kinase (PI3K)β specific inhibitor with an IC50 of 52 nM for this isoform.
  3. Vps34 inhibitor

    Vps34-IN-2 is a novel, potent and selective inhibitor of Vps34 with IC50s of 2 and 82 nM on the Vps34 enzymatic assay and the GFP-FYVE cellular assay, respectively.
  4. 4-Methylbenzylidene camphor(4-MBC; Enzacamene)is an organic camphor derivative that is used in the cosmetic industry for its ability to protect the skin against UV, specifically UV B radiation.
  5. EGFR/PI3K dual inhibitor

    MTX-211 is a dual inhibitor of EGFR and PI3K, which plays important roles in the progression of KRAS mutant colorectal cancer. MTX-211 has the potential for the treatment of KRAS mutant colorectal cancer.
  6. P110δ inhibitor

    P110δ-IN-1 is a potent and selective inhibitor of P110δ extracted from patent WO 2014055647 A1, with an IC50 of 8.4 nM.
  7. alpha-Bisabolol is a nontoxic sesquiterpene alcohol present in natural essential oil, with anticancer activity. alpha-Bisabolol exerts selective anticancer effect on A549 NSCLC cells (IC50=15 μM) via induction of cell cycle arrest, mitochondrial apoptosis and inhibition of PI3K/Akt signalling pathways. alpha-Bisabolol also strongly induces apoptosis in glioma cells.
  8. PI3Kγ inhibitor

    PI3Kγ inhibitor 3 is a potent and remarkably selective PI3Kγ inhibitor with pIC50s of 9.1, 5.1, <4.5, and 6.5 for PI3Kγ, PI3Kα, PI3Kβ, and PI3Kδ, respectively.
  9. dual pan-PI3K/mTORC1/2 inhibitor

    PQR-530 is a potent, oral and brain-penetrant dual pan-PI3K/mTORC1/2 inhibitor, exhibiting antitumor activity.
  10. PI3Kδ inhibitor

    PI3Kdelta inhibitor 1 (Compound 5d) is a potent, selective and orally available PI3Kδ inhibitor with an IC50 of 1.3 nM.
  11. PI3Kα inhibitor

    GDC-0077 (RG6114) is a potent, orally available, and selective PI3Kα inhibitor (IC50=0.038 nM).
  12. PI3Kδ inhibitor

    PI3Kδ-IN-1 is a potent, selective, and efficacious PI3Kδ inhibitor with an IC50 of 1.7 nM.
  13. PI3Kγ inhibitor

    PI3Kγ inhibitor 2 (Compound 16) is an orally bioavailable, CNS-penetrant, isoform selective PI3Kγ inhibitor with a Ki of 4 nM.
  14. dual pan-PI3K/mTOR inhibitor

    PI3K/mTOR Inhibitor-2 is a potent dual pan-PI3K/mTOR inhibitor with IC50s of 3.4/34/16/1 nM for PI3Kα/PI3Kβ/PI3Kδ/PI3Kγ and 4.7 nM for mTOR. Antitumor activity.
  15. PI3Kδ/PI3Kγ inhibitor

    Tenalisib R Enantiomer is an R enantiomer of Tenalisib.
  16. PI3Kδ inhibitor

    CHMFL-PI3KD-317 is a highly potent, selective and orally active PI3Kδ inhibitor, with an IC50 of 6 nM.
  17. PI3K/mTOR inhibitor

    PI3K/mTOR Inhibitor-1 is a potent, orally bioavailable dual PI3K/mTOR inhibitor with IC50s of 20/376/204/46 nM and 186 nM for PI3Kα/PI3Kβ/PI3Kγ/PI3Kδ and mTOR, respectively. Antitumor activity.
  18. Lysosomotropic autophagy inhibitor

    IITZ-01 is a potent lysosomotropic autophagy inhibitor with single-agent antitumor activity, with an IC50 of 2.62 μM for PI3Kγ.
  19. radioprotectant

    Recilisib is a radioprotectant, which can activate AKT, PI3K activities in cells.
  20. PI3Kδ inhibitor

    Linperlisib is a potent and selective inhibitor of PI3Kδ extracted from patent WO 2015055071 A1, compound 10; has an IC50 of 6.4 nM.
  21. PI3K/mTOR inhibitor

    NSC781406 is a highly potent PI3K and mTOR inhibitor with an IC50 of 2 nM for PI3Kα.
  22. PI3Kα inhibitor

    GDC-0326 is a potent and selective PI3Kα inhibitor with a Ki of 0.2 nM.
  23. PI3K inhibitor

    SF2523 is a highly selective and potent inhibitor of PI3K with IC50s of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively.
  24. p110β inhibitor

    Rac)-AZD 6482 ((Rac)-KIN-193) is a less active racemate of AZD 6482. AZD 6482 is a potent and selective p110β inhibitor with an IC50 of 0.69 nM.
  25. PI3K β/δ inhibitor

    PI3K-IN-6 (compound 20a) is an oral active and highly selective phosphoinositide 3-kinase (PI3K) β/δ inhibitor, with IC50 values of 7.8 nM/5.3 nM for PI3K β/δ, respectively.
  26. PI3Kδ inhibitor

    LAS191954 is a potent, selective and orally active PI3Kδ inhibitor for inflammatory diseases treatment, with an IC50 of 2.6 nM.
  27. ILK inhibitor

    OSU-T315 (ILK-IN-1) is a small Integrin-linked kinase (ILK) inhibitor with an IC50 of 0.6 μM, inhibiting PI3K/AKT signaling by dephosphorylation of AKT-Ser473 and other ILK targets (GSK-3β and myosin light chain).
  28. PI3Kδ inhibitor

    CAL-130 Racemate is the racemate of CAL-130. CAL-130 Racemate is a PI3Kδ inhibitor.
  29. PI3K/Akt activator

    YS-49 is a PI3K/Akt (a downstream target of RhoA) activator, to reduce RhoA/PTEN activation in the 3-methylcholanthrene-treated cells.
  30. PI3KC3 isoform Vps34 inhibitor

    SAR405 is a first-in-class, selective, and ATP-competitive PI3K class III (PI3KC3) isoform Vps34 inhibitor (IC50=1.2 nM; Kd=1.5 nM).
  31. PI3Kα inhibitor

    Alpelisib hydrochloride (BYL-719 hydrochloride) is a potent, orally active, and selective PI3Kα inhibitor with IC50s of 5 nM, 250 nM, 290 nM and 1200 nM for p110α, p110γ, p110δ, and p110β, respectively.
  32. multi-kinase inhibitor

    Rigosertib sodium (ON-01910 sodium) is a multi-kinase inhibitor and a selective anti-cancer agent, which induces apoptosis by inhibition the PI3K/Akt pathway, promotes the phosphorylation of histone H2AX and induces G2/M arrest in cell cycle.
  33. multi-kinase inhibitor

    Rigosertib (ON-01910) is a multi-kinase inhibitor and a selective anti-cancer agent, which induces apoptosis by inhibition the PI3 kinase/Akt pathway, promots the phosphorylation of histone H2AX and induces G2/M arrest in cell cycle.
  34. PI3Kδ inhibitor

    Umbralisib R-enantiomer (TGR-1202 R-enantiomer) is a PI3Kδ inhibitor, which is the less active enantiomer of TGR-1202.
  35. lysosomal exocytosis inhibitor

    Vacuolin-1 is a potent and cell-permeable lysosomal exocytosis inhibitor.
  36. pan-PI3K inhibitor

    GNE-490 is a highly selective pan-PI3K inhibitor that demonstrates selectivity over mTOR.
  37. Gβγ subunit signalling inhibitor

    Gallein is a G protein βγ (Gβγ) subunit signalling inhibitor. Gallein disrupts the interaction of Gβγ subunits with the PI3Kγ. Anticancer agent.
  38. Syk/PI3K inhibitor

    SRX3207 is an orally active and first-in-class dual Syk/PI3K inhibitor, with IC50 values of 10.7 nM and 861 nM for Syk and PI3Kα, respectively. SRX3207 relieves tumor immunosuppression.
  39. PI3Kδ inhibitor

    Nemiralisib (GSK2269557 free base) is a potent and highly selective PI3Kδ inhibitor with a pKi of 9.9.
  40. PI3Kδ inhibitor

    Selective PI3Kδ Inhibitor 1 (compound 7n) is an inhibitor of PI3Kδ with an IC50 of 0.9 nM and >1000-fold selectivity against other class I PI3K isoforms [PI3K α/γ/β=3670/1460/21300 nM].
  41. anti-tumor agent

    Sophocarpine (monohydrate) is one of the significant alkaloid extracted from the traditional herb medicine Sophora flavescens which has many pharmacological properties such as anti-virus, anti-tumor, anti-inflammatory.
  42. monounsaturated fatty acid

    Erucic acid, a monounsaturated fatty acid (MUFA), is isolated from the seed of Raphanus sativus L. Erucic acid can readily cross the blood-brain barrier (BBB), it has been reported to normalize the accumulation of very long-chain fatty acids in the brain. Erucic acid can improve cognitive impairment and be effective against dementia .
  43. PI3Kβ inhibitor

    AZD6482 (S-isomer), CAS#1173900-37-2, is an isomer of AZD6482 (MedKoo Cat#406268) with S-configuration. AZD6482 is a potent, selective and ATP competitive PI3Kβ inhibitor (IC(50) 0.01 μm).
  44. PI3K inhibitor

    MDK34597 is a PI3K inhibitor. MDK34597 has CAS#371934-59-7, the last 5 digits of which were used for its name. MDK34597 is an analog of PI-103 and acts as a dual PI3K/mTOR Inhibitor.
  45. ILK inhibitor

    ILK-IN-2 (OSU-T315 analog) is a ILK inhibitor.
  46. PI3K activator

    740 Y-P (740YPDGFR; PDGFR 740Y-P) is a potent and cell-permeable PI3K activator. 740 Y-P readily binds GST fusion proteins containing both the N- and C- terminal SH2 domains of p85 but fails to bind GST alone.

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