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Home >> Signaling Pathways >> PI3K/Akt/mTOR Signaling >> PI3K

PI3K

PI3K (phosphatidylinositol-4,5-bisphosphate 3-kinase) is a family of enzymes involved in cellular functions such as cell growth, proliferation, differentiation, motility, survival and intracellular trafficking, which in turn are involved in cancer.

Products for  PI3K

  1. Cat.No. 产品名称 Information
  2. GC50332 TC KHNS 11 强效选择性 PI 3-激酶 δ；抑制剂；口服生物利用度
  3. GC38694 Erucic acid A 22-carbon monounsaturated fatty acid
  4. GC38606 Glaucocalyxin A Glaucocalyxin A is a biologically active ent-kauranoid diterpenoid isolated from Rabdosia japonica var. glaucocalyx with antitumor and anti-inflammatory activity. Glaucocalyxin A induces G2/M cell cycle arrest and apoptosis through the PI3K/Akt pathway in human bladder cancer cells.
  5. GC38482 Desmethylglycitein An active metabolite of daidzein
  6. GC38473 WYE-687 dihydrochloride An mTOR inhibitor
  7. GC38401 rac-AZD 6482 rac-AZD 6482 (rac-KIN-193) 是 AZD 6482 的低活性外消旋体，AZD 6482 是一种有效的选择性 p110β 抑制剂，IC50 为 0.69 nM。
  8. GC38392 Euscaphic acid A triterpene with diverse biological activities
  9. GC38236 Esculetin A coumarin with diverse actions
  10. GC38168 Heterophyllin B Heterophyllin B is an active cyclic peptide isolated from Pseudostellaria heterophylla, which provides a novel strategy for the treatment of esophageal cancer.
  11. GC38088 Hederacolchiside A1 Hederacolchiside A1 是从白头翁中分离的，通过调节 PI3K/Akt/mTOR 信号通路诱导凋亡，从而抑制肿瘤细胞的增殖。Hederacolchiside A1 具有抗血吸虫病活性，影响体内和体外的寄生虫生存力。
  12. GC37955 YS-49 monohydrate An inhibitor of platelet aggregation
  13. GC37954 YS-49 An inhibitor of platelet aggregation
  14. GC37922 Voxtalisib A dual inhibitor of PI3K and mTORC
  15. GC37855 Umbralisib R-enantiomer Umbralisib R-enantiomer (TGR-1202 R-enantiomer) 是 PI3Kδ 抑制剂，是 TGR-1202 活性较低的对映体。
  16. GC37854 Umbralisib hydrochloride Umbralisib hydrochloride (TGR-1202 hydrochloride) 是一种新颖的 PI3Kδ 抑制剂，IC50 和 EC50 值分别为 22.2 nM 和 24.3 nM；Umbralisib hydrochloride (TGR-1202 hydrochloride) 同时可抑制 CK1ε，EC50 值为 6.0 μM。
  17. GC37633 SF1126 SF1126 是临床相关的双重 PI3K/BRD4 泛抑制剂，具有抗肿瘤和抗血管生成活性。SF1126 是 RGDS-缀合的 LY294002 前药，其设计为表现出增加的溶解度并与肿瘤区室内的特定整联蛋白结合。SF1126 诱导细胞凋亡 (apoptosis)。
  18. GC36917 Pilaralisib A class I PI3K inhibitor
  19. GC36911 PI3kδ inhibitor 1 PI3kδ inhibitor 1 是一种有效的选择性 PI3Kδ 抑制剂，IC50 为 3.8 nM。
  20. GC36910 PI3Kγ inhibitor 1 PI3Kγ inhibitor 1 是一种 PI3Kδ 和 PI3Kγ 抑制剂，详细信息请参考专利文献 WO2014004470A1 中 Table 4 中的化合物 168。PI3Kγ inhibitor 1 抑制 PI3Kδ 和 PI3Kγ，IC50<100 nM。
  21. GC36909 PI3Kα/mTOR-IN-1

    PI3Kα/mTOR-IN-1 是一种有效的 PI3Kα/mTOR 双重抑制剂，在细胞实验中对 PI3Kα 的 IC50 值为 7 nM，在体外酶实验中对 mTOR 和 PI3Kα 的 Ki 值分别为 10.6 nM 和 12.5 nM。
  22. GC36908 PI3K-IN-6 PI3K-IN-6 (compound 20a) 是具有口服有效的、高度选择性的磷脂酰肌醇三激酶(PI3K) β/δ 的抑制剂，其对 PI3K β/δ 的 IC50 值分别为 7.8 nM 和 5.3 nM。PI3K-IN-6 (compound 20a) 可用于治疗磷酸酶和紧张素同系物 (PTEN) 缺乏性肿瘤。
  23. GC36907 PI3K-IN-2 PI3K-IN-2 (compound 10) 是一种口服有效的 PI3Kβ/δ 抑制剂 (IC50=7.1/8.6 nM)，与 PI3Kσ、PI3Kγ 相比 (IC50=13/190 nM)，选择性更好。
  24. GC36906 PI3Kdelta inhibitor 1 PI3Kdelta inhibitor 1 (Compound 5d) 是口服有效的选择性 PI3Kδ 抑制剂，IC50 为1.3 nM。
  25. GC36905 PI3K/HDAC-IN-1 PI3K/HDAC-IN-1 是一种有效的 (PI3K/HDAC) 双重抑制剂，高效抑制 PI3Kδ 和 HDAC1 的 IC50 值分别为 8.1 nM 和 1.4 nM。
  26. GC36832 P110δ-IN-1 ME-401 (P110δ-IN-1, PWT-143) is an oral, potent and selective inhibitor of Phosphatidylinositol 3-Kinase (PI3K) P110δ with IC50 of 0.6 nM in cellular assay.
  27. GC36807 ON 146040 ON 146040 是一种有效的 PI3Kα 和 PI3Kδ 抑制剂，IC50 分别约为 14 和 20 nM。ON 146040 也抑制 Abl1 (IC50<150 nM)。
  28. GC36786 NVP-QAV-572 Nav1.7-IN-2 是一种有效的 PI3K 抑制剂，IC50 为 10 nM，详细信息可参考专利文献US7998990B2 中的化合物 Example 8。
  29. GC36714 Nemiralisib Nemiralisib, also known as GSK-2269557, is a potent and selective PI3Kδ inhibitor(pKi = 9.9).
  30. GC36426 LAS191954 LAS191954 是有效的、选择性的、口服有效的 PI3Kδ 的抑制剂，可用于炎症相关疾病的研究，其 IC50 值为 2.6 nM。
  31. GC36186 GS-9901 GS-9901 是高度选择性的、口服有效的 PI3Kδ 的抑制剂，其 IC50 值为 1 nM。有治疗风湿性关节炎的潜能。
  32. GC35580 CAL-130 Racemate CAL-130 Racemate 是 CAL-130 的外消旋体。CAL-130 Racemate 是一种 PI3Kδ 抑制剂。
  33. GC35579 CAL-130 CAL-130 是一种 PI3Kδ 和 PI3Kγ 抑制剂，IC50 分别为 1.3 和 6.1 nM。
  34. GC35509 BGT226 BGT226 (NVP-BGT226) maleate is a novel class I PI3K/mTOR inhibitor for PI3Kα/β/γ with IC50 of 4 nM/63 nM/38 nM. Phase 1/2.
  35. GC35395 Arnicolide D A sesquiterpene lactone with anticancer activity
  36. GC35037 1,3-Dicaffeoylquinic acid An HIV-1 integrase inhibitor and free radical scavenger
  37. GC41992 1-Deoxynojirimycin (hydrochloride) An iminosugar with diverse biological activities
  38. GC19540 α-Linolenic Acid

    An essential ω-3 polyunsaturated fatty acid
  39. GC33385 PQR-530 A dual inhibitor of PI3Kα and mTOR
  40. GC33162 Duvelisib R enantiomer (IPI-145 R enantiomer) Duvelisib R 对映异构体是一种 PI3K 抑制剂，是 Duvelisib 活性较低的对映异构体。
  41. GC33145 BEBT-908 (PI3Kα inhibitor 1) BEBT-908 (PI3Kα inhibitor 1) (PI3Kα inhibitor 1) 是一种选择性 PI3Kα从专利US/20120088764A1中提取的抑制剂化合物243，IC50<0.1 μM, PI3Kα抑制剂 1 还抑制 HDAC (0.1 μM≤IC50≤1 μM)。
  42. GC33130 Recilisib (Ex-RAD) Recilisib (Ex-RAD) (ON 01210) 是一种辐射防护剂，可激活细胞中的 AKT、PI3K 活性。
  43. GC33014 NSC781406 A dual inhibitor of PI3K and mTOR
  44. GC32932 Vps34-IN-2 Vps34-IN-2是一种新型的，有效且有选择性的Vps34抑制剂，在Vps34酶促测定和GFP-FYVE细胞测定中的IC50值分别为2和82nM。
  45. GC32916 Parsaclisib (INCB050465) Parsaclisib (INCB050465, INCB-50465, IBI376) is a potent and highly selective PI3Kδ(PI3K delta) inhibitor with an IC50 of 1 nM at 1 mM ATP in biochemical assay and approximately 20,000-fold selectivity for PI3Kα, PI3Kβ, PI3Kγ and 57 other kinases.
  46. GC32847 PI4KIIIbeta-IN-9 PI4KIIIbeta-IN-9是一种有效的PI4KIIIβ抑制剂，IC50为7nM。PI4KIIIbeta-IN-9也抑制PI3Kδ和PI3Kγ，IC50分别为152nM和1046nM。
  47. GC32828 Tenalisib (RP6530) Tenalisib (RP6530) is a potent and selective dual PI3Kδ/γ inhibitor with IC50 values of 24.5 nM and 33.2 nM for PI3Kδ and PI3Kγ, respectively. Its selectivity over α and β isoforms are more than 300-fold and 100-fold, respectively.
  48. GC32710 GDC-0077 (RG6114) Inavolisib (GDC-0077, RG6114, RO-7113755) is a potent selective inhibitor of PI3K alpha (PI3Kα) with an IC50 of 0.038 nM. GDC-0077 is >300-fold more selective for PI3K alpha over the other class I PI3K isoforms (beta, delta, and gamma) and >2000-fold more selective over PIK family members. GDC-0077 binds to the ATP binding site of PI3K and inhibits the phosphorylation of PIP2 to PIP3.
  49. GC31756 IPI-3063 IPI-3063 is a potent and selective p110δ inhibitor with biochemical IC50 of 2.5?±?1.2 nM and IC50 values for the other class I PI3K isoforms (p110α, p110β, p110γ) are at least 400-fold higher.
  50. GC31751 PI3Kδ-IN-2

    PI3Kδ-IN-2 (YY-20394) 是 PI3K&#948 的强效、口服生物利用度和选择性抑制剂；提取自专利WO 2015055071 A1，化合物10； IC50 为 6.4 nM。
  51. GC31666 Seletalisib (UCB5857) Seletalisib (UCB-5857) is a novel small-molecule inhibitor of PI3Kδ with an IC50 value of 12 nM and shows significant selectivity to PI3Kδ with respect to the other class I PI3K isoforms (between 24- and 303-fold).

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