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.
- Cat.No. Product Name Information
- GC62450 (S)-PI3Kα-IN-4 (S)-PI3Kα-IN-4 is a potent inhibitor of PI3Kα, with an IC50 of 2.3 nM. (S)-PI3Kα-IN-4 shows 38.3-, 4.25-, and 4.93-fold selectivity for PI3Kα over PI3Kβ, PI3Kδ, and PI3Kγ, respectively. (S)-PI3Kα-IN-4 can be used for the research of cancer.
- GC35037 1,3-Dicaffeoylquinic acid 1,3-Dicaffeoylquinic acid is a caffeoylquinic acid derivative, and activates PI3K/Akt.
- GC41992 1-Deoxynojirimycin (hydrochloride) 1-Deoxynojirimycin (1-dNM) (hydrochloride), produced by Bacillus species, is a glucose analog that potently inhibits α-glucosidase I and II.
3-Methyladenine is a classic autophagy inhibitor.
- GC16157 740 Y-P PI 3-kinase activator,cell permeable
- GC17550 A66 P110α inhibitor
- GC10860 Acalisib (GS-9820) Acalisib (GS-9820) is a potent and selective PI3Kδ inhibitor with an IC50 of 12.7 nM.
- GC13913 AMG319 PI3Kδ inhibitor
- GC35395 Arnicolide D Arnicolide D is a sesquiterpene lactone isolated from Centipeda minima. Arnicolide D modulates the cell cycle, activates the caspase signaling pathway and inhibits the PI3K/AKT/mTOR and STAT3 signaling pathways. Arnicolide D inhibits Nasopharyngeal carcinoma (NPC) cell viability in a concentration- and time-dependent manner.
- GC11910 AS-041164 PI3Kγ inhibitor
- GC13901 AS-252424 PI3Kγ inhibitor,novel and potent
- GC38061 AS-604850 A selective inhibitor of PI3Kγ
- GC12080 AS-604850 PI3Kγ inhibitor,selective and ATP-competitve
- GC12474 AS-605240 Potent and selective PI 3-Kγ inhibitor
- GC62335 AZ2 AZ2 is a highly selective PI3Kγ inhibitor (The pIC50 value for PI3Kγ is 9.3).
- GC64938 AZD-7648 AZD-7648 is a potent, orally active, selective DNA-PK inhibitor with an IC50 of 0.6 nM. AZD-7648 induces apoptosis and shows antitumor activity.
- GC65149 AZD3458 AZD3458 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.
PI3Kβ inhibitor,potent and selective
- GC65507 AZD8154 AZD8154 is a novel inhaled selective PI3Kγδ dual inhibitor targeting airway inflammatory disease.
- GC12576 AZD8186 Potent and selective inhibitor of PI3Kβ and PI3Kδ
- GC11248 AZD8835 PI3Kα and PI3Kδ inhibitor
- GC17766 BAY 80-6946 (Copanlisib) BAY 80-6946 (Copanlisib) (BAY 80-6946) is a potent, selective and ATP-competitive pan-class I PI3K inhibitor, with IC50s of 0.5 nM, 0.7 nM, 3.7 nM and 6.4 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ, respectively. BAY 80-6946 (Copanlisib) has more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR. BAY 80-6946 (Copanlisib) has superior antitumor activity.
- GC62164 BAY1082439 BAY1082439 is an orally bioavailable, selective PI3Kα/β/δ inhibitor. BAY1082439 also inhibits mutated forms of PIK3CA. BAY1082439 is highly effective in inhibiting Pten-null prostate cancer growth.
- GC33145 BEBT-908 (PI3Kα inhibitor 1) BEBT-908 (PI3Kα inhibitor 1) (PI3Kα inhibitor 1) is a selective PI3Kα inhibitor extracted from patent US/20120088764A1, Compound 243, has an IC50<0.1 μM, PI3Kα inhibitor 1 also inhibits HDAC (0.1 μM≤IC50≤1 μM) .
- GC10060 BEZ235 (NVP-BEZ235) BEZ235 (NVP-BEZ235) (BEZ235) is an orally active and dual pan-class I PI3K and mTOR kinase inhibitor with IC50s of 4 nM/5 nM/7 nM/75 nM, and 20.7 nM for p110α/p110γ/p110δ/p110β and mTOR, respectively. BEZ235 (NVP-BEZ235) (BEZ235) inhibits both mTORC1 and mTORC2.
- GC13271 BEZ235 Tosylate
- GC35509 BGT226 BGT226 (NVP-BGT226) is a PI3K (with IC50s of 4 nM, 63 nM and 38 nM for PI3Kα, PI3Kβ and PI3Kγ)/mTOR dual inhibitor which displays potent growth-inhibitory activity against human head and neck cancer cells.
- GC11931 BKM120 An inhibitor of class I PI3K isoforms
- GC65534 Boc-L-cyclobutylglycine Boc-L-cyclobutylglycine is a glycine derivative that can be used for PI3K inhibitor synthesis.
- GC30156 Brevianamide F (Cyclo(L-Pro-L-Trp)) Brevianamide F (Cyclo(L-Pro-L-Trp)) (Cyclo(L-Pro-L-Trp)) is a mycotoxin isolated from Colletotrichum gloeosporioides, with antibacterial activity.
- GC16462 BYL-719 BYL-719 (BYL-719) is a potent, selective, and orally active PI3Kα inhibitor. BYL-719 (BYL-719) shows efficacy in targeting PIK3CA-mutated cancer. BYL-719 (BYL-719) also inhibits p110α/p110γ/p110δ/p110β with IC50s of 5/250/290/1200 nM, respectively. Antineoplastic activity.
- GC13396 CAL-101 (Idelalisib, GS-1101) A selective PI3K p110δ inhibitor
- GC35579 CAL-130 CAL-130 is a PI3Kδ and PI3Kγ inhibitor with IC50s of 1.3 and 6.1 nM, respectively.
- GC11135 CAL-130 Hydrochloride
- GC35580 CAL-130 Racemate CAL-130 Racemate is the racemate of CAL-130. CAL-130 Racemate is a PI3Kδ inhibitor.
- GC14318 CAY10505 Potent PI3Kγ inhibitor
- GC10070 CGS 15943 adenosine receptor antagonist
- GC11868 CH5132799 Class I PI3K inhibitor
- GC65969 CHMFL-PI3KD-317 CHMFL-PI3KD-317 is a highly potent, selective and orally active PI3Kδ inhibitor, with an IC50 of 6 nM, and exhibits over 10-1500 fold selectivity over other class I, II and III PIKK family isoforms, such as PI3Kα (IC50, 62.6 nM), PI3Kβ (IC50, 284 nM), PI3Kγ (IC50, 202.7 nM), PIK3C2A (IC50, >10000 nM), PIK3C2B (IC50, 882.3 nM), VPS34 (IC50, 1801.7 nM), PI4KIIIA (IC50, 574.1 nM) and PI4KIIIB (IC50, 300.2 nM). CHMFL-PI3KD-317 inhibits PI3Kδ-mediated Akt T308 phosphorylation in Raji cells, with an EC50 of 4.3 nM. CHMFL-PI3KD-317 has antiproliferative effects on cancer cells.
- GC19109 CNX-1351 CNX-1351 is a potent and isoform-selective targeted covalent PI3Kα inhibitor with IC50 of 6.8 nM.
- GC12115 CUDC-907 A dual inhibitor of HDACs and PI3Ks
- GC68413 CYH33
- GC63391 CYH33 methanesulfonate CYH33 methanesulfonate is an orally active, highly selective PI3Kα inhibitor with IC50s of 5.9 nM/598 nM/78.7 nM/225 nM against α/β/δ/γ isoform, respectively. CYH33 methanesulfonate inhibits phosphorylation of Akt, ERK and induces significant G1 phase arrest in breast cancer cells and non-small cell lung cancer (NSCLC) cells. CYH33 methanesulfonate has potent activity against solid tumors.
- GC14798 CZC24832 A PI3Kγ inhibitor
- GC38482 Desmethylglycitein Desmethylglycitein (4',6,7-Trihydroxyisoflavone), a metabolite of daidzein, sourced from Glycine max with antioxidant, and anti-cancer activities.Desmethylglycitein binds directly to CDK1 and CDK2 in vivo, resulting in the suppresses CDK1 and CDK2 activity. Desmethylglycitein is a direct inhibitor of protein kinase C (PKC)α, against solar UV (sUV)-induced matrix matrix metalloproteinase 1 (MMP1). Desmethylglycitein binds to PI3K in an ATP competitive manner in the cytosol, where it inhibits the activity of PI3K and downstream signaling cascades, leading to the suppression of adipogenesis in 3T3-L1 preadipocytes.
- GC60782 Disitertide TFA Disitertide (P144) TFA is a peptidic transforming growth factor-beta 1 (TGF-β1) inhibitor specifically designed to block the interaction with its receptor. Disitertide (P144) TFA is also a PI3K inhibitor and an apoptosis inducer.
- GC62495 DS-7423 DS-7423 is a dual PI3K and mTOR inhibitor, with IC50 values of 15.6 nM, 34.9 nM for PI3Kα and mTOR, respectively. DS-7423 possesses anti-tumor activity.
- GC33162 Duvelisib R enantiomer (IPI-145 R enantiomer) Duvelisib R enantiomer is a PI3K inhibitor, which is the less active enantiomer of Duvelisib.
- GC38694 Erucic acid A 22carbon monounsaturated fatty acid
- GC38236 Esculetin A coumarin with diverse actions
- GC19145 ETP-46321 ETP-46321 is a potent and orally bioavailable PI3Kα and PI3Kδ inhibitor with Kiapps of 2.3 and 14.2 nM, respectively.
- GC38392 Euscaphic acid Euscaphic acid, a DNA polymerase inhibitor, is a triterpene from the root of the R. alceaefolius Poir. Euscaphic inhibits calf DNA polymerase α (pol α) and rat DNA polymerase β (pol β) with IC50 values of 61 and 108 μM. Euscaphic acid induces apoptosis.
- GC62973 FD223 FD223 is a potent and selective phosphoinositide 3-kinase delta (PI3Kδ) inhibitor. FD223 displays high potency (IC50=1 nM) and good selectivity over other isoforms (IC50s of 51 nM, 29 nM and 37 nM, respectively for α, β and γ). FD223 exhibits efficient inhibition of the proliferation of acute myeloid leukemia (AML) cell lines by suppressing p-AKT Ser473 thus causing G1 phase arrest during the cell cycle. FD223 has potential for the research of leukemia such as AML.
- GC17967 GDC-0032 GDC-0032 (GDC-0032) is a potent PI3K inhibitor targets PIK3CA mutations, with Kis of 0.12 nM, 0.29 nM, 0.97 nM, and 9.1 nM for PI3Kδ, PI3Kα, PI3Kγ and PI3Kβ, respectively.
- GC32710 GDC-0077 (RG6114) GDC-0077 (RG6114) is a potent, orally available, and selective PI3Kα inhibitor (IC50=0.038 nM). GDC-0077 (RG6114) exerts its activity by binding to the ATP binding site of PI3K, thereby inhibiting the phosphorylation of PIP2 to PIP3. GDC-0077 (RG6114) is more selective for mutant versus wild-type PI3Kα.
- GC10228 GDC-0084 PI3K and mTOR inhibitor, brain-permeable
- GC19161 GDC-0326 GDC-0326 is a potent and selective PI3Kα inhibitor with a Ki of 0.2 nM.
- GC10816 GDC-0941 GDC-0941 (GDC-0941) is a potent inhibitor of PI3Kα/δ with an IC50 of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold).
- GC16154 GDC-0941 dimethanesulfonate A pan inhibitor of class I PI3K isoforms
- GC11177 GDC-0980 (RG7422) GDC-0980 (RG7422) (GDC-0980; GNE 390; RG 7422) is a selective, potent, orally bioavailable Class I PI3 kinase and mTOR kinase (TORC1/2) inhibitor with IC50s of 5 nM/27 nM/7 nM/14 nM for PI3Kα/PI3Kβ/PI3Kδ/PI3Kγ, and with aKiof 17 nM for mTOR.
- GC64778 Gilmelisib Gilmelisib is an antineoplastic. Gilmelisib is a PI3K inhibitor (IC50 <1 nM for PI3K p110α) extracted from WO2017101847 A1, compound 1.
- GN10584 Ginsenoside Rk1
- GC38606 Glaucocalyxin A Glaucocalyxin A, an ent-kauranoid diterpene from Rabdosia japonica var., induces apoptosis in osteosarcoma by inhibiting nuclear translocation of Five-zinc finger Glis 1 (GLI1) via regulating PI3K/Akt signaling pathway. Glaucocalyxin A has antitumor effect.
- GC17338 GNE-317 potent, brain-penetrant PI3K inhibitor
- GC10340 GNE-477 dual PI3K/mTOR inhibitor
- GC68429 GNE-490
- GC15423 GNE-493 Pan-PI3K/mTOR inhibitor
- GC36186 GS-9901 GS-9901 is a highly selective and orally active PI3Kδ inhibitor, with an IC50 of 1 nM.
- GC65309 GSK-F1 GSK-F1 (Compound F1) is an orally active PI4KA inhibitor with pIC50 values of 8.0, 5.9, 5.8, 5.9, 5.9 and 6.4 against PI4KA, PI4KB, PI3KA, PI3KB, PI3KG and PI3KD, respectively.
- GC11018 GSK1059615 PI3K and mTOR inhibitor,potent and reversible
- GC15072 GSK2126458 GSK2126458 (GSK2126458) is an orally active and highly selective inhibitor of PI3K with Kis of 0.019 nM/0.13 nM/0.024 nM/0.06 nM and 0.18 nM/0.3 nM for p110α/β/δ/γ, mTORC1/2, respectively. GSK2126458 has anti-cancer activity.
- GC15595 GSK2269557 inhibitor of PI3Kδ
- GC15679 GSK2292767 PI3Kδ inhibitor,potent and selective
- GC64612 GSK251 GSK251 is a highly potent, highly selective, orally bioavailable inhibitor of PI3Kδ with a novel binding mode.
GSK2636771 is a potent adenosine triphosphate competitive oral inhibitor of PI3Kβ, with an IC50 of 5.
- GC38088 Hederacolchiside A1
- GC38168 Heterophyllin B Heterophyllin B is an active cyclic peptide isolated from Pseudostellaria heterophylla. Heterophyllin B provides a novel strategy for the treatment of esophageal cancer.
- GC64035 Hirsutenone Hirsutenone is an active botanical diarylheptanoid present in Alnus species and exhibits many biological activities, including anti-inflammatory, anti-tumor promoting and anti-atopic dermatitis effects.
- GC16713 HS-173 novel PI3K inhibitor
- GC62572 hSMG-1 inhibitor 11e hSMG-1 inhibitor 11e is a potent and selective hSMG-1 kinase inhibitor with an IC50 of 900-fold selectivity over mTOR (IC50 of 45 nM), PI3Kα/γ (IC50s of 61 nM and 92 nM) and CDK1/CDK2 (IC50s of 32 μM and 7.1 μM).
- GC61925 hSMG-1 inhibitor 11j hSMG-1 inhibitor 11j, a pyrimidine derivative, is a potent and selective inhibitor of hSMG-1, with an IC50 of 0.11 nM. hSMG-1 inhibitor 11j exhibits >455-fold selectivity for hSMG-1 over mTOR (IC50=50 nM), PI3Kα/γ (IC50=92/60 nM) and CDK1/CDK2 (IC50=32/7.1 μM). hSMG-1 inhibitor 11j can be used for the research of cancer.
- GC15540 IC-87114 PI3Kδ inhibitor
- GC62465 Idelalisib D5 Idelalisib D5 is a deuterium labeled Idelalisib. Idelalisib is a highly selective and orally bioavailable p110δ inhibitor.
- GC63017 IHMT-PI3Kδ-372 IHMT-PI3Kδ-372 is a potent and selective PI3Kδ inhibitor with an IC50 of 14 nM.
- GC19411 IITZ-01 IITZ-01 is a potent lysosomotropic autophagy inhibitor with single-agent antitumor activity, with an IC50 of 2.62 μM for PI3Kγ.
- GC13503 iMDK PI3K and endogenous midkine (MDK) expression inhibitor
- GC62376 iMDK quarterhydrate iMDK quarterhydrate is a potent PI3K inhibitor and inhibits the growth factor MDK (also known as midkine or MK). iMDK quarterhydrate suppresses non-small cell lung cancer (NSCLC) cooperatively with A MEK inhibitor without harming normal cells and mice.
- GC12416 INK1117 INK1117 (MLN1117) is a selective p110α inhibitor with an IC50 of 15 nM.
- GC10749 IPI-145 (INK1197) IPI-145 (INK1197) (IPI-145) is a selectivite p100δ inhibitor with IC50 of 2.5 nM, 27.4 nM, 85 nM and 1602 nM for p110δ, P110γ, p110β and p110α, respectively.
- GC31756 IPI-3063 IPI-3063 is a potent and selective PI3K p110δ inhibitor with an IC50 of 2.5?±?1.2 nM.
- GC19202 IPI549 IPI549 (IPI549) is a potent and selective PI3Kγ inhibitor with an IC50 of 16 nM. IPI549 shows >100-fold selectivity over other lipid and protein kinases.
- GN10023 Isorhamnetin
- GC14346 KU-0060648 Dual DNA-PK/PI3-K inhibitor, ATP-competitive
- GC36426 LAS191954 LAS191954 is a potent, selective and orally active PI3Kδ inhibitor for inflammatory diseases treatment, with an IC50 of 2.6 nM.
A potent and selective PI3Kδ inhibitor
- GC30884 LX2343 An inhibitor of BACE1 and PI3K
LY294002 is the first synthetic PI3Kα, δ and β inhibitor
- GC14371 LY3023414 LY3023414 (LY3023414) potently and selectively inhibits class I PI3K isoforms, DNA-PK, and mTORC1/2 with IC50s 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. LY3023414 potently inhibits mTORC1/2 at low nanomolar concentrations.
- GC19256 MTX-211 MTX-211 is a dual inhibitor of EGFR and PI3K, used for the treatment of cancer and other diseases.
- GC65442 Musk ketone Musk ketone (MK) is a widely used artificial fragrance.