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PI3Kα IC50

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149

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Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-10108
    LY294002
    Maximum Cited Publications
    1120 Publications Verification

    PI3K Casein Kinase DNA-PK Apoptosis Autophagy Infection Cancer
    LY294002 is a broad-spectrum inhibitor of PI3K with IC50s of 0.5, 0.57, and 0.97 μM for PI3Kα, PI3 and PI3, respectively . LY294002 also inhibits CK2 with an IC50 of 98 nM . LY294002 is a competitive DNA-PK inhibitor that binds reversibly to the kinase domain of DNA-PK with an IC50 of 1.4 μM. LY294002 is an apoptosis activator [3].
    LY294002
  • HY-101562
    Inavolisib
    5+ Cited Publications

    GDC-0077; RG6114

    PI3K Apoptosis Cancer
    Inavolisib (GDC-0077) is a potent, orally active, and selective PI3Kα inhibitor (IC50=0.038 nM). Inavolisib exerts its activity by binding to the ATP binding site of PI3K, thereby inhibiting the phosphorylation of PIP2 to PIP3. Inavolisib is more selective for mutant versus wild-type PI3Kα. Inavolisib can be used for the study of breast cancer .
    Inavolisib
  • HY-10681
    Gedatolisib
    5 Publications Verification

    PKI-587; PF-05212384

    PI3K mTOR Cancer
    Gedatolisib (PKI-587) is a highly potent dual inhibitor of PI3Kα, PI3, and mTOR with IC50s of 0.4 nM, 5.4 nM and 1.6 nM, respectively . Gedatolisib is equally effective in both complexes of mTOR, mTORC1 and mTORC2 .
    Gedatolisib
  • HY-139609
    Camonsertib
    2 Publications Verification

    RP-3500; ATR inhibitor 4

    ATM/ATR mTOR Cancer
    Camonsertib (RP-3500) is an orally active, selective ATR kinase inhibitor (ATRi) with an IC50 of 1.00 nM in biochemical assays. Camonsertib shows 30-fold selectivity for ATR over mTOR (IC50=120 nM) and >2,000-fold selectivity over ATM, DNA-PK, and PI3Kα kinases. Camonsertib has potent antitumor activity .
    Camonsertib
  • HY-15346
    Copanlisib
    30+ Cited Publications

    BAY 80-6946

    PI3K Apoptosis Cancer
    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, PI3, PI3 and PI3, respectively. Copanlisib has more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR. Copanlisib has superior antitumor activity .
    Copanlisib
  • HY-15346A
    Copanlisib dihydrochloride
    30+ Cited Publications

    BAY 80-6946 dihydrochloride

    PI3K Apoptosis Cancer
    Copanlisib dihydrochloride (BAY 80-6946 dihydrochloride) 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, PI3, PI3 and PI3, respectively. Copanlisib dihydrochloride has more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR. Copanlisib dihydrochloride has superior antitumor activity .
    Copanlisib dihydrochloride
  • HY-159852

    PI3K Ras Akt Cancer
    BBO-10203 is a potent inhibitor of PI3Kα and KRAS G12C, selectively and covalently binding to Cys242 in the RAS-Binding Domain of PI3Kα, and inhibiting both the GTP-bound and GDP-bound states of KRAS G12C with an IC50 of 0.031 nM and an EC50 of 0.02 nM. BBO-10203 disrupts the interaction between RAS isoforms and PI3Kα, leading to the inhibition of RAS-mediated PI3Kα activation, and reduces pERK expression, cell growth, and induces G1 arrest and apoptosis. BBO-10203 can be used for the research of breast cancer, colorectal cancer, and non-small cell lung cancer .
    BBO-10203
  • HY-154848
    UCL-TRO-1938
    3 Publications Verification

    PI3K Akt Cardiovascular Disease Neurological Disease Cancer
    UCL-TRO-1938 is a potent small molecule allosteric activator of PI3Kα with an EC50 value of approximately 60 μM. UCL-TRO-1938 can induce cell proliferation and has cardioprotective effects from ischaemia reperfusion injury and enhances nerve regeneration following nerve crush [3] .
    UCL-TRO-1938
  • HY-12868
    Bimiralisib
    4 Publications Verification

    PQR309

    PI3K mTOR Infection Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    Bimiralisib (PQR309) is a potent, brain-penetrant, orally bioavailable, pan-class I PI3K/mTOR inhibitor with IC50s of 33 nM, 451 nM, 661 nM, 708 nM and 89 nM for PI3Kα, PI3, PI3, PI3 and mTOR, respectively. Bimiralisib is an mTORC1 and mTORC2 inhibitor.
    Bimiralisib
  • HY-12513
    Samotolisib
    5+ Cited Publications

    LY3023414

    PI3K DNA-PK mTOR Autophagy Cancer
    Samotolisib (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. Samotolisib potently inhibits mTORC1/2 at low nanomolar concentrations .
    Samotolisib
  • HY-12046
    PIK-93
    5+ Cited Publications

    PI4K PI3K Virus Protease Cancer
    PIK-93 is the first potent, synthetic PI4K (PI4KIIIβ) inhibitor with IC50 of 19 nM, and also inhibits PI3 and PI3Kα with IC50 of 16 nM and 39 nM, respectively.
    PIK-93
  • HY-15174
    Dactolisib Tosylate
    65+ Cited Publications

    BEZ235 Tosylate; NVP-BEZ 235 Tosylate

    PI3K mTOR Autophagy Cancer
    Dactolisib Tosylate (BEZ235 Tosylate) is a dual PI3K and mTOR kinase inhibitor with IC50 values of 4, 75, 7, 5 nM for PI3Kα, β, γ, δ, respectively. Dactolisib Tosylate (BEZ235 Tosylate) inhibits mTORC1 and mTORC2.
    Dactolisib Tosylate
  • HY-12330
    AZD8186
    5+ Cited Publications

    PI3K Cancer
    AZD8186 is a PI3K inhibitor, which potently inhibits PI3(IC50=4 nM) and PI3Kδ (IC5050=12 nM) with selectivity over PI3Kα (IC50=35 nM) and PI3(IC50=675 nM).
    AZD8186
  • HY-173405

    Ras PI3K Akt Cancer
    VVD-699 is a covalent blocker of the RAS-p110α interaction with oral activity. VVD-699 inhibits activation of PI3Kα (IC50: 104 nM in H358 cells) . VVD-699 inhibits phosphorylated AKT. VVD-699 can be used for the research of KRAS mutant/amplified cancer .
    VVD-699
  • HY-16596

    PI3K Cancer
    CNX-1351 is a potent and isoform-selective targeted covalent PI3Kα inhibitor with IC50 of 6.8 nM.
    CNX-1351
  • HY-10683
    PKI-402
    10+ Cited Publications

    PI3K mTOR Cancer
    PKI-402 is a selective, reversible, ATP-competitive inhibitor of PI3K, including PI3K-α mutants, and mTOR (IC50=2, 3, 7,14 and 16 nM for PI3Kα, mTOR, PI3Kβ, PI3Kδ and PI3Kγ).
    PKI-402
  • HY-101146
    SF2523
    2 Publications Verification

    PI3K Epigenetic Reader Domain DNA-PK Cancer
    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, PI3, DNA-PK, BRD4 and mTOR, respectively.
    SF2523
  • HY-16526
    Pilaralisib
    5 Publications Verification

    XL-147; SAR245408

    PI3K Cancer
    Pilaralisib (XL147; SAR245408) is a potent and highly selective class I PI3Ks inhibitor with IC50s of 39 nM, 383 nM, 23 nM and 36 nM for PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ.
    Pilaralisib
  • HY-13334A
    BGT226
    5 Publications Verification

    NVP-BGT226

    PI3K mTOR Autophagy Cancer
    BGT226 (NVP-BGT226) is a PI3K (with IC50s of 4 nM, 63 nM and 38 nM for PI3Kα, PI3 and PI3)/mTOR dual inhibitor which displays potent growth-inhibitory activity against human head and neck cancer cells .
    BGT226
  • HY-15856B
    Flupentixol dihydrochloride
    2 Publications Verification

    Flupenthixol dihydrochloride

    Dopamine Receptor PI3K Apoptosis Neurological Disease Cancer
    Flupentixol is an orally active D1/D2 dopamine receptor antagonist and new PI3K inhibitor (PI3Kα IC50=127 nM). Flupentixol shows anti-proliferative activity to cancer cells and induces apoptosis. Flupentixol can also be used in schizophrenia, anxiolytic and depressive research [3].
    Flupentixol dihydrochloride
  • HY-16585
    VS-5584
    5 Publications Verification

    SB2343

    PI3K mTOR Cancer
    VS-5584 is a pan-PI3K/mTOR kinase inhibitor with IC50s of 16 nM, 68 nM, 42 nM, 25 nM, and 37 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ and mTOR, respectively. VS-5584 simultaneously blocks mTORC2 as well as mTORC1.
    VS-5584
  • HY-15466
    Izorlisib
    3 Publications Verification

    CH5132799

    PI3K Cancer
    Izorlisib (CH5132799) is a selective class I PI3K inhibitor. Izorlisib inhibits class I PI3Ks, particularly PI3Kα, with an IC50 of 14 nM.
    Izorlisib
  • HY-100385
    Brevianamide F
    2 Publications Verification

    Cyclo(L-Pro-L-Trp)

    PI3K Bacterial Infection
    Brevianamide F (Cyclo(L-Pro-L-Trp)) is a mycotoxin isolated from Colletotrichum gloeosporioides, with antibacterial activity. Brevianamide F shows potent PI3Kα inhibitory activity with an IC50 of 4.8 μM .
    Brevianamide F
  • HY-12034
    WYE-354
    5+ Cited Publications

    mTOR Autophagy Apoptosis Cancer
    WYE-354 is an ATP-competitive mTOR inhibitor with an IC50 of 5 nM. WYE-354 also inhibits PI3Kα and PI3 with IC50s of 1.89 μM and 7.37 μM, respectively. WYE-354 inhibits both mTORC1 and mTORC2. WYE-354 induces autophagy activation in vitro [3].
    WYE-354
  • HY-13431
    KU-0060648
    4 Publications Verification

    DNA-PK PI3K mTOR Cancer
    KU-0060648 is a dual inhibitor of PI3K and DNA-PK with IC50s of 4 nM, 0.5 nM, 0.1 nM, 0.594 nM and 8.6 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ and DNA-PK, respectively .
    KU-0060648
  • HY-10811
    GNE-493
    2 Publications Verification

    PI3K mTOR Cancer
    GNE-493 is a potent, selective, and orally available dual pan-PI3-kinase/mTOR inhibitor with IC50s of 3.4 nM, 12 nM, 16 nM, 16 nM and 32 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ and mTOR.
    GNE-493
  • HY-13334
    BGT226 maleate
    5 Publications Verification

    NVP-BGT226 maleate

    PI3K mTOR Autophagy Apoptosis Cancer
    BGT226 (NVP-BGT226 maleate) is a PI3K (with IC50s of 4 nM, 63 nM and 38 nM for PI3Kα, PI3 and PI3) /mTOR dual inhibitor which displays potent growth-inhibitory activity against human head and neck cancer cells .
    BGT226 maleate
  • HY-13531
    AS-604850
    1 Publications Verification

    PI3K Cancer
    AS-604850 is a potent, selective and ATP-competitive PI3 inhibitor with an IC50 value of 0.25 μM and a Ki value of 0.18 μM. AS-604850 shows isoform selective inhibitor of PI3 with over 30-fold selectivity for PI3Kδ and β, and 18-fold selectivity over PI3Kα, respectively .
    AS-604850
  • HY-12869
    AZD-8835
    1 Publications Verification

    PI3K Cancer
    AZD8835 is a potent and selective inhibitor of PI3Kα and PI3 with IC50s of 6.2 and 5.7 nM, respectively.
    AZD-8835
  • HY-131972

    PI3K Cancer
    PF-06843195 is a highly selective PI3Kα inhibitor with an IC50 of 18 nM in Rat1 fibroblasts. The Kis of PF-06843195 for PI3Kα and PI3 in biochemical kinase assay are less than 0.018 nM and 0.28 nM, respectively. PF-06843195 has great suppression of the PI3K/mTOR signaling pathway and durable antitumor efficacy .
    PF-06843195
  • HY-15271
    WYE-687
    3 Publications Verification

    mTOR PI3K Cancer
    WYE-687 is an ATP-competitive mTOR inhibitor with an IC50 of 7 nM. WYE-687 concurrently inhibits activation of mTORC1 and mTORC2. WYE-687 also inhibits PI3Kα and PI3 with IC50s of 81 nM and 3.11 μM, respectively.
    WYE-687
  • HY-13333

    BAG 956

    PI3K Cancer
    NVP-BAG956 is an ATP-competitive PI3K inhibitor with IC50s of 34, 56, 112 and 444 nM for PI3Kδ, PI3Kα, PI3Kγ and PI3Kβ, respectively.
    NVP-BAG956
  • HY-162713

    EGFR PI3K PPAR Cancer
    MTX-531 is an oral drug that inhibits EGFR (with an IC50 of 14.7 nM) and PI3K (with IC50 values of 6.4, 233, 8.3, and 1.1 nM for PI3Kα, PI3, PI3, and PI3 respectively), and it has anti-tumor effects. MTX-531 also acts as a weak agonist of PPARγ, with an IC50 of 2.5 µM, helping to alleviate hyperglycemia induced by PI3K inhibitors .
    MTX-531
  • HY-174461

    PROTACs PI3K Cancer
    PROTAC PI3Kα degrader-1 is a PI3Kα PROTAC degrader (DC50 = 0.08 μM), demonstrating good selectivity for PI3Kα degradation over PI3Kβ, PI3Kγ, and PI3Kδ. PROTAC PI3Kα degrader-1 effectively degrades PI3Kα in a time- and concentration-dependent, over PI3Kβ, PI3Ky and PI3Kδ, and potently inhibited the phosphorylation of AKT at the Ser473site. PROTAC PI3Kα degrader-1 shows significant in vivo anticancer efficacy in HGC-27 and DOHH2 xenograft models. (Pink: PI3Kα ligand : (HY-174798), Blue: E3 ligase CRBN Ligand (HY-10984), Black: Linker, E3 ligase ligand-linker conjugate (HY-W940885)) .
    PROTAC PI3Kα degrader-1
  • HY-118712

    mTOR Cancer
    WYE-23 is a mTOR inhibitor, and IC50 is 0.45 nM. It is selective to PI3Kα and IC50 is 661 nM. WYE-23 has antitumor activity .
    WYE-23
  • HY-124036

    PI3K mTOR Cancer
    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 .
    DS-7423
  • HY-136198

    Syk PI3K Cancer
    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 .
    SRX3207
  • HY-112443

    PI3K Metabolic Disease Inflammation/Immunology Cancer
    AZD3458 is a potent and remarkably selective PI3 inhibitor with pIC50s of 9.1, 5.1, <4.5, and 6.5 for PI3, PI3Kα, PI3, and PI3, respectively .
    AZD3458
  • HY-143404
    PI3K-IN-30
    3 Publications Verification

    PI3K Cancer
    PI3K-IN-30 (compound 6d) is a potent PI3K inhibitor with IC50s of 5.1, 136, 30.7 and 8.9 nM for PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ, respectively .
    PI3K-IN-30
  • HY-110109

    PI3K DNA-PK mTOR Cancer
    ETP-45658 is a potent PI3K inhibitor, with IC50s of 22.0 nM, 39.8 nM, 129.0 nM and 717.3 nM for PI3Kα, PI3, PI3 and PI3, respectively. ETP-45658 also can inhibit DNA-PK (IC50=70.6 nM) and mTOR (IC50=152.0 nM). ETP-45658 can be used for the research of cancer .
    ETP-45658
  • HY-100470
    NSC781406
    2 Publications Verification

    PI3K mTOR Cancer
    NSC781406 is a highly potent PI3K and mTOR inhibitor with an IC50 of 2 nM for PI3Kα.
    NSC781406
  • HY-150618
    PI3Kα-IN-9
    1 Publications Verification

    PI3K Apoptosis Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    PI3Kα-IN-9 (compound 27) is a selective, long-acting and oral active PI3Kα inhibitor with IC50 values of 4.4, 128, 146 and 153 nM for PI3Kα, PI3Kγ, PI3Kδ and PI3Kβ, respectively. PI3Kα-IN-9 has antiproliferative activity and induces apoptosis. PI3Kα-IN-9 can be used for cancer research .
    PI3Kα-IN-9
  • HY-147419

    PI3K Cancer
    Vulolisib is a potent and orally active phosphatidylinositol 3-kinase (PI3K) inhibitor, with IC50 values of 0.2 nM, 168 nM, 90 nM and 49 nM for PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ, respectively. Antiproliferative and antineoplastic activity .
    Vulolisib
  • HY-149669

    PI3K HDAC Apoptosis Cancer
    PH14 is a dual PI3K/HDAC inhibitor with IC50 values of 20.3 nM and 24.5 nM for PI3Kα and HDAC3, respectively. PH14 has antiproliferative activity and also induces apoptosis in Jeko-1 cells. PH14 can be used in cancer research, such as lymphoma .
    PH14
  • HY-10681R

    PI3K mTOR Reference Standards Cancer
    Gedatolisib (Standard) is the analytical standard of Gedatolisib. This product is intended for research and analytical applications. Gedatolisib (PKI-587) is a highly potent dual inhibitor of PI3Kα, PI3Kγ, and mTOR with IC50s of 0.4 nM, 5.4 nM and 1.6 nM, respectively . Gedatolisib is equally effective in both complexes of mTOR, mTORC1 and mTORC2 .
    Gedatolisib (Standard)
  • HY-10620

    PI3K mTOR Cancer
    PI3K-IN-22 is a PI3Kα/mTOR dual kinase inhibitor. PI3K-IN-22 has IC50s of 0.9, 0.6 nM for PI3Kα and mTOR, respectively. PI3K-IN-22 can be used for the research of cancer .
    PI3K-IN-22
  • HY-131345

    PI3K Cancer
    PI3Kα-IN-4 is a potent, selective and orally active inhibitor of PI3Kα, with an IC50 of 1.8 nM. PI3Kα-IN-4 has antitumor activity .
    PI3Kα-IN-4
  • HY-118717

    mTOR Cancer
    mTOR inhibitor WYE-28 (compound 28) is a selective inhibitor of mTOR>/b< (IC50)=0.08 nM. mTOR inhibitor WYE-28 inhibits PI3Kα with an IC50 value of 6 nM. mTOR inhibitor WYE-28 shows a metabolic time (T1/2) in nude mouse microsomes of 13 min .
    mTOR inhibitor WYE-28
  • HY-15174R

    BEZ235 Tosylate (Standard); NVP-BEZ 235 Tosylate (Standard)

    PI3K mTOR Autophagy Reference Standards Cancer
    Dactolisib (Tosylate) (Standard) is the analytical standard of Dactolisib (Tosylate). This product is intended for research and analytical applications. Dactolisib Tosylate (BEZ235 Tosylate) is a dual PI3K and mTOR kinase inhibitor with IC50 values of 4, 75, 7, 5 nM for PI3Kα, β, γ, δ, respectively. Dactolisib Tosylate (BEZ235 Tosylate) inhibits mTORC1 and mTORC2.
    Dactolisib Tosylate (Standard)
  • HY-15856A

    Flupenthixol

    Dopamine Receptor PI3K Apoptosis Neurological Disease
    Flupentixol is an orally active D1/D2 dopamine receptor antagonist and new PI3K inhibitor (PI3Kα IC50=127 nM). Flupentixol shows anti-proliferative activity to cancer cells and induces apoptosis. Flupentixol can also be used in schizophrenia, anxiolytic and depressive research [3].
    Flupentixol

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