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Isoforms Recommended: PI3Kα
Results for "

PI3Kα

" in MedChemExpress (MCE) Product Catalog:

201

Inhibitors & Agonists

1

Fluorescent Dyes

1

Biochemical Assay Reagents

4

Natural
Products

2

Isotope-Labeled Compounds

1

GMP Molecules

Cat. No. 상품명 Target 연구분야 Chemical Structure
  • 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, 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
  • HY-156681
    Tersolisib
    1 Publications Verification

    STX-478; STX-478-101; LY4064809

    PI3K Cancer
    STX-478 (compound 80) is an oral CNS-penetrant allosteric mutant-selective PI3Kα inhibitor. STX-478 shows robust and durable tumor regression and can be used in cancer research .
    Tersolisib
  • 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-19962
    Paxalisib
    5 Publications Verification

    GDC-0084

    PI3K mTOR Cancer
    Paxalisib (GDC-0084) is a brain penetrant inhibitor of PI3K and mTOR, with Kis of 2 nM, 46 nM, 3 nM, 10 nM and 70 nM for PI3Kα PI3Kβ, PI3Kδ, PI3Kγ and mTOR, respectively .
    Paxalisib
  • HY-15177
    PF-04691502
    10+ Cited Publications

    PI3K mTOR Autophagy Cancer
    PF-04691502 is a potent and selective inhibitor of PI3K and mTOR. PF-04691502 binds to human PI3Kα, β, δ, γ and mTOR with Kis of 1.8, 2.1, 1.6, 1.9 and 16 nM, respectively.
    PF-04691502
  • HY-100398
    PF-04979064
    2 Publications Verification

    PI3K mTOR Cancer
    PF-04979064 is a potent and selective PI3K/mTOR dual kinase inhibitor with Kis of 0.13 nM and 1.42 nM for PI3Kα and mTOR, respectively.
    PF-04979064
  • 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-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 PI3Kγ and PI3Kα with IC50 of 16 nM and 39 nM, respectively.
    PIK-93
  • 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-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, PI3Kγ, 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-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-143275

    PROTACs PI3K Akt Cancer
    HL-8 is a PI3Kα PROTAC degrader. HL-8 promotes the ubiquitination and degradation of PI3Kα. HL-8 reduces pAKT levels. HL-8 has anticancer activity against colon and cervical cancer (Pink: PI3Kα ligand (HY-143277); Blue: E3 ligase VHL ligand (HY-138678); Black: linker (HY-W002042)) .
    HL-8
  • HY-W1126235

    D223

    Molecular Glues Ras PI3K GLUT Metabolic Disease
    DS02312223 (D223) is a molecular glue that promotes the binding of RAS to PI3Kα, with a Kd of 0.76 μM for p110α. DS02312223 increases the binding affinity between GTP-bound KRAS (KRAS-GMPPNP) and p110α by nearly three orders of magnitude (KD = 0.017 μM). DS02312223 stimulates the translocation of GLUT4 to the plasma membrane. DS02312223 promotes glucose uptake in the absence of insulin. DS02312223 can be used in diabetes research .
    DS02312223
  • 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-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 PI3Kδ 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-13440
    AMG 511
    5 Publications Verification

    PI3K Cancer
    AMG 511 is a potent and orally available pan inhibitor of class I PI3Ks, with Kis of 4 nM, 6 nM, 2 nM and 1 nM for PI3Kα, β, δ and γ, respectively. AMG 511 significantly suppresses PI3K signaling that is indicated by p-Akt (Ser473) decrease. AMG 511 exhibits anti-tumor activity in mouse glioblastoma xenograft model .
    AMG 511
  • HY-101272
    GDC-0326
    1 Publications Verification

    PI3K Cancer
    GDC-0326 is a potent and selective PI3Kα inhibitor with a Ki of 0.2 nM.
    GDC-0326
  • HY-12869
    AZD-8835
    1 Publications Verification

    PI3K Cancer
    AZD8835 is a potent and selective inhibitor of PI3Kα and PI3Kδ with IC50s of 6.2 and 5.7 nM, respectively.
    AZD-8835
  • 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-107365

    PI3K mTOR Cancer
    PQR530 is a potent, ATP-competitive, orally bioavailable and brain-penetrant dual pan-PI3K/mTORC1/2 inhibitor, with a subnanomolar Kd toward PI3Kα and mTOR (0.84 and 0.33 nM, respectively). Antitumor activity .
    PQR530
  • 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 PI3Kγ with IC50s of 81 nM and 3.11 μM, respectively.
    WYE-687
  • 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-B1550

    DL-Benzoin; Desyl alcohol; (±)-2-Hydroxy-2-phenylacetophenone

    PI3K Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    Benzoin (DL-Benzoin) is a PI3Kα inhibitor with anticancer effects. Benzoin inihits the growth of colon cancer cell line (HCT-116) .
    Benzoin
  • 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-13864
    PF-4989216
    1 Publications Verification

    PI3K Apoptosis Cancer
    PF-4989216 is a potent and selective PI3Kα inhibitor with a Ki of 0.6 nM.
    PF-4989216
  • HY-174798

    PI3K Ligands for Target Protein for PROTAC Cancer
    PI3Kα Ligand-1 is the ligand for PI3Kα that can be used for synthesis of PROTACs, such as PI3Kα degrader-1 (HY-174461) .
    PI3Kα Ligand-1
  • HY-12340

    PI3K Cancer
    ETP-46321 is a potent and orally bioavailable PI3Kα and PI3Kδ inhibitor with Kiapps of 2.3 and 14.2 nM, respectively.
    ETP-46321
  • 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-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-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-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-156681A

    (S)-STX-478; (S)-STX-478-101; (S)-LY4064809

    PI3K Cancer
    (S)-STX-478 is the S-enantiomer of STX-478. STX-478 is a selective inhibitor of PI3Kα mutants, preventing metabolic dysfunction and demonstrating antitumor activity in xenograft mouse models with PI3Kα mutant tumors .
    (S)-Tersolisib
  • 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-128333

    PI3K mTOR Cancer
    PI3K/mTOR Inhibitor-4 is an orally active pan-class I PI3K/mTOR inhibitor. PI3K/mTOR Inhibitor-4 has enzymatic inhibition activity for PI3Kα, PI3Kγ, PI3Kδ and mTOR with IC50 values of 0.63 nM, 22 nM, 9.2 nM and 13.85 nM, respectively. PI3K/mTOR Inhibitor-4 can be used for the research of cancer .
    PI3K/mTOR Inhibitor-4
  • HY-10812

    PI3K mTOR Cancer
    GNE-490, a (thienopyrimidin-2-yl)aminopyrimidine, is a potent pan-PI3K inhibitor with IC50s of 3.5 nM, 25 nM, 5.2 nM, 15 nM for  PI3Kα, PI3Kβ, PI3Kδ and PI3Kγ, respectively. GNE-490 has >200 fold selectivity for mTOR (IC50=750 nM). GNE-490 shows potent suppression efficacy profile against MCF7.1 breast cancer xenograft model .
    GNE-490
  • HY-11105
    Pilaralisib analogue
    1 Publications Verification

    XL147 analogue

    PI3K Apoptosis Cancer
    Pilaralisib analogue (XL147 analogue) is a representative and selective PI3Kα inhibitor extracted from patent WO2012006552A1, Compound 147 in Table 1.
    Pilaralisib analogue
  • HY-131345A

    PI3K Cancer
    (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 .
    (S)-PI3Kα-IN-4
  • HY-143403

    PI3K Cancer
    PI3K-IN-31 (Compound 6b) is a potent PI3K inhibitor with IC50s of 3.7 nM, 74 nM, 14.6 nM, and 9.9 nM for PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ, respectively. PI3K-IN-31 has anticancer effects .
    PI3K-IN-31
  • HY-123849

    PI3K mTOR Cancer
    SN32976 is a potent and selective class I PI3K and mTOR inhibitor with IC50s of 15.1 nM, 461 nM, 110 nM, 134 nM and 194 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ and mTOR, respectively. SN32976 shows high selectivity among other 442 kinases. SN32976 shows anticancer effects .
    SN32976
  • HY-176281

    PI3K CDK Cancer
    PI3Kα-IN-26 (Compound 11e) is a PI3Kα inhibitor with an IC50 of 75.31 nM. PI3Kα-IN-26 has a broad-spectrum anticancer activity, such as leukemia, colon and breast cancer, without significant cytotoxic effect on the normal Vero cells (mean IC50s of 2.74, 3.50, 3.34 and 85.29 μM, respectively) .
    PI3Kα-IN-26
  • HY-147767

    PI3K Apoptosis Reactive Oxygen Species (ROS) Cancer
    PI3Kα-IN-6 (Compound 5b) is a PI3Kα inhibitor. PI3Kα-IN-6 exhibits anticancer potential and no toxicity in normal cells. PI3Kα-IN-6 increases generation of ROS, reduces mitochondrial membrane potential (MMP) and induces apoptosis .
    PI3Kα-IN-6
  • HY-160458

    PI3K Others
    PI3Kα-IN-17 (example 4) is a potent inhibitor of PI3Kα .
    PI3Kα-IN-17
  • HY-116563

    PI3K Cancer
    PI3Kα-IN-24 (WR23) is a PI3Kα inhibitor with an IC50 of 0.025 μM and exhibits a significant pAkt Ser473 suppression effect. PI3Kα-IN-24 can be utilized in cancer research .
    PI3Kα-IN-24
  • HY-161140

    PI3K Wnt Cancer
    PI3Kα-IN-16 (Z86) is a novel PI3Kα inhibitor with an IC50 value of 4.28 μM. PI3Kα-IN-16 has potent inhibitory efficiency on PI3K-mediated CRCs growth and migration. PI3Kα-IN-16 also inhibits the Wnt signaling pathway .
    PI3Kα-IN-16
  • HY-163360

    PI3K Cancer
    PI3Kα-IN-19 (Compound 1) is a PI3Kα inhibitor with a targeted binding site at the p110α catalytic subunit. PI3Kα is one of the most common dysregulated kinases used in cancer research .
    PI3Kα-IN-19

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