Search Result
| Isoforms Recommended: |
PI3Kδ
|
Results for "
PI3K-δ
" in MedChemExpress (MCE) Product Catalog:
3
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-101921
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- HY-15288
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PI3K
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Cancer
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PI3kδ inhibitor 1 is a potent and selective PI3Kδ inhibitor with an IC50 of 3.8 nM.
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- HY-142646
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PI3K
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Cancer
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PI3Kδ-IN-9 is a selective PI3Kδ inhibitor with an IC50 value of 3.8 nM.
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- HY-157128
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PI3K
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Inflammation/Immunology
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Se15 is a selective inhibitor of PI3Kδ with an IC50 value less than 0.1nM. Se15 can be used in research on autoimmune .
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- HY-108418
-
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PI3K
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Cancer
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PI3Kδ-IN-15 (compound 6b) is a selective PI3Kδ inhibitor with an IC50 of 0.5 nM for p110δ. PI3Kδ-IN-15 inhibits PI3Kδ with >30-fold higher potency than PI3Kγ, PI3Kβ, and PI3Kα .
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- HY-144993
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PI3K
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Cancer
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PI3Kδ/γ-IN-1 is a potent, selective PI3K-δ/γ inhibitor for research of hematological malignancies.
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- HY-122593
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PI3K
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Cancer
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PI3Kδ-IN-5 (compound 7n) is a highly potent and selective inhibitor of PI3Kδ with an IC50 of 0.9 nM .
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- HY-134472
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PI3K
|
Cancer
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PI3Kδ-IN-8 is a potent, selective and orally active PI3Kδ inhibitor, with an IC50 of 3.3 nM. PI3Kδ-IN-8 shows selectivity for PI3Kδ over PI3Kα, PI3Kβ, and PI3Kγ (IC50=377.2, 241.6, 17.9 nM, respectively). PI3Kδ-IN-8 has anti-tumor activity .
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- HY-155975
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PI3K
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Inflammation/Immunology
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PI3Kδ-IN-14 (Compound (S)-29) is a selective PI3Kδ inhibitor (IC50: 0.8 nM, Kd: 84.8 nM). PI3Kδ-IN-14 binds to the ATP-binding site of the kinase domain of PI3Kδ. PI3Kδ-IN-14 has anti-inflammatory activity by inhibiting the PI3K/AKT pathway. PI3Kδ-IN-14 ameliorates acute lung injury (ALI) .
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- HY-155232
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PI3K
Apoptosis
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Cancer
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PI3Kδ-IN-16 is a potent and selective inhibitor of PI3Kδ. PI3Kδ-IN-16 has a strong anti-proliferative effect on cells, causing cell cycle arrest and inducing apoptosis .
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- HY-144254
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PI3K
Akt
Apoptosis
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Cancer
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PI3Kδ-IN-10 is a highly potent and orally active PI3Kδ inhibitor with IC50 of 2 nM. PI3Kδ-IN-10 robustly suppresses the downstream AKT pathway to induce subsequent apoptosis in hepatocellular carcinoma models .
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- HY-155833
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PI3K
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Infection
Inflammation/Immunology
Cancer
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PI3Kδ-IN-13 (compound 89) is a PI3Kδ inhibitor (IC50=2.6 nM). PI3Kδ-IN-13 can be used in the research of cell proliferation diseases such as cancer, infection, inflammation and autoimmune diseases .
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- HY-125376
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PI3K
|
Cancer
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PI3Kδ-IN-3 (Compound 11) is a PI3Kδ inhibitor (IC50: 9 nM). PI3Kδ-IN-3 inhibits B cell function. PI3Kδ-IN-3 has good pharmacokinetic properties .
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- HY-149634
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PI3K
|
Cancer
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PI3Kδ-IN-17 (Compound S5) is a potent inhibitor of PI3Kδ, with IC50 of 2.82?nM. PI3Kδ-IN-17 shows strong inhibitory activity of proliferation in SU-DHL-6 cells (IC50 = 0.035 μM) .
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- HY-150638
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PI3K
Apoptosis
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Cancer
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PI3Kδ/γ-IN-3 (Compound 58) is a potent and orally active PI3Kδ and PI3Kγ dual inhibitor with IC50s of 1 nM and 16 nM, respectively. PI3Kδ/γ-IN-3 induces tumor cell apoptosis and can be used for B-cell malignancies research .
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- HY-158147
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PI3K
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Cancer
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PI3Kδ-IN-20 (compound ( S )-36) is a potent inhibitor of PI3Kδ, with the IC50 of 6.4 nM. PI3Kδ-IN-20 has oral bioactivity. PI3Kδ-IN-20 shows significant suppression of cell proliferation and remarkable induction of apoptosis both in vitro and in vivo .
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- HY-143472
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PI3K
Akt
Apoptosis
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Cancer
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PI3Kδ-IN-11 is a highly potent and selective PI3Kδ inhibitor with IC50 value of 27.5 nM. PI3Kδ-IN-11 dose-dependently blocks the activity of PI3K/Akt pathway. PI3Kδ-IN-11 can be used for researching B or T cell-related malignancies .
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- HY-146789
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PI3K
|
Cancer
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PI3Kδ/γ-IN-2 is a potent PI3Kδ and PI3Kγ dual inhibitor with IC50s of 1 nM and 4.3 nM, respectively. PI3Kδ/γ-IN-2 has favorable oral bioavailability. PI3Kδ/γ-IN-2 has potential for battling B-cell malignancies .
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- HY-149235
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PI3K
|
Inflammation/Immunology
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PI3Kδ-IN-12 (compound 13) is a PI3Kδ inhibitor (pIC50 = 5.8), with pKi values of 8.0/6.5/6.4/6.7 for PI3Kδ/γ/β/α, respectively. PI3Kδ-IN-12 can be used in the study of chronic respiratory diseases such as asthma and chronic obstructive pulmonary disease (COPD) .
|
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- HY-11080
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PI3K
mTOR
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Cancer
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PKI-179 is a potent and orally active dual PI3K/mTOR inhibitor, with IC50s of 8 nM, 24 nM, 74 nM, 77 nM, and 0.42 nM for PI3K-α, PI3K-β, PI3K-γ, PI3K-δ and mTOR, respectively. PKI-179 also exhibits activity over E545K and H1047R, with IC50s of 14 nM and 11 nM, respectively. PKI-179 shows anti-tumor activity in vivo .
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- HY-11080A
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PI3K
mTOR
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Cancer
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PKI-179 hydrochloride is a potent and orally active dual PI3K/mTOR inhibitor, with IC50s of 8 nM, 24 nM, 74 nM, 77 nM, and 0.42 nM for PI3K-α, PI3K-β, PI3K-γ, PI3K-δ and mTOR, respectively. PKI-179 hydrochloride also exhibits activity over E545K and H1047R, with IC50s of 14 nM and 11 nM, respectively. PKI-179 hydrochloride shows anti-tumor activity in vivo .
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- HY-12644
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GS-9820; CAL-120
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PI3K
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Cancer
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Acalisib is a potent and selective PI3Kδ inhibitor with an IC50 of 12.7 nM.
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- HY-12948
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PI3K
|
Cancer
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AMG319 is a potent and selective PI3Kδ kinase inhibitor with IC50 of 18 nM.
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- HY-16754
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- HY-19535
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GSK2269557
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Nemiralisib hydrochloride (GSK2269557) is a potent and highly selective PI3Kδ inhibitor with a pKi of 9.9.
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- HY-147898
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PI3K
Apoptosis
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Cancer
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PI3K-IN-33 (Compound 6e) is a highly selective PI3K inhibitor with IC50 values of 11.73, 6.09 and 11.18 μM for PI3K-α、PI3K-β and PI3K-δ , respectively. PI3K-IN-33 arrests cell cycle at G2/M phase and induces apoptosis. PI3K-IN-33 can be used in leukemia research .
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- HY-147900
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PI3K
Apoptosis
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Cancer
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PI3K-IN-35 (Compound 6l) is a highly selective PI3K inhibitor with IC50 values of 13.98, 7.22 and 10.94 μM for PI3K-α、PI3K-β and PI3K-δ, respectively. PI3K-IN-35 arrests cell cycle at G2/M phase and induces apoptosis. PI3K-IN-35 can be used in leukemia research .
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- HY-147899
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PI3K
Apoptosis
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Cancer
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PI3K-IN-34 (Compound 6g) is a highly selective PI3K inhibitor with IC50 values of 11.73, 6.09 and 11.18 μM for PI3K-α、PI3K-β and PI3K-δ , respectively. PI3K-IN-34 arrests cell cycle at G2/M phase and induces apoptosis. PI3K-IN-34 can be used in leukemia research .
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- HY-10110
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PI3K
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Cancer
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IC-87114 is a potent and selective PI3Kδ inhibitor with IC50 of 0.5 μM.
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- HY-16122
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PI3K
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Cancer
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CAL-130 Racemate is the racemate of CAL-130. CAL-130 Racemate is a PI3Kδ inhibitor.
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- HY-19535A
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GSK2269557 free base
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PI3K
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Cancer
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Nemiralisib (GSK2269557 free base) is a potent and highly selective PI3Kδ inhibitor with a pKi of 9.9.
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- HY-17635
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CDZ173
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PI3K
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Inflammation/Immunology
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Leniolisib (CDZ173) is a potent and selective PI3Kδ inhibitor. Leniolisib has the potential for immunodeficiency disorders treatment.
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- HY-132880
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PI3K
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Cancer
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GSK251 is a highly potent, highly selective, orally bioavailable inhibitor of PI3Kδ with a novel binding mode.
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- HY-17635A
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CDZ173 phosphate
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PI3K
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Inflammation/Immunology
|
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Leniolisib (CDZ173) phosphate is a potent and selective PI3Kδ inhibitor. Leniolisib phosphate has the potential for immunodeficiency disorders treatment.
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- HY-12279F
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TGR-1202 R-enantiomer; RP5264 R-enantiomer
|
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Umbralisib R-enantiomer (TGR-1202 R-enantiomer) is a PI3Kδ inhibitor, which is the less active enantiomer of TGR-1202.
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- HY-101114
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LAS191954 is a potent, selective and orally active PI3Kδ inhibitor for inflammatory diseases treatment, with an IC50 of 2.6 nM .
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- HY-162292
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PI3K
Kinesin
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Cancer
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Anticancer agent 190 (compound 3e) is an inhibitor targeting KSP (Kinesin) and PI3Kδ with activity against breast cancer .
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- HY-100694
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GS-9901 is a highly selective and orally active PI3Kδ inhibitor, with an IC50 of 1 nM. Has potential to treat rheumatoid arthritis .
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- HY-16122A
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PI3K
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Cancer
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CAL-130 is a PI3Kδ and PI3Kγ inhibitor with IC50s of 1.3 and 6.1 nM, respectively.
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- HY-16122B
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PI3K
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Cancer
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CAL-130 is a PI3Kδ and PI3Kγ inhibitor with IC50s of 1.3 and 6.1 nM, respectively.
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- HY-17645
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RP6530
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PI3K
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Cancer
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Tenalisib (RP6530) is a novel, potent, and selective PI3Kδ and PI3Kγ inhibitor with IC50 values of 25 and 33 nM, respectively.
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- HY-12340
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PI3K
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Cancer
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ETP-46321 is a potent and orally bioavailable PI3Kα and PI3Kδ inhibitor with Kiapps of 2.3 and 14.2 nM, respectively.
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- HY-12869
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PI3K
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Cancer
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AZD8835 is a potent and selective inhibitor of PI3Kα and PI3Kδ with IC50s of 6.2 and 5.7 nM, respectively.
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- HY-112439
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- HY-133029
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PI3K
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Cancer
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PI3K-IN-9 (compound 1-14) is a potent and selective PI3Kδ inhibitor with an IC50 of 8.9 nM .
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- HY-10111
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- HY-13514
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PI3K
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Cancer
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TG 100713 is an inhibitor of PI3K, with IC50s of 24, 50, 165, and 215 nM for PI3Kδ, γ, α and β isoforms respectively .
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- HY-109029
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INCB040093
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PI3K
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Cancer
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Dezapelisib (NCB040093) is a potent inhibitor of phosphatidylinositol 3-kinase δ (PI3Kδ). Dezapelisib is a promising research strategy for select R/R B-cell lymphomas .
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- HY-135827A
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MSC2360844 hemifumarate; IOA-244 hemifumarate
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PI3K
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Inflammation/Immunology
Cancer
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Roginolisib (MSC2360844) hemifumarate is a potent, orally active and selective PI3Kδ inhibitor, with an IC50 of 145 nM. Roginolisib hemifumarate shows highly selective against a panel of 278 additional kinases .
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- HY-12338
-
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PI3K
Bcr-Abl
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Cancer
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ON 146040 is a potent PI3Kα and PI3Kδ (IC50≈14 and 20 nM, respectively) inhibitor. ON 146040 also inhibits Abl1 (IC50<150 nM).
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- HY-102031
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YY-20394
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PI3K
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Inflammation/Immunology
Cancer
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Linperlisib (YY-20394) is a potent, orally bioavailable and selective inhibitor of PI3Kδ extracted from patent WO 2015055071 A1, compound 10; has an IC50 of 6.4 nM .
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- HY-135827
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MSC2360844; IOA-244
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PI3K
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Inflammation/Immunology
Cancer
|
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Roginolisib (MSC2360844; IOA-244) is a potent, orally active and selective PI3Kδ inhibitor, with an IC50 of 145 nM. Roginolisib shows highly selective against a panel of 278 additional kinases .
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- HY-112172
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RP6530 R Enantiomer
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PI3K
|
Cancer
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Tenalisib R Enantiomer (RP6530 R Enantiomer) is an R enantiomer of Tenalisib. Tenalisib is a potent and selective PI3Kδ and PI3Kγ inhibitor with IC50 values of 25 and 33 nM, respectively .
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- HY-10549
-
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PI3K
|
Cancer
|
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PI3Kγ inhibitor 1 is a PI3Kδ and PI3Kγ inhibitor extracted from patent WO2014004470A1, Compound 168 in Table 4, has IC50s of <100 nM.
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- HY-12517
-
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PI3K
|
Inflammation/Immunology
|
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GNE-293 is a potent and selective PI3Kδ inhibitor (IC50 = 4.38 nM). GNE-293 has favorable pharmacokinetic properties. GNE-293 can be used for research of asthma, rheumatoid arthritis, and other inflammatory disorders .
|
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- HY-15280
-
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PI3K
|
Inflammation/Immunology
|
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GSK2292767 is a potent and selective inhibitor of PI3Kδ, with a pIC50 of 10.1. GSK2292767 showing greater than 500-fold selective over the other PI3K isoforms. GSK2292767 can be used for the research of respiratory disease .
|
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- HY-50847
-
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PI3K
Autophagy
|
Cancer
|
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ZSTK474 is an ATP-competitive pan-class I PI3K inhibitor with IC50s of 16 nM, 44 nM, 4.6 nM and 49 nM for PΙ3Κα, PI3Kβ, PI3Kδ and PI3Kγ, respectively.
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- HY-128582
-
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PI3K
HDAC
|
Cancer
|
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PI3K/HDAC-IN-1 is a potent dual inhibitor of PI3K/HDAC, potently inhibits PI3Kδ and HDAC1 with IC50s of 8.1 nM and 1.4 nM, respectively .
|
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- HY-13333
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BAG 956
|
PI3K
|
Cancer
|
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NVP-BAG956 is an ATP-competitive PI3K inhibitor with IC50s of 34, 56, 112 and 444 nM for PI3Kδ, PI3Kα, PI3Kγ and PI3Kβ, respectively.
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- HY-18085
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- HY-147792
-
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PI3K
Apoptosis
|
Cancer
|
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WNY1613 is a potent and selective PI3Kδ inhibitor with piperazinone-containing purine scaffold. WNY1613 induces cancer cell apoptosis and inhibits the phosphorylation of PI3K downstream components in NHL cell lines. WNY1613 exhibits anti-NHL activity in vitro and in vivo .
|
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- HY-18085A
-
-
- HY-19962
-
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GDC-0084
|
|
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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 .
|
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- HY-16526
-
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XL-147; SAR245408
|
PI3K
|
Cancer
|
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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.
|
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- HY-N0146
-
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PI3K
Apoptosis
|
Inflammation/Immunology
Cancer
|
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Quercetin dihydrate, a natural flavonoid, is a stimulator of recombinant SIRT1 and a PI3K inhibitor with IC50s of 2.4 μM, 3.0 μM and 5.4 μM for PI3K γ, PI3K δ and PI3K β, respectively .
|
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- HY-13898
-
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GDC-0032; RG-7604
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PI3K
|
Cancer
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Taselisib (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.
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- HY-19798
-
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PI4K
PI3K
|
Cancer
|
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PI4KIIIbeta-IN-9 is a potent PI4KIIIβ inhibitor with an IC50 of 7 nM. PI4KIIIbeta-IN-9 also inhibits PI3Kδ and PI3Kγ with IC50s of 152 nM and 1046 nM, respectively.
|
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- HY-109068
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INCB050465; IBI-376
|
PI3K
|
Cancer
|
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Parsaclisib (INCB050465) is a potent, selective and orally active inhibitor of PI3Kδ, with an IC50 of 1 nM at 1 mM ATP. Parsaclisib shows approximately 20000-fold selectivity over other PI3K class I isoforms. Parsaclisib can be used for the research of relapsed or refractory B-cell malignancies [3].
|
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- HY-112443
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- HY-109068A
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INCB050465 hydrochloride; IBI-376 hydrochloride
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PI3K
|
Cancer
|
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Parsaclisib hydrochloride (INCB050465 hydrochloride) is a potent, selective and orally active inhibitor of PI3Kδ, with an IC50 of 1 nM at 1 mM ATP. Parsaclisib hydrochloride shows approximately 20000-fold selectivity over other PI3K class I isoforms. Parsaclisib hydrochloride can be used for the research of relapsed or refractory B-cell malignancies [3].
|
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- HY-147419
-
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PI3K
|
Cancer
|
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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 .
|
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- HY-146159
-
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PI3K
HDAC
|
Cancer
|
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PI3K/HDAC-IN-2 is a potent dual PI3K/HDAC inhibitor with IC50s of 226 nM, 279 nM, 467 nM, 29 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ, respectively, and IC50s of 1.3 nM, 3.4 nM, 972 nM, 17 nM, 12 nM for HDAC1, HDAC2, HDC4, HDAC6, HDAC8, respectively. PI3K/HDAC-IN-2 exhibits PI3Kδ and class I and IIb HDAC selectivity. PI3K/HDAC-IN-2 has remarkable anticancer effects .
|
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- 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.
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- HY-13431
-
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DNA-PK
PI3K
mTOR
|
Cancer
|
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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 .
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- HY-12330
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AZD8186
5 Publications Verification
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PI3K
|
Cancer
|
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AZD8186 is a PI3K inhibitor, which potently inhibits PI3Kβ (IC50=4 nM) and PI3Kδ (IC5050=12 nM) with selectivity over PI3Kα (IC50=35 nM) and PI3Kγ (IC50=675 nM).
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- HY-18085S1
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-
- HY-18085S
-
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PI3K
Autophagy
Mitophagy
Apoptosis
|
Cancer
|
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Quercetin-d5 is a deuterium labeled Quercetin. Quercetin, a natural flavonoid, is a stimulator of recombinant SIRT1 and also a PI3K inhibitor with IC50 of 2.4 μM, 3.0 μM and 5.4 μM for PI3K γ, PI3K δ and PI3K β, respectively[1].
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- HY-18085S2
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-
- HY-143404
-
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PI3K
|
Cancer
|
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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 .
|
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- HY-10683
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PKI-402
5 Publications Verification
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PI3K
mTOR
|
Cancer
|
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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).
|
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- HY-16585
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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.
|
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- HY-12279
-
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TGR-1202; RP5264
|
PI3K
Casein Kinase
|
Cancer
|
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Umbralisib (TGR-1202) is an orally active, potent and selective dual PI3Kδ and casein kinase-1-ε (CK1ε) inhibitor, with EC50 of 22.2 nM and 6.0 μM, respectively. Umbralisib exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib can be used for haematological malignancies reseach [3] .
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- HY-12279C
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TGR-1202 hydrochloride; RP5264 hydrochloride
|
PI3K
Casein Kinase
|
Cancer
|
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Umbralisib (TGR-1202) hydrochloride is an orally active, potent and selective dual PI3Kδ and casein kinase-1-ε (CK1ε) inhibitor, with EC50 of 22.2 nM and 6.0 μM, respectively. Umbralisib hydrochloride exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib hydrochloride can be used for haematological malignancies reseach [3] .
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-
- HY-12279A
-
|
TGR-1202 tosylate; RP5264 tosylate
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PI3K
Casein Kinase
|
Cancer
|
|
Umbralisib (TGR-1202) tosylate is an orally active, potent and selective dual PI3Kδ and casein kinase-1-ε (CK1ε) inhibitor, with EC50 of 22.2 nM and 6.0 μM, respectively. Umbralisib tosylate exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib tosylate can be used for haematological malignancies reseach [3] .
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-
- HY-155996
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PI3K
Apoptosis
|
Cancer
|
|
FD2157 is a photosensitive PI3K inhibitor, with IC50s of 43 nM, 83 nM, 84 nM, 14 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ respectively. FD2157 potently inhibits cancer cell proliferation and induces cell apoptosis when exposed to 365 nm UV light .
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-
- HY-12279B
-
|
TGR-1202 sulfate; RP-5264 sulfate
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PI3K
Casein Kinase
|
Cancer
|
|
Umbralisib (TGR-1202) sulfate is an orally active, potent and selective dual PI3Kδ and casein kinase-1-ε (CK1ε) inhibitor, with EC50 of 22.2 nM and 6.0 μM, respectively. Umbralisib sulfate exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib sulfate can be used for haematological malignancies reseach [3] .
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-
- HY-12868
-
|
PQR309
|
PI3K
mTOR
|
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, PI3Kδ, PI3Kβ, PI3Kγ and mTOR, respectively. Bimiralisib is an mTORC1 and mTORC2 inhibitor.
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-
- HY-13531
-
|
|
PI3K
|
Cancer
|
|
AS-604850 is a potent, selective and ATP-competitive PI3Kγ inhibitor with an IC50 value of 0.25 μM and a Ki value of 0.18 μM. AS-604850 shows isoform selective inhibitor of PI3Kγ with over 30-fold selectivity for PI3Kδ and β, and 18-fold selectivity over PI3Kα, respectively .
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-
- HY-118521
-
|
|
PI3K
|
Inflammation/Immunology
|
|
AS-041164 is a potent, selective and orally active PI3Kγ isoform inhibitor with an IC50 of 70 nM. AS-041164 shows less activity against PI3Kα, PI3Kβ, and PI3Kδ (IC50s of 240 nM, 1.45 μM, and 1.70 μM, respectively). AS-041164 has anti-inflammatory effects .
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-
- HY-139810
-
|
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PI3K
|
Others
|
|
ETP-47037 is a potent and inhibitor of PI3Kα isoform with an IC50 value of 0.99 nM. ETP-47037 also inhibits the PI3Kβ, PI3Kδ, and PI3Kγ isoforms, with IC50 values of 49.2, 7.13, and 49.1 nM, respectively. ETP-47037 has the potential for the research of chemical modulation of telomere protection .
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-
- HY-147285
-
|
|
mTOR
PI3K
|
Neurological Disease
|
|
PI3K/mTOR Inhibitor-9 (Compound 1) is a potent mTOR and PI3K inhibitor with IC50 values of 38 nM, 6.6 μM, 6.6 μM and 0.8 μM against mTOR (phospho-S6 cellular assay), PI3Kα, PI3Kγ and PI3Kδ, respectively .
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-
- 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 .
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-
- 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 .
|
-
- 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 .
|
-
- HY-10108
-
LY294002
Maximum Cited Publications
705 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, PI3Kδ and PI3Kβ, 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].
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-
- HY-13522
-
|
CUDC-907
|
PI3K
HDAC
Apoptosis
|
Cancer
|
|
Fimepinostat (CUDC-907) potently inhibits class I PI3Ks as well as classes I and II HDAC enzymes with an IC50 of 19/54/39 nM and 1.7/5.0/1.8/2.8 nM for PI3Kα/PI3Kβ/PI3Kδ and HDAC1/HDAC2/HDAC3/HDAC10 , respectively.
|
-
- HY-112602
-
|
|
PI3K
mTOR
|
Cancer
|
|
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 .
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-
- HY-15346
-
|
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, PI3Kδ, PI3Kβ and PI3Kγ, respectively. Copanlisib has more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR. Copanlisib has superior antitumor activity .
|
-
- HY-12513
-
|
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 .
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-
- HY-112614
-
|
|
ATM/ATR
|
Cancer
|
|
ATM Inhibitor-1 is a highly potent, selective and orally active ATM inhibitor, with an IC50 of 0.7 nM, shows weak activity against mTOR (IC50, 21 μM), DNAPK (IC50, 2.8 μM), PI3Kα (IC50, 3.8 μM), PI3Kβ (IC50, 10.3 μM), PI3Kγ (IC50, 3 μM) and PI3Kδ (IC50, 0.73 μM). ATM Inhibitor-1 exhibits anti-tumor activity .
|
-
- HY-15346A
-
|
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, PI3Kδ, PI3Kβ and PI3Kγ, 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 .
|
-
- 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, PI3Kδ, PI3Kβ and PI3Kγ, 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 .
|
-
- HY-144806
-
|
|
PI3K
Akt
Apoptosis
|
Cancer
|
|
PI3K/AKT-IN-1 is an effective PI3K/AKT dual inhibitor (IC50 of 6.99, 4.01 and 3.36 μM for PI3Kγ, PI3Kδ and AKT, respectively). PI3K/AKT-IN-1 has anticancer activity and acts by inhibiting PI3K/AKT axis and inducing caspase 3 dependent apoptosis .
|
-
- HY-153894
-
|
|
CDK
Epigenetic Reader Domain
PI3K
|
Cancer
|
|
SRX3177 is a triple inhibitor of CDK4/6, PI3K, and BRD4, with IC50s of 33 nM (BRD4 BD1), 89 nM (BRD4 BD2), 79 nM (PI3Kα), 83 nM (PI3Kδ), 3.18 μM (PI3Kγ), <2.5 nM (CDK4), 3.3 nM (CDK6), respectively. SRX3177 exerts broad cytotoxic activity against cancer cells, but acts friendly with normal epithelial cells .
|
-
- HY-131910
-
|
|
PI3K
Cytochrome P450
|
Inflammation/Immunology
|
|
IHMT-PI3Kδ-372 is a potent and selective PI3Kδ inhibitor with an IC50 of 14 nM. IHMT-PI3Kδ-372 shows high selectivity over other class I PI3Ks (56∼83 fold) and other protein kinases. IHMT-PI3Kδ-372 can be uesd for chronic obstructive pulmonary disease (COPD) research .
|
-
- HY-132231
-
|
|
PI3K
Apoptosis
|
Cancer
|
|
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 .
|
-
- HY-144692
-
|
|
MEK
PI3K
PERK
|
Cancer
|
|
MEK/PI3K-IN-1 (compound 6r) is a potent MEK/PI3K inhibitor, with IC50 values of 124 nM (MEK1), 130 nM (PI3Kα), and 236 nM (PI3Kδ), respectively. MEK/PI3K-IN-1 suppresses pAKT and pERK1/2 levels. MEK/PI3K-IN-1 shows anti-proliferative activity against tumor cell lines .
|
-
- HY-144693
-
|
|
MEK
PI3K
PERK
|
Cancer
|
|
MEK/PI3K-IN-2 (compound 6s) is a potent MEK/PI3K inhibitor, with IC50 values of 352 nM (MEK1), 107 nM (PI3Kα), and 137 nM (PI3Kδ), respectively. MEK/PI3K-IN-2 suppresses pAKT and pERK1/2 levels. MEK/PI3K-IN-2 shows anti-proliferative activity against tumor cell lines .
|
-
- HY-150618
-
|
|
PI3K
Apoptosis
|
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 .
|
-
- 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 .
|
-
- HY-133124
-
|
|
PARP
PI3K
Apoptosis
|
Cancer
|
|
PARP/PI3K-IN-1 (compound 15) is a potent PARP/PI3K inhibitor with pIC50 values of 8.22, 8.44, 8.25, 6.54, 8.13, 6.08 for PARP-1, PARP-2, PI3Kα, PI3Kβ, PI3Kδ, and PI3Kγ, respectively. PARP/PI3K-IN-1 is a highly effective anticancer compound targeted against a wide range of oncologic diseases .
|
-
- 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 .
|
-
- 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 .
|
-
- HY-151622
-
|
|
PI3K
mTOR
|
Cancer
|
|
PI3K/mTOR Inhibitor-11 is an orally active PI3K/mTOR inhibitor (IC50: 3.5, 4.6, and 21.3 nM for PI3Kα, PI3Kδ, and mTOR). PI3K/mTOR Inhibitor-11 regulates the PI3K/AKT/mTOR signaling pathway by inhibiting the phosphorylation of AKT and S6 proteins. PI3K/mTOR Inhibitor-11 can be used in the research of cancers .
|
-
- HY-153703
-
|
|
PI3K
|
Cancer
|
|
PI3Kγ inhibitor 7 (compound 2) is a potent and orally active PI3Kγ inhibitor with IC50 values of 4768, 878.1, 3.42, 355.2 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ, respectively. PI3Kγ inhibitor 7 shows antitumor activity . PI3Kγ inhibitor 7 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-149521
-
|
|
PI3K
|
Cancer
|
|
PI3K-IN-47 (Compound 27) is a bivalent PI3K inhibitor (IC50: 0.44 nM for PI3Kα, 7.18 nM, 13.92 nM, 22.83 nM for PI3Kβ, PI3Kγ, PI3Kδ). PI3K-IN-47 induces cell cycle arrest in G1 phase, inhibits colony formation and cell migration. PI3K-IN-47 inhibits tumor growth in HGC-27 xenograft mice .
|
-
- HY-149493
-
|
|
PI3K
|
Inflammation/Immunology
Cancer
|
|
IHMT-PI3K-455 (Compound 15u) is a potent, selective, orally active PI3Kγ/δ dual inhibitor with IC50s of 7.1 nM and 0.57 nM for PI3Kγ and PI3Kδ, respectively. IHMT-PI3K-455 suppresses the AKT phosphorylation. IHMT-PI3K-455 inhibits tumor growth by recruiting and activating more CD8 + killing T cells.IHMT-PI3K-455 is used in cancer research .
|
-
- HY-155180
-
|
|
PI3K
|
Cancer
|
|
FD2056 is a potent and orally active PI3K inhibitor. FD2056 inhibits PI3Kα/PI3Kβ/PI3Kγ/PI3Kδ with IC50s of 0.30, 0.80, 1.10, 0.42 nM. FD2056 also inhibits CDK2-CyclinA2 and CDK4-CyclinD3 with IC50 of 115.95 and 2782.15 nM. FD2056 inhibits breast cancer cell proliferation with IC50s of 1.06, 0.04, 1.40 μM for MDA-MB-231, MDA-MB-468, MCF-7 cells. FD2056 also induces cancer apoptosis and inhibits tumor growth .
|
-
- HY-112608
-
|
|
PI3K
|
Cancer
|
|
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 .
|
-
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-18085S1
-
|
|
|
Quercetin-d3 is the deuterium labeled Quercetin. Quercetin, a natural flavonoid, is a stimulator of recombinant SIRT1 and also a PI3K inhibitor with IC50 of 2.4 μM, 3.0 μM and 5.4 μM for PI3K γ, PI3K δ and PI3K β, respectively[1].
|
-
-
- HY-18085S
-
|
|
|
Quercetin-d5 is a deuterium labeled Quercetin. Quercetin, a natural flavonoid, is a stimulator of recombinant SIRT1 and also a PI3K inhibitor with IC50 of 2.4 μM, 3.0 μM and 5.4 μM for PI3K γ, PI3K δ and PI3K β, respectively[1].
|
-
-
- HY-18085S2
-
|
|
|
Quercetin- 13C3 is the 13C-labeled Quercetin. Quercetin, a natural flavonoid, is a stimulator of recombinant SIRT1 and also a PI3K inhibitor with IC50 of 2.4 μM, 3.0 μM and 5.4 μM for PI3K γ, PI3K δ and PI3K β, respectively[1].
|
-
| Cat. No. |
Product Name |
Application |
Reactivity |
-
- HY-P81872
-
|
PIK3CD; Phosphatidylinositol 4; 5-bisphosphate 3-kinase catalytic subunit delta isoform; PI3-kinase subunit delta; PI3K-delta; PI3Kdelta; PtdIns-3-kinase subunit delta; Phosphatidylinositol 4; 5-bisphosphate 3-kinase 110 kDa catalytic subunit delta; PtdIns-3-kinase subunit p110-delta; p110delta
|
WB, ICC/IF
|
Human, Mouse, Rat |
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