Search Result
| Isoforms Recommended: |
PI3Kδ
|
Results for "
PI3Kδ
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
5
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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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-109068
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INCB050465; IBI-376
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PI3K
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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-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-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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AMG319
1 Publications Verification
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PI3K
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Cancer
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AMG319 is a potent and selective PI3Kδ kinase inhibitor with IC50 of 18 nM.
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- HY-10111
-
-
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- HY-50847
-
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PI3K
Autophagy
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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-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-109198
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ME-401; PWT-143
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PI3K
Akt
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Cancer
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Zandelisib (ME-401) is a selective, orally active, non-covalent inhibitor of PI3Kδ. Zandelisib can sustainably inhibit AKT phosphorylation and downstream signaling pathways. Zandelisib can be used in the study of malignancies such as relapsed/refractory B-cell lymphoma .
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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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-
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- HY-19535A
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GSK2269557 free base
|
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-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-16754
-
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- HY-176239
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PROTACs
PI3K
Akt
Apoptosis
Autophagy
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Cancer
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PROTAC PI3Kδ degrader-1 is a Lysine-targeted covalent PI3Kδ PROTAC degrader with a DC50 of 3.98 nM. PROTAC PI3Kδ degrader-1 has a potent antiproliferative activity and selective PI3Kδ inhibition (IC50: 8 nM). PROTAC PI3Kδ degrader-1 also significantly degrades p-AKT, induces cell cycle arrest in G1 phase and prompts cell apoptosis and autophagy. PROTAC PI3Kδ degrader-1 effectively inhibits the tumor growth in SU-DHL-6 xenograft mice model . Pink: PI3Kδ ligand (HY-169983); Blue: VHL ligase ligand (HY-112078); Black: linker (HY-W013381)
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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-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-15280
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PI3K
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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-115870
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PI3K
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Inflammation/Immunology
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AZD8154 is a selective PI3Kγδ dual inhibitor. AZD8154 can suppress PI3Kγ and PI3Kδ signaling pathway activation. AZD8154 can be used for the researches of inflammation and immunology, such as asthma .
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- HY-131910A
-
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PI3K
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Inflammation/Immunology
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(R)-IHMT-PI3Kδ-372 (R-18) is a potent and selective PI3Kδ inhibitor with an IC50 of 19 nM. (R)-IHMT-PI3Kδ-372 (R-18) can be used in chronic obstructive pulmonary disease (COPD) research .
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- HY-143404
-
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PI3K
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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-17635A
-
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CDZ173 phosphate
|
PI3K
|
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-101921
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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-147419
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PI3K
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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-128333
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PI3K
mTOR
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Cancer
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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 .
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- HY-10812
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PI3K
mTOR
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Cancer
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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 .
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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-131910
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PI3K
Cytochrome P450
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Inflammation/Immunology
|
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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 .
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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-W040417
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PI3K
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Others
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Boc-L-cyclobutylglycine is a Boc-protected L-cyclic amino acid and synthetic intermediate in the preparation of purinyl quinazolinone PI3Kδ inhibitors .
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- HY-100694
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PI3K
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Inflammation/Immunology
|
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GS-9901 is a highly selective and orally active PI3Kδ inhibitor with an IC50 of 1 nM. GS-9901 has ≥100 fold selectivity for PI3Kα (IC50 of 750 nM), PI3Kβ (IC50 of 100 nM) and PI3Kγ (IC50 of 190 nM). GS-9901 can be used for the study of rheumatoid arthritis .
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- HY-125376
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PI3K
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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-143403
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PI3K
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Cancer
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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 .
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- HY-123849
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PI3K
mTOR
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Cancer
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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-131345A
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PI3K
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Cancer
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(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 .
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- HY-17635S
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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-175369
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PI3K
Akt
PD-1/PD-L1
Interleukin Related
CD3
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Inflammation/Immunology
Cancer
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PI3Kδ-IN-25 is an orally active selective PI3Kδ inhibitor (IC50 = 2.1 nM). PI3Kδ-IN-25 has IC50s of 272, 285, and 1171 nM for PI3Kα, PI3Kγ, and PI3Kβ, respectively. PI3Kδ-IN-25 inhibits AKT Ser473 phosphorylation, suppresses Treg cell proliferation, and downregulates PD-L1 expression in B16F10 cells. PI3Kδ-IN-25 exhibits anticancer effects in B16F10 melanoma and Lewis lung cancer mouse models by reducing tumor-infiltrating Treg cells and enhancing immune responses. PI3Kδ-IN-25 is potentially useful in the study of melanoma, lung cancer, and other cancers .
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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-174396
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PI3K
HDAC
Bcl-2 Family
Caspase
Reactive Oxygen Species (ROS)
Apoptosis
Histone Methyltransferase
Microtubule/Tubulin
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Cancer
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PI3Kδ/HDAC6-IN-1 (Compound 22E) is an orally active and dual inhibitor of PI3Kδ and HDAC6 with IC50 values of 2.4 nM and 6.2 nM, respectively. PI3Kδ/HDAC6-IN-1 exhibits potent antiproliferative effects on non-Hodgkin lymphoma (NHL) cells and possesses in vivo antitumor activity without significant toxicity. PI3Kδ/HDAC6-IN-1 arrests the cell cycle at the G0/G1 phase and induces apoptosis. PI3Kδ/HDAC6-IN-1 blocks the PI3K/AKT/mTOR signaling pathway and increases the acetylation levels of α-tubulin and histone H3 .
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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-134472
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PI3K
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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-155232
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PI3K
Apoptosis
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Cancer
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PI3Kδ-IN-16 is a potent and selective PI3Kδ inhibitor with an IC50 value of 0.9 nM. PI3Kδ-IN-16 has a strong anti-proliferative effect on SU-DHL-6 cells, causing cell cycle arrest and inducing apoptosis. PI3Kδ-IN-16 tightly bins to PI3Kδ protein with a planar-shaped conformation. The kinase activity of PI3Kδ-IN-16 which is ~378-fold over PI3Kα, 412-fold over PI3Kβ, and 10-fold over PI3Kγ. PI3Kδ-IN-16 can be used for the study of hematologic malignancies .
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- HY-109068A
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INCB050465 hydrochloride; IBI-376 hydrochloride
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PI3K
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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-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-178445
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PI3K
SARS-CoV
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Infection
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PI3Kδ-IN-27 is an PI3Kδ inhibitor with an IC50 of 355.3 nM. PI3Kδ-IN-27 exhibits anti-SARS-CoV-2 activity. PI3Kδ-IN-27 can be used for the research of infection, such as COVID-19 .
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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-12482
-
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PI3K
Apoptosis
PDK-1
MEK
Akt
ERK
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Cancer
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X-370 is a PI3Kδ inhibitor (IC50 = 7 nM). X-370 inhibits the survival of leukemia cells, inducing G1 arrest and apoptosis. X-370 blocks PDK1 binding and phosphorylation of MEK1/2, eliminating Akt and Erk1/2 signaling. X-370 can be used in research on B-cell acute lymphoblastic leukemia (B-ALL) .
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- HY-175734
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PI3K
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Inflammation/Immunology
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PI3Kδ-IN-26 (Compound 58) is a selective and orally active PI3Kδ inhibitor with an IC50 of 14 nM. PI3Kδ-IN-26 significantly attenuates the inflammatory responses in house dust mite (HDM) induced chronic asthma mouse models. PI3Kδ-IN-26 can be used for inflammatory, autoimmune and hyperproliferative diseases research .
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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-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-169983
-
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PI3K
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Cancer
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PI3Kδ-IN-23 (compound A11) is a potent inhibitor of PI3Kδ, with the IC50 of 0.27 nM. PI3Kδ-IN-23 bounds to PI3Kδ by covalent-bonding interactions with Lys779. PI3Kδ-IN-23 plays an important role in cancer research .
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- HY-112439
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- HY-40029
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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-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-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-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-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-149634
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PI3K
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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-172130
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PI3K
Epigenetic Reader Domain
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Cancer
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PI3Kδ/BET-IN-1 (compound 10b) shows excellent and balanced activities against PI3Kδ (IC50 = 112 nM) and BRD4-BD1 (IC50 = 19 nM) and exhibits strong antiproliferative activities in DLBCL cells .
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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-162647
-
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PI3K
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Inflammation/Immunology
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PI3Kδ-IN-22 (Compound 26) is a selective inhibitor for PI3Kδ with pKi of 9.3. PI3Kδ-IN-22 inhibits PI3Kδ-AKT signaling pathway in THP-1 cells, with pIC50 of 9.4. PI3Kδ-IN-22 exhibits good pharmacokinetic characters in rats .
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- HY-149235
-
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PI3K
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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-146789
-
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PI3K
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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-158688
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PI3K
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Inflammation/Immunology
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PI3Kδ-IN-21 (Compound 31) is a selective inhibitor for phosphoinositide 3-kinases δ (PI3Kδ), with an IC50 of 13.6 nM. PI3Kδ-IN-21 inhibits proliferation and differentation of T cells through PI3K/AKT/mTOR signaling pathway. PI3Kδ-IN-21 exhibits good pharmacokinetic characters in rat model, and attenuates the experimental autoimmune encephalomyelitis in myelin oligodendrocyte glycoprotein (MOG)-induced EAE model .
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- HY-175002
-
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PI3K
Akt
Apoptosis
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Cancer
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PI3Kδ-IN-24 is a selective PI3Kδ inhibitor (IC50 = 0.1 nM). PI3Kδ-IN-24 exhibits significant antiproliferative effects against PI3Kδ-overexpressing cancer cell lines. PI3Kδ-IN-24 reduces p-AKT levels and induces cell cycle arrest and apoptosis in tumor cells. PI3Kδ-IN-24 is useful in cancer research, such as diffuse large B-cell lymphoma (DLBCL) .
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- HY-147792
-
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PI3K
Apoptosis
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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-113572
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PI3K
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Cancer
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PX-866-17OH is the metabolite of PX-866 (Sonolisib, HY-N6775) and a pan-isoform inhibitor of PI3K with IC50s of 14, 57, 131, and 148 nM against PI3Kα, PI3Kβ, PI3K , and PI3Kδ, respectively .
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- HY-101798
-
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PI3K
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Cancer
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MDVN1003 is a Bruton's tyrosine kinase (BTK) and phosphatidylinositol-3-kinase delta (PI3Kδ) dual inhibitor which prevents the activation of B cells and inhibits the phosphorylation of protein kinase B (AKT) and extracellular signal-regulated kinase 1/2 (ERK 1/2). MDVN1003 can be used for non-Hodgkin’s lymphoma (NHL) research .
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- HY-19535B
-
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GSK2269557 succinate
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PI3K
|
Cancer
|
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Nemiralisib Succinate is a potent and highly selective PI3Kδ inhibitor with a pKi of 9.9.
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- HY-108418A
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- HY-19535
-
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GSK2269557
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PI3K
|
Cancer
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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-123862
-
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PI3K
Lipase
G Protein-coupled Receptor Kinase (GRK)
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Inflammation/Immunology
|
|
LAS195319 is an orally active and potent inhibitor against PI3Kδ with an IC50 value of 0.5 nM. LAS195319 is also a highly selective inhibitor against an extensive panel of proteins, lipid kinases and GPCRs. LAS195319 causes an inhibition of neutrophil and eosinophil infiltration. LAS195319 is promising for research of respiratory diseases such as asthma and chronic obstructive pulmonary disease (COPD) .
|
-
- HY-132880
-
|
|
PI3K
|
Cancer
|
|
GSK251 is a highly potent, highly selective, orally bioavailable inhibitor of PI3Kδ with a novel binding mode.
|
-
- HY-12279F
-
|
TGR-1202 R-enantiomer; RP5264 R-enantiomer
|
PI3K
|
Cancer
|
|
Umbralisib R-enantiomer (TGR-1202 R-enantiomer) is a PI3Kδ inhibitor, which is the less active enantiomer of TGR-1202.
|
-
- HY-101114
-
|
|
PI3K
|
Inflammation/Immunology
|
|
LAS191954 is a potent, selective and orally active PI3Kδ inhibitor for inflammatory diseases treatment, with an IC50 of 2.6 nM .
|
-
- HY-106006
-
|
|
PI3K
|
Others
Inflammation/Immunology
|
|
RV-1729 is an inhibitor of the phosphatidylinositol 3-kinase-δ (PI3Kδ). RV-1729 identifies inhibition of the PI3K isotype by quantifying the release of phosphatidylinositol 3,4, 5-triphosphate (PIP3) (IC50=12 nM), showing twice the selectivity for PI3Kδ relative to PI3Kγ. RV-1729 is also 16 times more selective to PI3Kα. RV-1729 regulates immune and inflammatory responses by inhibiting PI3Kδ. RV-1729 can be used in studies of asthma and chronic obstructive pulmonary disease (COPD) .
|
-
- HY-162292
-
|
|
PI3K
Kinesin
|
Cancer
|
|
Anticancer agent 190 (compound 3e) is an inhibitor targeting KSP (Kinesin) and PI3Kδ with activity against breast cancer .
|
-
- HY-162878
-
|
|
PI3K
|
Inflammation/Immunology
|
|
CHF-6523 is an orally active PI3Kδ inhibitor that can be used in research related to chronic obstructive pulmonary disease (COPD) .
|
-
- HY-16122B
-
|
|
PI3K
|
Cancer
|
|
CAL-130 is a PI3Kδ and PI3Kγ inhibitor with IC50s of 1.3 and 6.1 nM, respectively.
|
-
- HY-123790
-
|
|
PI3K
|
Inflammation/Immunology
|
|
AS2541019 is a PI3Kδ (p110δ) inhibitor. AS2541019 inhibits B cell activation and proliferation, and suppresses xenograft antibody production .
|
-
- HY-133029
-
|
|
PI3K
|
Cancer
|
|
PI3K-IN-9 (compound 1-14) is a potent and selective PI3Kδ inhibitor with an IC50 of 8.9 nM .
|
-
- HY-19535AR
-
|
GSK2269557 free base (Standard)
|
PI3K
Reference Standards
|
Cancer
|
|
Nemiralisib (Standard) is the analytical standard of Nemiralisib. This product is intended for research and analytical applications. Nemiralisib (GSK2269557 free base) is a potent and highly selective PI3Kδ inhibitor with a pKi of 9.9.
|
-
- HY-135827A
-
|
MSC2360844 hemifumarate; IOA-244 hemifumarate
|
PI3K
|
Inflammation/Immunology
Cancer
|
|
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 .
|
-
- HY-112172
-
|
RP6530 R Enantiomer
|
PI3K
|
Cancer
|
|
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 .
|
-
- HY-10110R
-
|
|
Reference Standards
PI3K
|
Cancer
|
|
IC-87114 (Standard) is the analytical standard of IC-87114. This product is intended for research and analytical applications. IC-87114 is a potent and selective PI3Kδ inhibitor with IC50 of 0.5 μM.
|
-
- HY-10549
-
|
|
PI3K
|
Cancer
|
|
PI3Kγ inhibitor 1 is a PI3Kδ and PI3Kγ inhibitor extracted from patent WO2014004470A1, Compound 168 in Table 4, has IC50s of <100 nM.
|
-
- HY-12517
-
|
|
PI3K
|
Inflammation/Immunology
|
|
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 .
|
-
- HY-109198A
-
|
ME-401 hydrochloride; PWT-143 hydrochloride
|
PI3K
Akt
|
Cancer
|
|
Zandelisib (ME-401) hydrochloride is a selective, orally active, non-covalent inhibitor of PI3Kδ. Zandelisib hydrochloride can sustainably inhibit AKT phosphorylation and downstream signaling pathways. Zandelisib hydrochloride can be used in the study of malignancies such as relapsed/refractory B-cell lymphoma .
|
-
- HY-120135
-
|
|
PI3K
|
Cancer
|
|
LTURM 36 (20i) is a PI3K inhibitor, with IC50 values of 0.64 μM and 5.0 μM for PI3Kδ and PI3Kβ, respectively. LTURM 36 can be used in anticancer research .
|
-
- HY-101921R
-
|
|
Reference Standards
PI3K
|
Inflammation/Immunology
|
|
PI3Kδ-IN-1 (Standard) is the analytical standard of PI3Kδ-IN-1 (HY-101921). This product is intended for research and analytical applications. PI3Kδ-IN-1 is a potent, selective, and efficacious PI3Kδ inhibitor with an IC50 of 1.7 nM.
|
-
- HY-120116
-
|
|
PI3K
Akt
|
Inflammation/Immunology
|
|
AM-8508 is an orally bioactive PI3Kδ inhibitor with an IC50 of 0.016 μM. AM-8508 selectively inhibits PI3Kδ, thereby blocking AKT phosphorylation mediated by the B cell receptor. AM-8508 suppresses the formation of antigen-specific IgG and IgM in rats immunized with keyhole limpet hemocyanin. AM-8508 can be used for the research of inflammatory diseases .
|
-
- HY-109068AR
-
|
INCB050465 hydrochloride (Standard); IBI-376 hydrochloride (Standard)
|
Reference Standards
PI3K
|
Cancer
|
|
Parsaclisib hydrochloride (Standard) is the analytical standard of Parsaclisib (hydrochloride) (HY-109068A). This product is intended for research and analytical applications. 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].
|
-
- HY-109068R
-
|
INCB050465 (Standard); IBI-376 (Standard)
|
Reference Standards
PI3K
|
Cancer
|
|
Parsaclisib (Standard) is the analytical standard of Parsaclisib (HY-109068). This product is intended for research and analytical applications. 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].
|
-
- HY-182693
-
|
|
PI3K
IFNAR
Reactive Oxygen Species (ROS)
Interleukin Related
|
Inflammation/Immunology
|
|
CPL302-253 is a PI3Kδ inhibitor with an IC50 of 12.20 nM and a human Ka of 0.85 nM. CPL302-253 functionally regulates PI3Kδ activity, blocks the production of IFNγ, IL-33 and ROS in immune cells, and affects immune function. CPL302-253 blocks the progression of asthma-inducing inflammatory responses in a mouse model of asthma. CPL302-253 can be used for research related to asthma .
|
-
- HY-16754R
-
|
UCB5857 (Standard)
|
PI3K
Reference Standards
|
Inflammation/Immunology
|
|
Seletalisib (Standard) is the analytical standard of Seletalisib. This product is intended for research and analytical applications. Seletalisib (UCB5857) is potent and selective PI3Kδ inhibitor with an IC50 of 12 nM.
|
-
- HY-118903
-
|
|
PI3K
|
Cancer
|
|
PIK-124 is a thiazolidinone-based PI3Kγ-biased PI3K inhibitor, with an IC50 of 3 nM against PI3Kγ. PIK-124 exhibits cross-reactivity with PI3Kα (IC50 = 23 nM), PI3Kδ (IC50 = 340 nM), PI3KC2α (IC50 = 140 nM) and PI3KC2β (IC50 = 370 nM). PIK-124 is applicable to breast cancer-related research .
|
-
- HY-183770
-
|
|
Akt
PI3K
Epigenetic Reader Domain
c-Myc
|
Cancer
|
|
LCI40 is an orally active dual PI3K/BRD4 inhibitor (PI3Kα IC50 = 0.071 μM, PI3Kβ IC50 = 0.17 μM, PI3Kγ IC50 = 0.66 μM, PI3Kδ IC50 = 0.072 μM, BRD4 BD1 IC50 = 0.19 μM, and BRD4 BD2 IC50 = 1.88 μM. LCI40 inhibits phosphorylation of pAKT (S473) and suppresses c-MYC levels in mantle cell lymphoma cells. LCI40 displays immunomodulatory capacity with minimal toxicity to normal mouse immune cells. LCI40 can be used for the research of mantle cell lymphoma .
|
-
- 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.
|
-
- HY-128582
-
|
|
PI3K
HDAC
|
Cancer
|
|
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 .
|
-
- HY-18085
-
-
- HY-19962
-
|
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 .
|
-
- HY-18085A
-
-
- HY-N0146
-
|
|
PI3K
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
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 .
|
-
- HY-16526
-
|
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.
|
-
- HY-19798
-
|
|
PI4K
PI3K
|
Cancer
|
|
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.
|
-
- HY-10111R
-
|
|
PI3K
Reference Standards
|
Cardiovascular Disease
Cancer
|
|
TG100-115 (Standard) is the analytical standard of TG100-115 (HY-10111). This product is intended for research and analytical applications. TG100-115 is a selective PI3Kγ/PI3Kδ inhibitor with IC50s of 83 and 235 nM, respectively.
|
-
- HY-112443
-
-
- HY-13898
-
|
GDC-0032; RG-7604
|
PI3K
|
Cancer
|
|
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.
|
-
- HY-146159
-
|
|
PI3K
HDAC
|
Cancer
|
|
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 .
|
-
- HY-13431
-
|
|
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 .
|
-
- HY-118374
-
|
|
PI3K
Akt
|
Inflammation/Immunology
|
|
AM-9635 is a selective PI3Kδ inhibitor with oral bioavailability, good in vitro and in vivo activity and pharmacodynamic properties. AM-9635 inhibits PI3Kδ-dependent B cell receptor-mediated AKT phosphorylation and suppresses the production of specific IgG and IgM antibodies in rats immunized with Aplysia leocyanin (KLH).
|
-
- 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.
|
-
- HY-18085S1
-
-
- HY-18085S
-
|
|
PI3K
Autophagy
Mitophagy
Apoptosis
|
Cancer
|
|
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 .
|
-
- HY-N0078
-
|
Ginkgolic acid (13:0); Ginkgoneolic Acid; 6-Tridecylsalicylic acid
|
Bacterial
PI3K
Parasite
|
Infection
Inflammation/Immunology
|
|
Ginkgolic Acid (C13:0) (Ginkgoneolic Acid) is an anti-cariogenic agent and a PI3Kδ inhibitor (IC50: 2.49 μM). Ginkgolic Acid (C13:0) exhibits antibacterial and anti-parasitic activities. Ginkgolic Acid (C13:0) can also inhibit mast cell degranulation (IC50: 2.40 μM) [3].
|
-
- HY-12330
-
|
|
PI3K
|
Cancer
|
|
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).
|
-
- HY-18085S2
-
-
- HY-18085R
-
-
- HY-W937057
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-Me-10-bromodecanoic acid is an E3 ligase ligand-linker conjugate that incorporates a VHL ligand 2 (HY-112078) and linker 10-bromoheptanoic acid. (S,R,S)-AHPC-Me-10-bromodecanoic acid can be used for synthesis of PROTAC PI3Kδ degrader-1 (HY-176239) .
|
-
- HY-162848
-
|
|
PI3K
|
Cancer
|
|
IHMT-PI3K-315 (20e) is a potent and selective PI3Kγ/δ inhibitor with IC50 values for PI3Kγ and PI3Kδ of 4.0 and 9.1 nM, respectively. IHMT-PI3K-315 has antitumor activity .
|
-
- HY-120471
-
|
|
PI3K
|
Inflammation/Immunology
|
|
AM-0687 is a selective inhibitor for PI3Kδ with an IC50 of 2.9 nM. AM-0687 decreases the levels of IgG and IgM specific antibodies, inhibits the anti-IgM/CD40L-induced proliferation of human B cell (IC50=0.8 nM) and the phosphorylation of AKT (IC50=0.7 nM), and exhibits anti-inflammatory efficacy .
|
-
- HY-10683
-
|
|
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).
|
-
- HY-12279
-
|
TGR-1202; RP5264
|
PI3K
Casein Kinase
|
Cancer
|
|
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] .
|
-
- HY-155996
-
|
|
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 .
|
-
- HY-108958
-
|
|
PI3K
|
Cancer
|
|
Rac)-AZD8186 is the racemate of AZD8186 (HY-12330), a PI3K inhibitor that inhibits PI3Kβ (IC50=4 nM), PI3Kδ (IC50=12 nM), PI3Kα (IC50=35 nM) and PI3Kγ (IC50=675 nM) .
|
-
- HY-12279A
-
|
TGR-1202 tosylate; RP5264 tosylate
|
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] .
|
-
- 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.
|
-
- HY-18085AS
-
-
- HY-16526R
-
|
XL-147 (Standard); SAR245408 (Standard)
|
PI3K
Reference Standards
|
Cancer
|
|
Pilaralisib (Standard) is the analytical standard of Pilaralisib. This product is intended for research and analytical applications. 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.
|
-
- HY-12279C
-
|
TGR-1202 hydrochloride; RP5264 hydrochloride
|
PI3K
Casein Kinase
|
Cancer
|
|
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] .
|
-
- HY-N0146R
-
|
|
Reference Standards
PI3K
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Quercetin (dihydrate) (Standard) is the analytical standard of Quercetin (dihydrate). This product is intended for research and analytical applications. 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 .
|
-
- HY-12279B
-
|
TGR-1202 sulfate; RP-5264 sulfate
|
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] .
|
-
- 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 .
|
-
- HY-12868
-
|
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, PI3Kδ, PI3Kβ, PI3Kγ and mTOR, respectively. Bimiralisib is an mTORC1 and mTORC2 inhibitor.
|
-
- 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 .
|
-
- 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 .
|
-
- HY-163538
-
|
|
PI3K
Apoptosis
|
Cancer
|
|
TYM-3-98 is a selective inhibitor for PI3Kδ, with an IC50 of 7.1 nM. TYM-3-98 inhibits proliferationso of B-lymphoma cells. TYM-3-98 inhibits PI3K/AKT/mTOR signaling pathway through induction of apoptosis. TYM-3-98 exhibits good pahrmacokinetic characters and antitumor efficacy in mouse/rat model, without significant toxicity .
|
-
- HY-12279CR
-
|
TGR-1202 hydrochloride (Standard); RP5264 hydrochloride (Standard)
|
PI3K
Casein Kinase
Reference Standards
|
Cancer
|
|
Umbralisib (hydrochloride) (Standard) is the analytical standard of Umbralisib (hydrochloride). This product is intended for research and analytical applications. 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] .
|
-
- HY-120265
-
|
|
PI3K
|
Cardiovascular Disease
|
|
MIPS-9922 is a potent and selective PI3Kβ inhibitor with an IC50 of 63 nM. MIPS-9922 inhibits PI3Kβ with >30-fold higher potency than PI3Kδ. MIPS-9922 blocks PI3K mediated activation of platelet glycoprotein αIIbβ3 activation and platelet adhesion in vitro. MIPS-9922 shows anti-platelet and anti-thrombotic activities .
|
-
- 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-12279R
-
|
TGR-1202 (Standard); RP5264 (Standard)
|
PI3K
Casein Kinase
Reference Standards
|
Cancer
|
|
Umbralisib (Standard) is the analytical standard of Umbralisib. This product is intended for research and analytical applications. 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-174366
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c-Fms
PI3K
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Cancer
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JMC14 is a selective and orally active PI3Kδ and CSF1R inhibitor with IC50 values of 12 nM and 143 nM, respectively. JMC14 preferentially inhibits PI3Kδ-mediated signaling at the cellular level. JMC14 demonstrates potent antitumor activity against B-cell lymphomas and triple-negative breast cancer (TNBC) in both in vitro and vivo studies. JMC14 can be used for the study of antitumor immunity .
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- HY-174461
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PROTACs
PI3K
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Cancer
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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)) .
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- HY-10108
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LY294002
Maximum Cited Publications
1120 Publications Verification
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PI3K
Casein Kinase
DNA-PK
Apoptosis
Autophagy
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Infection
Cancer
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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-155890
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CUDC-907 mesylate
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PI3K
HDAC
Apoptosis
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Cancer
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Fimepinostat mesylate 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.
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- HY-10811R
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Reference Standards
PI3K
mTOR
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Cancer
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|
GNE-493 (Standard) is the analytical standard of GNE-493 (HY-10811). This product is intended for research and analytical applications. 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-13522
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CUDC-907
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PI3K
HDAC
Apoptosis
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Cancer
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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.
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- HY-N0078R
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Ginkgolic acid (13:0) (Standard); Ginkgoneolic Acid (Standard); 6-Tridecylsalicylic acid (Standard)
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Reference Standards
Bacterial
PI3K
Parasite
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Infection
Inflammation/Immunology
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Ginkgolic Acid (C13:0) (Standard) is the analytical standard of Ginkgolic Acid (C13:0) (HY-N0078). This product is intended for research and analytical applications. Ginkgolic Acid (C13:0) (Ginkgoneolic Acid) is an anti-cariogenic agent and a PI3Kδ inhibitor (IC50: 2.49 μM). Ginkgolic Acid (C13:0) exhibits antibacterial and anti-parasitic activities. Ginkgolic Acid (C13:0) can also inhibit mast cell degranulation (IC50: 2.40 μM) .
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- HY-112602
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PI3K
mTOR
|
Cancer
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|
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-110109
-
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PI3K
DNA-PK
mTOR
|
Cancer
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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 .
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-
- HY-12513
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LY3023414
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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-15346
-
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BAY 80-6946
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PI3K
Apoptosis
|
Cancer
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|
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 .
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- HY-10683R
-
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Reference Standards
PI3K
mTOR
|
Cancer
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|
PKi-402 (Standard) is the analytical standard of PKi-402 (HY-10683). This product is intended for research and analytical applications. 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-15346A
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BAY 80-6946 dihydrochloride
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PI3K
Apoptosis
|
Cancer
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|
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 .
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- HY-162713
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EGFR
PI3K
PPAR
|
Cancer
|
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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, PI3Kβ, PI3Kγ, and PI3Kδ 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 .
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-
- HY-144806
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PI3K
Akt
Apoptosis
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Cancer
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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 .
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- HY-112614
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ATM/ATR
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Cancer
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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 .
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- HY-150618
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-
- HY-132231
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PI3K
Apoptosis
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Cancer
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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 .
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- HY-144693
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MEK
PI3K
PERK
|
Cancer
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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 .
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-
- HY-144692
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MEK
PI3K
PERK
|
Cancer
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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 .
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-
- HY-10108R
-
|
|
Reference Standards
PI3K
Casein Kinase
DNA-PK
Apoptosis
Autophagy
|
Infection
Cancer
|
|
LY294002 (Standard) is the analytical standard of LY294002. This product is intended for research and analytical applications. 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-115814
-
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PI3K
|
Inflammation/Immunology
|
|
AM-1430 is an efficient, highly selective and orally active small molecule inhibitor of PI3Kδ with an IC50 of 4.6 nM. AM-1430 exhibits IC50s for PI3Kα, PI3Kβ and PI3Kγ of 14.18, 2.2 and 3.22 μM, respectively. AM-1430 inhibits B cell proliferation and exhibits excellent in vivo activity in pAKT inhibition models and the hemoglobin (KLH) immune response model. AM-1430 can be used for the study of inflammation and autoimmune diseases .
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-
- HY-15346R
-
|
BAY 80-6946 (Standard)
|
Reference Standards
PI3K
Apoptosis
|
Cancer
|
|
Copanlisib (Standard) is the analytical standard of Copanlisib. This product is intended for research and analytical applications. 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 .
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-
- HY-133124
-
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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 .
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-
- HY-147898
-
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PI3K
Apoptosis
|
Cancer
|
|
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-147899
-
|
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PI3K
Apoptosis
|
Cancer
|
|
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-151622
-
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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 .
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-
- HY-149521
-
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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 .
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-
- HY-147900
-
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PI3K
Apoptosis
|
Cancer
|
|
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-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.
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-
- HY-11080A
-
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PI3K
mTOR
|
Cancer
|
|
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-11080
-
PKI-179
1 Publications Verification
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PI3K
mTOR
|
Cancer
|
|
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-149493
-
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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 .
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-
- HY-100603A
-
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PI3K
PI4K
|
Infection
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(S)-GSK-F1 (Compound 28) is an inhibitor for type III phosphatidylinositol 4-kinase α (PI4KIIIα). (S)-GSK-F1 inhibits PI4Kα, PI4Kβ, PI4Kγ, PI3Kα, PI3Kβ and PI3Kδ with pIC50 of 8.3, 6.0, 5.6, 5.6, 5.1 and 5.6, respectively. (S)-GSK-F1 exhibits anti-hepatitis C virus (HCV) activity through inhibition of HCV replication. (S)-GSK-F1 exhibits moderate pharmacokinetic characters in rat model .
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-
- HY-153894
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CDK
Epigenetic Reader Domain
PI3K
NF-κB
SARS-CoV
|
Infection
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
SRX3177 is a triple inhibitor of CDK4/6, PI3K, and BRD4, with IC50s of <2.5 nM (CDK4), 3.3 nM (CDK6), 33 nM (BRD4 BD1), 89 nM (BRD4 BD2), 79 nM (PI3Kα), 83 nM (PI3Kδ), 3.18 μM (PI3Kγ) , respectively. SRX3177 blocks the interaction between the SARS-CoV-2 E protein and the BRD2/4 BD1 domain, restores E protein-attenuated NF-κB activity. SRX3177 exerts broad cytotoxic activity against cancer cells. SRX3177 can be used for the study of anti-SARS-CoV-2 and cancer .
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-
- HY-177277
-
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PI3K
|
Inflammation/Immunology
|
|
HM5023507 is an orally active and selective PI3Kδ/γ inhibitor with IC50s of 4 and 5 μM for PI3Kδ and PI3Kγ over PI3Kβ and PI3Kα. HM5023507 attenuates the PI3Kδ/γ signaling in human basophils. HM5023507 also attenuates the activation and function of human B and T cells and cytokine and IgG production during cocultures, and Th17 differentiation of CD4 T cells. HM5023507 inhibited semiestablished collagen-induced arthritic inflammation in the rat models. HM5023507 can be used for inflammatory diseases like rheumatoid arthritis research .
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-
- HY-178485
-
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PI3K
HDAC
Akt
Histone Methyltransferase
|
Cancer
|
|
SJY26 is a PI3K/HDAC dual-target inhibitor with IC50s of 0.59 nM (PI3Kα and PI3Kδ), 2.02 nM (PI3Kγ), 12.69 nM (PI3Kβ) and 114 nM (HDAC1). SJY26 exhibits potent broad-spectrum anti-proliferative activity, and is particularly sensitive to Jurkat and PC9R cells. SJY26 inhibited the migration of PC9R cells, arrested the cell cycle and induced cell apoptosis. SJY26 reduces AKT phosphorylation, and decreases histone H3 deacetylation (Ac-H3). SJY26 can be used for the studies of non-small cell lung cancer and leukemia .
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-
- HY-182083
-
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PROTACs
PI3K
|
Cancer
|
|
PROTAC PI3Kα/δ degrader-1 is an orally active PI3Kα/δ PROTAC degrader, with an IC50 of 0.34 nM for PI3Kα and 1.85 nM for PI3Kδ. PROTAC PI3Kα/δ degrader-1 inhibits the proliferation and migration of cancer cells, induces G1-phase cell cycle arrest and PI3Kα degradation. PROTAC PI3Kα/δ degrader-1 suppresses tumor growth in breast cancer xenograft mouse models. PROTAC PI3Kα/δ degrader-1 can be used for the research of breast cancer .
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-
- HY-120281
-
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MEK
PI3K
Akt
Apoptosis
Caspase
|
Cancer
|
|
ST-168 is an orally active MEK/PI3K inhibitor with an IC50 of 182 nM against MEK1 and IC50 values of 69.2, 41.7, 1482 and 2293 nM against PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ respectively. ST-168 completely inhibits the phosphorylation of ERK1/2 and AKT and induces cancer cell death in a 3D tumor sphere model. ST-168 demonstrates significant antitumor effects in the A375 melanoma mouse model. ST-168 improves the ocular toxicity profile of MEK inhibitors, showing lower caspase activation levels, indicating reduced apoptosis induction. ST-168 can be used in melanoma research .
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-
- HY-155180
-
|
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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 .
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-
- HY-136765
-
|
|
PI3K
|
Cancer
|
|
PI3K-IN-11 (compound 13) is a PI3K inhibitor, which selectively inhibits PI3Kα, PI3Kβ, PI3K, and PI3Kδ (IC50s=6.4, 13, 8, and 11 nM, respectively) over mTOR (IC50=2.9 μM). PX-13-17OH is greater than 420-fold selective for PI3K in a panel of 20 lipid and protein kinases. PX-13-17OH inhibits phosphorylation of Akt and S6 kinase (S6K) in PTEN-negative U87MG cells when used at concentrations ranging from 0.03 to 1 μg/mL. It inhibits tumor growth in a U87MG mouse xenograft model when administered at doses ranging from 2.5 to 10 mg/kg.
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-
- HY-182671
-
|
|
PI3K
Btk
Apoptosis
|
Cancer
|
|
SRX3305 is an BTK/PI3K/BRD4 inhibitor with IC50s of 6.5 nM, 15 nM, and 4 nM toward BTK, PI3Kɑ and PI3Kδ, respectively. SRX3305 attenuates chronic lymphocytic leukemia (CLL) and mantle cell lymphoma (MCL) cell proliferation and promotes apoptosis in a dose-dependent fashion. SRX3305 yields potent anti-tumor effects but spares healthy bystander cells. SRX3305 inhibits the activation-induced proliferation of primary CLL cells in vitro and effectively blocks microenvironment-mediated survival signals. SRX3305 blocks CLL cell migration toward CXCL-12 and CXCL-13. SRX3305 maintains its anti-tumor effects in Ibrutinib (HY-10997)-resistant CLL cells. SRX3305 can be used for research in CLL, diffuse large B-cell lymphoma (DLBCL) and MCL .
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-
- 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 .
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-
- HY-130133
-
|
|
PI3K
mTOR
Akt
Apoptosis
Paraptosis
p38 MAPK
Mitochondrial Metabolism
P-glycoprotein
CDK
MMP
HIF/HIF Prolyl-Hydroxylase
VEGFR
|
Cancer
|
|
DHW-221 is a potent orally active dual PI3K/mTOR inhibitor, exhibiting low nanomolar potency against all four Class I PI3K isoforms and mTOR (PI3Kα, IC50 = 0.50 nM; PI3Kβ, IC50 = 1.9 nM; PI3Kγ, IC50 = 1.8 nM; PI3Kδ, IC50 = 0.74 nM; mTOR, IC50 = 3.9 nM). DHW-221 exerts antitumor effects by blocking the PI3K/Akt/mTOR pathway and inducing mitochondrial apoptosis and paraptosis (via Endoplasmic Reticulum (ER) stress and MAPK signaling) and arrests cell cycle, thereby inhibiting cell migration, invasion and angiogenesis. DHW-221 inhibits tumor growth in both the A549/Taxol (HY-B0015) and the HCC827 xenograft mouse models. DHW-221 can be used for non-small cell lung cancer (NSCLC), colon and breast cancer research [3].
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-
- HY-128633
-
|
|
PI3K
Akt
Apoptosis
|
Cancer
|
|
PI3K-IN-4 is a potent Pan-PI3K inhibitor. PI3K-IN-4 has high activity for three PI3K isoforms with the IC50 values of picomole. PI3K-IN-4 shows superior inhibitory activity against PI3Kα (IC50 = 0.20 nM), PI3Kβ (IC50 = 2.99 nM), PI3Kδ (IC50 = 0.48 nM) and PI3Kγ (IC50 = 0.58 nM) and has no significant activity against EGFR. PI3K-IN-4 inhibits cancer cell growth though PI3K/Akt signaling pathway, leading to the inhibition of colony formation and the induction of apoptosis. PI3K-IN-4 can be used for lung, colon and breast cancer research .
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-
- 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 .
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- HY-182368
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PI3K
Akt
Apoptosis
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Cancer
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PI3Kα-IN-30 is an orally active, selective PI3Kα inhibitor with an IC50 of 2.8 nM. PI3Kα-IN-30 inhibits cancer cell proliferation, as well as the phosphorylation of Akt (S473) and pS6 (S240/244). PI3Kα-IN-30 shows low growth inhibitory activity against normal somatic cell lines at a concentration of 30 μM. PI3Kα-IN-30 induces cancer cell apoptosis and exerts anti-tumor efficacy in xenograft models. PI3Kα-IN-30 can be used for the research of breast cancer .
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- HY-181581
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PI3K
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Cancer
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IMM-H012 is a specific PI3K inhibitor with an IC50 of 0.80 nM against PI3Kα. IMM-H012 combined with [ 177Lu]Lu-P4 shows synergistic antitumor effects against stomach cancer and lung cancer .
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- HY-183787
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PI3K
Akt
mTOR
Apoptosis
CDK
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Cancer
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PI3Kα-IN-33 is an orally active and selective PI3Kα inhibitor with an IC50 of 9.9 nM. PI3Kα-IN-33 blocks the PI3K/Akt/mTOR signaling pathway. PI3Kα-IN-33 induces apoptosis and triggers G2/M-phase arrest via Cyclin B1 and CDK1 downregulation. PI3Kα-IN-33 can be used for the research of colorectal cancer .
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- HY-100424
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PI3K
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Cancer
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PI3K-IN-63 (compound 9) is a PI3Kα inhibitor with a Ki of 0.35 nM against human targets. PI3K-IN-63 inhibits the phosphorylation of AKT at the S473 site in cellular assays. PI3K-IN-63 reduces the viability of non-small cell lung cancer cell lines carrying PIK3CA mutations. PI3K-IN-63 can be used in studies related to non-small cell lung cancer .
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Product Name |
Type |
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- HY-40029
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(S)-(+)-3-Amino-1-boc-PIperidine
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Biochemical Assay Reagents
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(S)-1-Boc-3-aminopiperidine is a key intermediate for the synthesis of various novel inhibitors, such as CHK1 inhibitors and PI3Kδ inhibitors .
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Product Name |
Target |
Research Area |
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- HY-W040417
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PI3K
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Others
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Boc-L-cyclobutylglycine is a Boc-protected L-cyclic amino acid and synthetic intermediate in the preparation of purinyl quinazolinone PI3Kδ inhibitors .
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Product Name |
Category |
Target |
Chemical Structure |
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Product Name |
Chemical Structure |
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- HY-18085S1
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1 Publications Verification
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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 .
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- HY-18085S2
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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 .
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- HY-17635S
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Leniolisib-d5 is a deuterated labeled Leniolisib . Leniolisib (CDZ173) is a potent and selective PI3Kδ inhibitor. Leniolisib has the potential for immunodeficiency disorders treatment.
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- HY-18085S
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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 .
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- HY-18085AS
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1 Publications Verification
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Quercetin-d3 hydrate is a deuterium labeled Quercetin hydrate (HY-18085A), a flavonoid which can stimulate recombinant SIRT1 and also 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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