pi3kδ

IHMT-PI3Kδ-372 is a selective inhibitor of PI3Kδ with an IC50 of 14 nM and can be used in studies about chronic obstructive pulmonary disease.

IHMT-PI3Kδ-372 S-isomer is a potent and selective PI3Kδ inhibitor with an IC50 of 14 nM. IHMT-PI3Kδ-372 S-isomer 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.

PI3Kδ-IN-15 is a selective PI3Kδ inhibitor that inhibits PI3Kδ more than 30-fold more effectively than PI3Kγ, PI3Kβ, and PI3Kα.

PI3Kδ-IN-16 is a selective and potent PI3Kδ inhibitor with anticancer and antiproliferative activity, induces cell cycle arrest and apoptosis.

Quercetin, a flavonoid natural product, is a SIRT1 activator. It is also a PI3K inhibitor, inhibiting PI3Kγ, PI3Kδ, and PI3Kβ with IC50 values of 2.4, 3.0, and 5.4 μM, respectively. Recognized as a heat shock protein inhibitor, Quercetin can significantly reduce exosome release in TII models by downregulating Hsp70 or Hsp90.

GS-9901 is a selective, orally active and potent PI3Kδ inhibitor (IC50: 1 nM) for the study of non-Hodgkin's lymphoma and chronic lymphocytic leukemia.

Duvelisib (INK1197, IPI-145) is a selective inhibitor of phosphatidylinositol 3-kinase (PI3K) and p100δ, with effects on p110δ (IC50 value is 0.0025 μM), p110γ (IC50 value is 0.274 μM), p110β (IC50 value is 0.85 μM) and p110α (IC50 value is 1.602 μM).

GSK2292767 is a potent and selective inhibitor of PI3Kδ.

GSK2292767 FA is a potent and selective inhibitor of PI3Kδ (pIC50 : 10.1).GSK2292767 FA is more than 500-fold more selective than other PI3K isoforms.GSK2292767 FA can be used in the study of respiratory diseases.

CZC24832 is a selective inhibitor of PI 3-kinase γ.

PF-04691502 is a potent and selective inhibitor of PI3K and mTOR kinases with antitumor activity.

AS-041164 is a selective and orally active PI3Kγ isoform inhibitor(IC50 of 70 nM), and shows less activity against PI3Kα, PI3Kβ, and PI3Kδ (IC50s of 240 nM, 1.45 μM, and 1.70 μM, respectively). It has anti-inflammatory effects.

NIBR-17 is a pan class I PI3K inhibitor. NIBR-17 inhibits PI3KKα, PI3KKβ, PI3KKγ, and PI3KKδ with IC50 of 1 nM, 9.2 nM, 9 nM, and 20 nM respectively.

Acalisib (CAL-120) (GS-9820) is a potent and selective inhibitor of PI3Kδ.

ON 146040 is an effective inhibitor of PI3K isoforms with IC50s of 14 and 20 nM for PI3Kα and PI3Kδ, respectively.

PARP/PI3K-IN-1 is a novel dual poly (ADP-ribose) polymerase (PARP) and phosphatidylinositol 3-kinase (PI3K) dual inhibitor with anticancer, antitumour and antiproliferative activities for the study of breast, pancreatic and lung cancers.

Tenalisib (RP6530) (RP6530) is a potent and selective inhibitor of PI3Kδ and PI3Kγ(IC50 values of 25 and 33 nM, respectively.)

Umbralisib R-enantiomer (RP5264 R-enantiomer) is a delta inhibitor of PI3K and a less active enantiomer of TGR-1202. The IC50 of Umbralisib R-enantiomers against δPI3 kinase is at least 20 times lower than that of the inhibitors against other PI3K isoforms (A, β, and γ).

Copanlisib dihydrochloride (BAY 80-6946 dihydrochloride) is an ATP-competitive pan-class I PI3K inhibitor, with IC50 values of 0.5 nM for PI3Kα, 0.7 nM for PI3Kδ, 3.7 nM for PI3Kβ, and 6.4 nM for PI3Kγ. It exhibits superior antitumor activity and demonstrates more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR.

LTURM34 is an inhibitor of DNA-PK with IC50 of 34 nM. LTURM34 displays effective antiproliferative activity in a wide range of tumor cell lines. LTURM34 shows 170-fold selectivity for DNA-PK over PI3K .

Umbralisib hydrochloride is a novel PI3Kδ inhibitor (IC50 and EC50 of 22.2 nM and 24.3 nM, respectively). Umbralisib hydrochloride is also active against CK1ε (EC50: 6.0 μM).

Sapanisertib (INK 128) is an orally bioavailable inhibitor of raptor-mTOR (TOR complex 1 or TORC1) and rictor-mTOR (TOR complex 2 or TORC2) with potential antineoplastic activity.

PI3Kδ-IN-23 (compound A11) is a potent inhibitor of PI3Kδ, with an IC50 of 0.27 nM. It binds to PI3Kδ through covalent interaction with Lys779 and plays a significant role in cancer research.

PI3Kδ BET-IN-1 (compound 10b) exhibits excellent and balanced activity against PI3Kδ (IC50= 112 nM) and BRD4-BD1 (IC50= 19 nM), while also demonstrating strong antiproliferative effects in DLBCL cells.