sub-nanomolar

Copanlisib (BAY 80-6946) is a phosphoinositide 3-kinase (PI3K) inhibitor with potential antineoplastic activity. By inhibiting the PI3K signaling pathway, Copanlisib may impede tumor cell growth and survival in certain tumor populations. Dysregulated PI3K signaling, often linked to tumorigenesis, may also contribute to tumor resistance to various antineoplastic agents.

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.

AMG580 is a selective PDE10A antagonist exhibiting sub-nanomolar affinity towards PDE10A in rats, primates, and humans. It is utilized in research as a non-invasive radiotracer.

AZD5991 is a potent and selective Mcl-1 inhibitor aimed at treating hematological cancers. As a well-designed macrocyclic compound, AZD5991 exhibits sub-nanomolar affinity for Mcl-1. It primarily inhibits the myeloid cell leukemia-1 protein (Mcl-1; Bcl2-L-3), showing potential pro-apoptotic and anti-tumor activity. AZD5991 binds to Mcl-1, preventing its interaction with certain pro-apoptotic proteins, leading to apoptosis in cells overexpressing Mcl-1.

PARP1-IN-34 (compound 30) is a selective PARP1 inhibitor with an IC50 of 0.32 nM. It is a sub-nanomolar PARP1 inhibitor with 1000-fold selectivity over PARP2, having an IC50 of 326 nM, and exhibits anticancer activity.

JNK-1-IN-5 (Compound 14) is a potent JNK1 inhibitor with sub-nanomolar efficacy. It effectively inhibits TGF-β-induced epithelial-mesenchymal transition and shows promise for research targeting JNK1 as an anti-pulmonary fibrosis agent.

WWL0245 is a potent and selective BRD4-targeting PROTAC that exhibits sub-nanomolar degradation efficiency (DC50 < 1 nM) for BRD4 over BRD2 3 and PLK1 (DC50 > 1 μM). It demonstrates pronounced selective cytotoxicity in BETi-sensitive cancer cell lines, particularly in AR-positive prostate cancer lines, making it a promising candidate for research in AR-positive prostate cancer and a valuable tool for the investigation of BRD4's biological function [1].

BLU-263 is an investigational, potent, and selective oral small molecule inhibitor of KIT with sub-nanomolar potency against D816V-mutant KIT.

Argifin is a sub-nanomolar chitinase inhibitor produced by soil microorganisms (IC50: 0.025 μM, 6.4 μM, 1.1 μM, and 4.5 μM for SmChiA [Serratia marcescens chitinase A], SmChiB, Aspergillus fumigatus chitinase B1, and human chitotriosidase).