Pim

PIM1-IN-1 is a potent and highly selective PIM1/3 inhibitor, with IC50s of 7, 5530 and 70 nM for PIM1, PIM2, and PIM3, respectively, inhibits the phosphorylation of BAD, a downstream target of PIM, with an EC50 of 262 nM.

CX-6258 hydrochloride hydrate is a potent, orally efficacious Pim 1/2/3 kinase(IC50=5 nM/25 nM/16 nM) inhibitor with excellent biochemical potency and kinase selectivity.

PIM-1 inhibitor 2 is a potent Pim-1 kinase inhibitor (Ki = 91 nM).

TCS PIM-1 1 is a potent and selective ATP-competitive Pim-1 kianse inhibitor with IC50 of 50 nM, displays good selectivity over Pim-2 and MEK1/MEK2(IC50s >20,000 nM).

PIM-447 dihydrochloride is a potent and selective pan-PIM kinase inhibitor targeting PIM1, PIM2, and PIM3 with Ki values of 6, 18, and 9 pM, respectively. This compound exhibits significant antimyeloma activity and protective effects on bone tissue. PIM-447 dihydrochloride also induces apoptosis, making it a valuable tool for research into cancer therapies and bone disease studies.

NSC756093 is a GBP1:PIM1 interaction inhibitor with a binding affinity of 38 nM. This compound demonstrates significant biological activity by suppressing cell proliferation, reducing migration, inducing G1 phase cell-cycle arrest, and promoting apoptosis in ovarian cancer cells. Additionally, NSC756093 decreases proteasomal activity and leads to the accumulation of ubiquitinated proteins, thereby inhibiting tumor progression and lung metastasis in murine ovarian cancer xenograft models. Furthermore, it enhances sensitivity of prostate cancer cells to Docetaxel and sensitizes GBP1-overexpressing ovarian cancer cells to Paclitaxel, making it a valuable reagent for research in prostate and ovarian cancer.

CK2/PIM1-IN-1 is a selective inhibitor targeting casein kinase 2 (CK2) and PIM1, demonstrating IC50 values of 3.787 μM and 4.327 μM, respectively. This compound is designed for research into proliferative disorders, particularly cancer, and has potential applications in studying kinase-related conditions such as inflammation, pain, vascular disorders, pathogenic infections, and certain immunological disorders.

PIM-1/HDAC-IN-1 is a selective inhibitor of PIM-1 as well as histone deacetylases HDAC 1 and HDAC 6, exhibiting an IC50 of 343.87 nM for PIM-1 and 63.65 nM and 62.39 nM for HDAC 1 and HDAC 6, respectively. This compound demonstrates significant apoptotic activity in MCF-7 cell lines, inducing pre-G1 apoptosis and causing cell cycle arrest at the G2/M phase. PIM-1/HDAC-IN-1 is a valuable tool for research on cancer biology and the regulation of cell proliferation and apoptosis.

PIM1-IN-3 is a selective inhibitor of the PIM1 kinase, known for its role in promoting cell survival and proliferation. This compound effectively induces apoptosis in Colo320 cells, demonstrating its potential as a therapeutic agent in cancer research. PIM1-IN-3 serves as a valuable tool for studying PIM1-related signaling pathways and exploring targeted cancer treatments.

Pim-1 kinase inhibitor 1 is a selective inhibitor of Pim-1 kinase, demonstrating an IC50 value of 0.11 μM. This compound exhibits significant anticancer activity across various cancer cell lines by promoting cellular apoptosis. Pim-1 kinase inhibitor 1 is a valuable tool for research applications focused on cancer biology and therapeutic development.

VS-II-173 is a potent pan-Pim kinase inhibitor, exhibiting IC50 values of 0.07 μM for Pim1 and 0.02 μM for Pim3, with a residual activity of 46% at 1 μM for Pim2. This compound selectively targets acute myeloid leukemia (AML) cells, demonstrating significant inhibition of key phosphorylation events, including Stat5 (Y694) and MDM2 (S166), which disrupts pro-survival signaling pathways and promotes apoptosis. VS-II-173 shows enhanced anti-AML efficacy when used in combination with Daunorubicin and is especially relevant for research involving AML characterized by FLT3-ITD and NPM1 mutations. Its minimal toxicity to non-malignant cells makes it a valuable tool in cancer research.

Quercetagetin, also known as 6-Hydroxyquercetin, is a flavonoid that serves as a selective inhibitor of Pim-1 kinase, exhibiting an IC50 of 0.34 μM. This compound demonstrates notable anti-inflammatory and anticancer activities, making it a valuable tool in cancer research. Its ability to penetrate cell membranes allows for diverse applications in studies focused on cellular signaling pathways and therapeutic interventions.