pim in 1

PIM-IN-1 is a pan-PIM kinase inhibitor with an EC50 of 61 nM in KG-1 and an EC50 of 71 nM in pS6.

MNK/PIM-IN-1 is a novel dual inhibitor targeting both MNK and PIM pathways, characterized by its favorable pharmacokinetic profile.

Pim-1/2 Kinase Inhibitor 1, an orally active inhibitor, impedes the action of Pim kinases by preventing their ability to phosphorylate peptides. It particularly inhibits the phosphorylation of 4E-BP1 and p27 Kip1 by Pim protein kinases. This compound is valuable in cancer research, with a notable application in studying prostate cancer [1].

Pim-1 kinase inhibitor 8 is a potent Pim-1 kinase inhibitor with anticancer activity and can effectively inhibit cell migration.Pim-1 kinase inhibitor 8 is cytotoxic to MCF-7 and HepG2 cells, and is a candidate compound for breast cancer research.

PIM1-IN-1 is a potent and highly selective PIM kinase inhibitor with strong preference for PIM1 and PIM3 over PIM2, effectively inhibiting BAD phosphorylation without detectable effects on FLT3 or hERG binding, and exhibiting antiproliferative and anticancer activity suitable for mechanistic studies of PIM-driven oncogenic signaling.

PIM-1/CK2-IN-2 (compound 3aA) is an inhibitor of the PIM-1/CK2 enzymes. This compound can induce the mitochondrial apoptosis pathway in CCRF-CEM cells and is utilized in cancer research.

Pim-1 kinase inhibitor 9 (compound 8b) is a specific inhibitor targeting Pim-1 kinase, with an IC50 value of 0.24 µM. It causes cell cycle arrest at the S phase in breast cancer T47D cells and exhibits antitumor activity.

PIM-1/HDAC-IN-2 is a potent dual inhibitor of PIM/HDAC, exhibiting an IC50 value of 0.11 μM. It synergistically impedes cell proliferation through the inhibition of PIM1 kinase and the selective suppression of HDAC6. This compound effectively induces PARP cleavage, causing cell cycle arrest in the G1 phase and reducing S phase cells. PIM-1/HDAC-IN-2 demonstrates significant anticancer activity in the MV4-11 tumor xenograft model, with minimal toxicity.

PIM-1 Inhibitor 2 (PIM1-IN-2) is a potent Pim-1 inhibitor with potential anti-cancer activity, used in cancer research.

Pim1/AKK1-IN-1 (LKB1/AAK1 dual inhibitor) is a potent multi-kinase inhibitor with Kd values of 35 nM/53 nM/75 nM/380 nM for Pim1/AKK1/MST2/LKB1 respectively, and also inhibits MPSK1 and TNIK.

Pim-1 kinase inhibitor 1 can be used in cancer research, showing anticancer activity against a variety of cancer cell lines by promoting cell apoptosis. Pim-1 kinase inhibitor 1 is an inhibitor of Pim-1 kinase with an IC 50 value of 0.11 μM [1].

PIM-1/HDAC-IN-1 (compound 4d) is a potent PIM-1 inhibitor with an IC50 of 343.87 nM, and it exhibits strong inhibitory activity and selectivity against HDAC 1 and HDAC 6, with IC50 values of 63.65 and 62.39 nM, respectively. Additionally, it induces apoptosis and causes G2/M phase cell cycle arrest in MCF-7 cell lines, specifically inducing pre-G1 apoptosis [1].

PIM1-IN-7 (compound 6c) is a potent PIM-1 inhibitor with an IC50 of 0.67 μM, and it also shows notable cytotoxicity against HCT-116 and MCF-7 cells, with IC50 values of 42.9 and 7.68 μM, respectively [1].

PIM1-IN-6 (compound 5h) is a potent PIM-1 inhibitor with an IC50 of 0.60 μM and exhibits high cytotoxicity on HCT-116 and MCF-7 cells, with IC50 values of 1.51 μM and 15.2 μM, respectively.

PIM1-IN-3 (Compound HL8) is a potent, selective PIM-1 enzyme inhibitor that effectively induces apoptosis in Colo320 cells, demonstrating significant research potential for cancer diseases.

Pim-1 kinase inhibitor 4 is a potent Pim-1 kinase inhibitor with an IC50 value of 17.01 nM.Pim-1 kinase inhibitor 4 also possesses antioxidant activity and potential anticancer activity, and inhibits DPPH.Pim-1 kinase inhibitor 4 promotes apoptosis and inhibits the growth of PC-3 cells with an IC50 value of 16 nM. Pim-1 kinase inhibitor 4 promotes apoptosis and inhibits PC-3 cell growth with an IC50 of 16 nM. Pim-1 kinase inhibitor 4 can be used in prostate cancer research.

Compound 5b, designated as Pim-1/2 kinase inhibitor 2, acts as a competitive inhibitor of both PIM-1 and PIM-2 kinases, demonstrating IC50 values of 1.31 μM and 0.67 μM, respectively. This compound exhibits potent in-vitro anticancer activity against various cancer cell lines, including myeloid leukemia (NFS-60), liver (HepG-2), prostate (PC-3), and colon (Caco-2), while showing low cytotoxicity to the normal human lung fibroblast Wi-38 cell line [1].

CK2/PIM1-IN-1 is an inhibitor of CK2 (IC50: 3.787 μM) and PIM1 (IC50: 4.327 μM), developed for researching proliferative disorders like cancer and other kinase-associated conditions.

(1S,3R,5R)-PIM447 (dihydrochloride) is an inhibitor of PIM with IC50 values of 0.095 μM for Pim1, 0.522 μM for Pim2, and 0.369 μM for Pim3.

Pim-1 kinase inhibitor 11 (10f) is an inhibitor of PIM-1 with an IC50 value of 0.18 μM. It exhibits anticancer activity by inducing apoptosis and causing cell cycle arrest.

CDK2/PIM1-IN-1 is an inhibitor of the kinases CDK2 (IC50: 0.27 μM) and PIM1 (IC50: 0.67 μM). It can induce apoptosis (cell death) and reduce the expression of TNF-α, which promotes tumors. CDK2/PIM1-IN-1 exhibits antitumor activity.

PIM3-IN-1 hydrochloride (Compound 19a) is an inhibitor of PIM2/3 kinases, showing the strongest inhibition against PIM3 with an IC50 in the nanomolar range. PIM3-IN-1 hydrochloride is applicable in cancer research.

CDK6/PIM1-IN-1 (Compound 51) hydrochloride is an orally active and potent dual inhibitor of CDK6 and PIM1, with IC50 values of 39 nM and 88 nM, respectively. It also inhibits CDK4 with an IC50 of 3.6 nM. This compound significantly suppresses the proliferation of acute myeloid leukemia (AML) cells, arrests the cell cycle at the G1 phase, and induces apoptosis. CDK6/PIM1-IN-1 hydrochloride demonstrates anti-AML activity.

PIM1-IN-8 is an inhibitor targeting the PIM1/p65 signaling pathway. It suppresses the expression of α-SMA and type I collagen in activated fibroblasts and inhibits TGF-β-induced migration. In a Bleomycin (BLM)-induced pulmonary fibrosis mouse model, PIM1-IN-8 alleviates lung fibrosis. This compound can be utilized in research on idiopathic pulmonary fibrosis (IPF).