pim-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.

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].

TCS PIM-1 1 (SC 204330)(sc-204330) is an effective and specific ATP-competitive Pim-1 kinase inhibitor (IC50: 50 nM), exhibiting good specificity over MEK1/MEK2 and Pim-2 (IC50s > 20,000 nM).

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.

TCS-PIM-1-4a (SMI-4a), a Pim inhibitor, blocks mTORC1 activity through activation of AMPK and kills a wide range of both myeloid and lymphoid cell lines (IC50=0.8-40 μM).

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.

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.

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 kinase inhibitor 3 (Compound H5) is a potent inhibitor of Pim-1 kinase with an inhibitory concentration (IC50) of 35.13 nM [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].

Pim-1 kinase inhibitor 2 (Compound 13) is a potent inhibitor of Pim-1 kinase with potential for cancer research due to its ability to induce apoptosis [1].

Pim-1 kinase inhibitor 5 (Compound 4c) has an IC50 of 0.61 μM and exhibits cytotoxicity against cancer cell lines HepG2, MCF-7, PC3, and HCT-116, with IC50 values ranging from 6.95 to 20.19 μM [1].

Pim-1 Kinase Inhibitor 10 (compound 13a) acts as both a competitive and non-competitive inhibitor of PIM-1/2 kinase, promoting cell apoptosis and displaying anticancer properties. Additionally, this compound triggers the activation of caspase 3/7 [1].

Pim-1 kinase inhibitor 6 (Compound 4d) is a robust inhibitor of Pim-1 kinase, demonstrating an IC 50 of 0.46 μM. It significantly exhibits cytotoxic effects on cancer cells [1].

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/ERK8-IN-1 (TMCB) is a dual inhibitor of casein kinase 2 (CK2) (Ki: 0.25 µM) and ERK8 (IC50s: 0.50 μM) with pro-apoptotic efficacy. CK2/ERK8-IN-1 also binds to PIM1, DYRK1A, and HIPK2 (Kis: 8.65 µM, 11.9 µM, and 15.25 µM).

XL-413 is an orally bioavailable cell division cycle 7 homolog (CDC7) kinase inhibitor with potential antineoplastic activity. XL-413 binds to and inhibits the activity of CDC7, which may result in the inhibition of DNA replication and mitosis, the induct

PIM1-IN-1 is a potent and highly selective inhibitor of PIM1/3 (IC50s: 7 nM for PIM1, 5530 nM for PIM2, and 70 nM for PIM3) with antiproliferative and anti-cancer activity.

CX-6258 is an orally valid Pim 1/2/3 kinase(IC50=5 nM/25 nM/16 nM) inhibitor. It has good biological activity and kinase specificity.

(Z)-SMI-4a (TCS PIM-1 4a) is a selective ATP-competitive Pim-1 kinase inhibitor with an IC50 of 21 nM.

SGI-1776 (Pim-Kinase Inhibitor IX) has been used in trials studying the treatment of Prostate Cancer, Non-Hodgkins Lymphoma, and Relapsed/Refractory Leukemias.