Pim Inhibitor

FD1024 is PIM inhibitor (IC₅₀s: 1.96, 38.9, 4.17 nM for PIM1, 2, 3). FD1024 can be used for research of acute myeloid leukemia. FD1024 has strong antiproliferative activity against the tested AML cell lines, with 0.16 μM, 0.12 μM, 1.05 μM, 1.39μM for EOL-1, MV-4-11, KG-1, MOLM-16 cells. FD1024 also has antitumor efficacy in mice.

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

FD2024 is a pan-PIM kinase inhibitor with IC₅₀ values of 0.17 nM, 1.86 nM, and 0.38 nM against PIM-1, PIM-2, and PIM-3, respectively. FD2024 induces cell apoptosis. FD2024 inhibits the phosphorylation of mTOR, p70S6K, S6, 4EBP1, and BAD proteins. FD2024 exhibits anti-acute myeloid leukemia activity. FD2024 can be used in studies related to acute myeloid leukemia.

Protein kinase inhibitor 11 (Compound I-96) is a protein kinase inhibitor that can inhibit the activity of PIM-1, CDK-2, GSK-3, and SRC. Protein kinase inhibitor 11 holds promise for research in cancer, immune disorders, and neurodegenerative diseases.

CDK2/PIM1-IN-1 is an inhibitor of CDK2 (IC₅₀: 0.27 μM) and PIM1 (IC₅₀: 0.67 μM) kinases. CDK2/PIM1-IN-1 induces apoptosis and reduces tumor-promoting TNF-α expression. CDK2/PIM1-IN-1 has antitumor activity.

PIM-IN-5 is a PIM kinase inhibitor. PIM-IN-5 can be used for the research of acute myeloid leukemia.

PIM1-IN-8 is a PIM1/p65 pathway inhibitor. PIM1-IN-8 suppresses the expression of α-SMA and collagen I in activated fibroblasts and blocks TGF-β induced migration. PIM1-IN-8 alleviates pulmonary fibrosis in a Bleomycin (BLM) (HY-17565A)-induced pulmonary fibrosis mice model. PIM1-IN-8 can be used for the study of idiopathic pulmonary fibrosis (IPF).

10-DEBC is a selective Akt inhibitor. 10-DEBC shows strong inhibitory activity against Moloney murine leukemia virus (Pim) kinase-1 (IC₅₀=1.28 μM).

Pim-1 kinase-IN-15 (Compound 15) is a highly potent and selective Pim-1 kinase inhibitor (IC₅₀=0.212 μM). Pim-1 kinase-IN-15 induces tumor cell apoptosis and suppresses cell migration. Pim-1 kinase-IN-15 is promising for research of oncology, such as breast cancer.

VB1080 (compound 12) is a potent PIM inhibitor with IC₅₀ values of 69.5, 4996, 9.88 µM for PIM1, PIM2, PIM3, respectively. VB1080 shows cytotoxicity. VB1080 shows anthelmintic activity.

Pim3 Rat Pre-designed siRNA Set A contains three designed siRNAs for Pim3 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

PIM1-IN-4 (Compound 8) is a potent inhibitor of PIM1. PIM1-IN-4 reveals strong inhibition of five other enzymes, i.e., SGK-1, PKA, CaMK-1, GSK3β, and MSK1. PIM1-IN-4 has the potential for the research of cancer diseases.

BTK-IN-48 is a BTK inhibitor with an IC₅₀ of 1.14 μM. BTK-IN-48 inhibits recombinant BTK and c-Src, and exerts moderate inhibitory effects on LCK, BMX/ETK, FLT3 and PIM1. BTK-IN-48 can be used in the research of B-cell malignancies and autoimmune diseases.

LGB321 monohydrochloride is a potent, selective, orally active and ATP competitive inhibitor of all three PIM kinases. LGB321 monohydrochloride inhibits proliferation, mTOR-C1 signaling and phosphorylation of BAD in a number of cell lines derived from diverse hematologic malignancies. LGB321 monohydrochloride can be used for the research of hematologic malignancies.

Pim3 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Pim3 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

PIM-1/HDAC-IN-2 is a robust PIM/HDAC inhibitor (IC₅₀ = 0.11 μM in MV4-11cells), which exerts a synergistic antiproliferative effect through a dual mechanism of inhibiting PIM1 kinase and selectively inhibiting HDAC6. PIM-1/HDAC-IN-2 induces cell apoptosis. PIM-1/HDAC-IN-2 remarkably induces the cleavage of PARP, thereby initiating the arrest of the cell cycle in G1 phase and a reduction in S phase. PIM-1/HDAC-IN-2 demonstrates significant anticancer efficacyin the MV4-11 xenograft model without notable toxicity^[1]_.

Multi-target kinase-IN-8 (3d) is an anti-cancer agent. Multi-target kinase-IN-8 exhibits inhibitory activity against various protein kinases (B-Raf V600E (IC₅₀ = 0.078 µg/mL), c-Met (IC₅₀ = 0.405 µg/mL), Pim-1 (IC₅₀ = 1.053 µg/mL), EGFR WT (IC₅₀ = 0.177 µg/mL), VEGFR-2 (IC₅₀ = 0.275 µg/mL)). Multi-target kinase-IN-8 can induce cell cycle arrest and promote early and late apoptosis. Multi-target kinase-IN-8 is commonly used in cancer research.

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

MNK/PIM-IN-1 represents an innovative dual MNK/PIM inhibitor with a good pharmacokinetic profile.

PIM3 Human Pre-designed siRNA Set A contains three designed siRNAs for PIM3 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.