Pim Inhibitor

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.

Multi-kinase-IN-6 (compound 10e) is a multikinase inhibitor that shows good enzyme inhibitory activity against TrkA, ALK2, c-KIT, EGFR, PIM1, CK2α, CHK1, and CDK2. Multi-kinase-IN-6 reveals antiproliferative activity against MCF7, HCT116 and EKVX with IC₅₀ values of 3.36 μM, 1.40 μM and 3.49 μM, respectively. Multi-kinase-IN-6 shows cell cycle arrest at the G1/S phase and G1 phase in MCF7 and HCT116 cells with good apoptotic effect.

NMS-P645 is a PIM1 inhibitor. NMS-P645 exhibits anti-proliferative activity when combined with GDC-0941 (HY-50094) in TMPRSS2/ERG positive and negative PCa cells. NMS-P645 can reverse PIM1-induced pro-survival signals in prostate cells. NMS-P645 can be studied in research on prostate cancer.

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

Pim-1 kinase inhibitor 9 (compound 8b) is a selective inhibitor against Pim-1 kinase with IC₅₀ value of 0.24 µM. Pim-1 kinase inhibitor 9 inhibits cell cycle of T47D at S phase. Pim-1 kinase inhibitor 9 reveals antitumor activity.

Pim-1 kinase inhibitor 4 (Compound 10f) is a Pim-1 kinase inhibitor (IC₅₀: 17.01 nM). Pim-1 kinase inhibitor 4 also has antioxidant activity and inhibits DPPH. Pim-1 kinase inhibitor 4 induces apoptosis in PC-3 cell, and inhibits PC-3 cell growth with an IC₅₀ of 16 nM. Pim-1 kinase inhibitor 4 can be used for research of prostate cancer.

SGI-1776 is an inhibitor of Pim kinases, with IC₅₀s of 7 nM, 363 nM, and 69 nM for Pim-1, Pim-2 and Pim-3, respectively.

PC-046 is a multi-target inhibitor for tyrosine receptor kinase B (TrkB), IRAK-4 and Pim-1, with IC₅₀ of 13.4 μM, 15.4 μM and 19.1 μM, respectively. PC-046 exhibits cytotoxicity against pancreatic cancer cell BxPC3 with IC₅₀ of 7.5-130 nM. PC-046 induces apoptosis and arrests cell cycle at G2/M phase in BxPC3. PC-046 exhibits antitumor efficacy and exhibits good pharmacokinetic characteristics in mice.

PIM3-IN-1 hydrochloride (Compound 19a) is an inhibitor of (PIM2/3), with the highest inhibition level being against PIM3, having an IC₅₀ value in the nanomolar range. PIM3-IN-1 hydrochloride can be used in cancer research.

Pim-1 kinase inhibitor 6 (Compound 4d) is a potent Pim-1 kinase inhibitor with IC₅₀ value of 0.46 μM, and has significant cytotoxic effect on cancer cells.

MNK/PIM-IN-2 is a Mnk/Pim kinase inhibitor with an IC₅₀ of 32 nM for Mnk1, 3 nM for Mnk2, and 37 nM for Pim1. MNK/PIM-IN-2 reduces the levels of p-eIF4E and p-4EBP1. MNK/PIM-IN-2 induces cell cycle arrest, apoptosis (apoptosis) and exerts antiproliferative effects in leukemia cells. MNK/PIM-IN-2 can be used in studies related to leukemia.

PIM1-IN-3 (Compound HL8) is a potent inhibitor of PIM1. PIM1-IN-3 shows selective inhibition for the PIM-1 enzyme. PIM1-IN-3 induces apoptosis efficiently in Colo320 cells. PIM1-IN-3 has the potential for the research of cancer diseases.

Bufothionine is an alkaloid. Bufothionine can be isolated from Cinobufacini. Bufothionine induces mitochondria-mediated Apoptosis. Bufothionine significantly reduces serum IL-6 concentration, suppresses p-Stat3^tyr705, p-Stat3^ser727 and Jak2 expressions. Bufothionine upregulates Atg5, Atg7 and LC3Ⅱ expressions. Bufothionine induces Autophagy. Bufothionine suppresses PIM3 expression. Bufothionine relieves symptoms of H22-tumor-bearing mice and exerts anti-inflammation activity. Bufothionine exerts anti-cancer activities against gastric cancer.

Pim-1 kinase inhibitor 1 is a Pim-1 kinase inhibitor with an IC₅₀ of 0.11 μM for Pim-1 kinase. Pim-1 kinase inhibitor 1 shows anticancer activity to several cancer cell lines by promotes cell apoptosis. Pim-1 kinase inhibitor 1 can be used for the research of cancer.

Pim-1 kinase-IN-14 is a PIM-1 kinase inhibitor with an IC₅₀ value of 94 nM. Pim-1 kinase-IN-14 shows broad-spectrum and high-efficiency anticancer activity against multiple human cancer cell lines, including liver cancer (HepG-2), colon cancer (Caco-2), myeloid leukemia (NFS-60), and prostate cancer (PC-3) cells. Pim-1 kinase-IN-14exerts its anticancer effects by inducing apoptosis and activating caspase 3/7. Pim-1 kinase-IN-14 can be used for the study of cancers associated with PIM-1 kinase overexpression.

PIM-IN-4 is a Pim kinase inhibitor with K_i values of 2, 3, and 0.5 nM against Pim-1, 2, 3, respectively. PIM-IN-4 blocks the phosphorylation of the pro-apoptotic protein Bad. PIM-IN-4 inhibits the growth of leukemia cells. PIM-IN-4 is applicable for leukemia-related research.

Pim-1 kinase inhibitor 10 (compound 13a) is a both competitive and non-competitive inhibitor of PIM-1/2 kinase. Pim-1 kinase inhibitor 10 can induce cell apoptosis and exhibits anticancer activity. Pim-1 kinase inhibitor 10 also induces caspase 3/7 activation.

PIM-IN-6 is an inhibitor of PIM1 and PIM2, with an IC₅₀ of 254 nM against PIM1 and an IC₅₀ of 1.78 μM against PIM2. PIM-IN-6 can be used for the research of acute myeloid leukemia.

Uzansertib phosphate (Standard) is the analytical standard of Uzansertib phosphate (HY-101870B). This product is intended for research and analytical applications. Uzansertib (INCB053914) phosphate is an orally active, ATP-competitive pan-PIM kinase inhibitor with IC₅₀s of 0.24 nM, 30 nM, 0.12 nM for PIM1, PIM2, PIM3, respectively. Uzansertib phosphate has broad anti-proliferative activity against a variety of hematologic tumor cell lines.

Nuvisertib (Standard) (TP-3654 (Standard)) is the analytical standard of Nuvisertib (HY-101126). This product is intended for research and analytical applications. Nuvisertib (TP-3654) is an orally active second-generation pan-PIM kinase inhibitor with K_i values of 5 nM, 239 nM, and 42 nM against PIM-1, PIM-2, and PIM-3, respectively. Nuvisertib inhibits JAK-independent inflammatory and survival signaling pathways, reduces the production of proinflammatory cytokines, restores apoptotic sensitivity, inhibits mTORC1, MYC, and TGF-β signaling pathways, and decreases the expression of fibrosis markers. Nuvisertib selectively impairs the transport function of ABCG2, resensitizes multidrug-resistant cancer cells to cytotoxic drugs, and overcomes JAK2 inhibitor resistance. Nuvisertib can be used in research related to myelofibrosis, renal cell carcinoma, multidrug-resistant cancer, advanced solid tumors, urothelial carcinoma, and prostate adenocarcinoma.