Pim
The PIM kinases, which constitute a class of serine/threonine kinase, act as oncoproteins and promote cell survival by transcriptional activation of genes involved in cell proliferation. The family of PIM kinase consists of three isoforms, PIM-1, PIM-2, and PIM-3. Each of the PIM kinases plays an important role in tumorigenesis. While PIM-1 has been reported to be over-expressed in several hematological and solid tumors PIM-2 is highly expressed in myeloma, lymphoma and leukemia. The elevated expression of PIM-3 has been noted in adeno-carcinomas. Diverse roles that the PIM kinases play in carcinogenesis include multiple myeloma proliferation, anti- apoptosis, cell cycle modulation, and mediating bone destruction.
PIM kinases could inhibit apoptosis and promote cell cycle progression in prostate cancer and their overexpression relates to the grade and neoplastic transformation. The overexpression of PIM-1 in breast cancer is related to poor prognosis in HER2- and hormone-negative tumors. Thus, PIM kinases play an important role in tumorigenesis. PIM kinases are involved in downstream physiological pathways via phosphorylating many cellular substrates, for example, transcriptional modulators including myelocytomatosis (MYC); cell cycle modulators including p21Cip1/Waf1 (CDKN1A), p27KIP1 (CDKN1B), and cell division cycle 25A (CDC25A) and 25C (CDC25C); signaling intermediates such as Notch homolog, translocation-associated (Notch1); and apoptosis modulators such as BCL-2-associated agonist of cell death (BAD).
Both the PIM family and protein kinase b (PKB)/AKT family belong to the serine/threonine protein kinases family and both play important roles in cancer development.35 PIM kinases have constitutive activity, and the half-lives of their mRNA and proteins are relatively short. EPH-like tyrosine kinase (ETK) phosphorylates PIM-1 at the Thr-218 residue, and this process is involved in the interlukin (IL)-6-induced activation of androgen-mediated transcription. Furthermore, protein phosphatase 2 (PP2A) can decrease the stability of PIM kinases. PIM kinases received much attention for anticancer drug development since they have aberrantly expressed in distinct cancer types.
References
1.Xinning Zhang,et al. J Cancer Prev. 2018 Sep; 23(3): 109–116.
PIM kinases could inhibit apoptosis and promote cell cycle progression in prostate cancer and their overexpression relates to the grade and neoplastic transformation. The overexpression of PIM-1 in breast cancer is related to poor prognosis in HER2- and hormone-negative tumors. Thus, PIM kinases play an important role in tumorigenesis. PIM kinases are involved in downstream physiological pathways via phosphorylating many cellular substrates, for example, transcriptional modulators including myelocytomatosis (MYC); cell cycle modulators including p21Cip1/Waf1 (CDKN1A), p27KIP1 (CDKN1B), and cell division cycle 25A (CDC25A) and 25C (CDC25C); signaling intermediates such as Notch homolog, translocation-associated (Notch1); and apoptosis modulators such as BCL-2-associated agonist of cell death (BAD).
Both the PIM family and protein kinase b (PKB)/AKT family belong to the serine/threonine protein kinases family and both play important roles in cancer development.35 PIM kinases have constitutive activity, and the half-lives of their mRNA and proteins are relatively short. EPH-like tyrosine kinase (ETK) phosphorylates PIM-1 at the Thr-218 residue, and this process is involved in the interlukin (IL)-6-induced activation of androgen-mediated transcription. Furthermore, protein phosphatase 2 (PP2A) can decrease the stability of PIM kinases. PIM kinases received much attention for anticancer drug development since they have aberrantly expressed in distinct cancer types.
References
1.Xinning Zhang,et al. J Cancer Prev. 2018 Sep; 23(3): 109–116.
Pim
-
Pim-1/2 kinase inhibitor 1
产品货号 : M37616
cas no: 6320-51-0
Pim-1/2 kinase inhibitor 1 是一种口服有效的 Pim-1/2 激酶抑制剂。Pim-1/2 kinase inhibitor 1 能阻断 Pim 激酶对肽的磷酸化能力,并且抑制 4E-BP1 和 p27Kip1 的 Pim 蛋白激酶定向磷酸化。Pim-1/2 kinase inhibitor 1 可用于癌症,尤其是前列腺癌的研究。 -
R8-T198wt
产品货号 : M30814
cas no: 2305815-72-7
Cell-permeable peptide inhibitor of Pim-1 kinase, derived from p27Kip1. Inhibits Pim-1 phosphorylation of p27Kip1 and Bad; induces cell cycle arrest (at G1) and apoptosis in DU145 prostate cancer cells. Also inhibits Pim-1-dependent growth of DU145 cells in vitro and in vivo. Displays no effect on the growth of normal prostate epithelial RPWE-1 cells at concentrations of 10 and 20 μM. -
1-phenoxazin-10-ylethanone
产品货号 : M28779
cas no: 6192-43-4
1-phenoxazin-10-ylethanone 是一种 Pim-2 抑制剂。 1-phenoxazin-10-ylethanone 诱导三阴性人类乳腺癌细胞凋亡和自噬性细胞死亡。 -
K00135
产品货号 : M27892
cas no: 869650-21-5
K00135 是 Pim 激酶的选择性抑制剂,可用于胃癌和抗白血病治疗的研究。 -
INCB053914 phosphate
产品货号 : M23938
cas no: 2088852-47-3
INCB053914 磷酸盐是一种口服活性、ATP 竞争性泛 PIM 激酶抑制剂。