p27kip1

SJ572403 is an inhibitor of disordered protein p27 with Kd of 2.2 mM for specific regions within the D2 subdomain of p27-KID. SJ572403 can be used in studies about diseases with intrinsically disordered proteins.

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 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].

CC0651 is an allosteric inhibitor of the human Cdc34 ubiquitin-conjugating enzyme that potently inhibits the ubiquitination of p27Kip1 (IC50: 1.72 μM).

NSC-689857 is an inhibitor that acts in the Skp2-Cks1 protein-protein interaction and p27Kip1 ubiquitination in vitro.

CEP-1612 is a proteasomal inhibitor responsible for the proteolysis of proteins that regulate important cell cycles and apoptosis. CEP-1612 can induce p21WAF1 and p27KIP1 expression and apoptosis, and inhibit tumor growth of human lung cancer.

Tpl2 kinase inhibitor is an inhibitor of tumor progression locus 2 (Tpl2; IC50= 0.05 μM).1It is selective for Tpl2 over MEK, p38 MAPK, Src, MK2, and PKC (IC50s = >40, 180, >400, 110, and >400 μM, respectively). Tpl2 kinase inhibitor inhibits LPS-induced TNF-α production in isolated human monocytes and whole blood (IC50s = 0.7 and 8.5 μM, respectively). It enhances differentiation induced by calcitriol in HL-60 and U937 leukemia cells when used at a concentration of 5 μM.2Tpl2 kinase inhibitor (5 μM) inhibits the proliferation of KG-1a leukemia cells.3 1.Garvin, L.K., Green, N., Hu, Y., et al.Inhibition of Tpl2 kinase and TNF-α production with 1,7-naphthyridine-3-carbonitriles: Synthesis and structure-activity relationshipsBioor. Med. Chem. Lett.15(23)5288-5292(2005) 2.Wang, X., and Studzinski, G.P.Expression of MAP3 kinase COT1 is up-regulated by 1,25-dihydroxyvitamin D3 in parallel with activated c-jun during differentiation of human myeloid leukemia cellsJ. Steroid. Biochem. Mol. Biol.121(1-2)395-398(2010) 3.Wang, X., Gocek, E., Novik, V., et al.Inhibition of Cot1/Tlp2 oncogene in AML cells reduces ERK5 activation and up-regulates p27Kip1 concomitant with enhancement of differentiation and cell cycle arrest induced by silibinin and 1,25-dihydroxyvitamin D3Cell Cycle9(22)4542-4551(2010)

Argyrin A is a cyclic peptide and potent antitumor agent. It functions by inhibiting the proteasome (proteasome), leading to increased levels of endogenous p27kip1 by preventing protein turnover.

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