Pim
Pim kinases
The PIM kinase, also known as serine/threonine kinase plays an important role in cancer biology and is found in three different isoforms namely PIM-1, PIM-2, and PIM-3. Pim kinases are mainly responsible for cell cycle regulation, antiapoptotic activity and the homing and migration of receptor tyrosine kinases mediated via the JAK/STAT pathway.
Pim kinases are over-expressed in various types of tumors and regulate the activation of signaling pathways that are important for tumor cell proliferation, survival and expression of drug efflux proteins. This makes Pim kinases attractive targets for the development of anti-cancer chemotherapeutic drugs.
Alle Pim Isoform-spezifische Produkte anzeigen
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Pim Verwandte Produkte (111)
Verwandte Produkte (111)
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Antibodies (3)
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Pim Isoform Comparison
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Nuvisertib
0 ImagesSynonyms: TP-3654Nuvisertib (TP-3654) is an orally active second-generation pan-PIM kinase inhibitor with Ki 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.
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CRT0066101 dihydrochloride
0 ImagesCRT0066101 dihydrochloride is a potent and orally active PKD inhibitor with IC50 values of 1 nM, 2.5 nM and 2 nM for PKD1, PKD2, and PKD3, respectively. CRT0066101 dihydrochloride is also a potent PIM2 inhibitor with an IC50 of ~135.7 nM. CRT0066101 dihydrochloride exhibits anti-inflammatory activity in mice LPS (HY-D1056)-induced lung injury models, and has anticancer effects.
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Pim-1 kinase-IN-17
0 ImagesArt. -Nr.: HY-184268Pim-1 kinase-IN-17 is a non-orthosteric inhibitor of PIM-1 onco-protein. Pim-1 kinase-IN-17 physically interacts with PIM-1 via a non-orthosteric binding site (Kd of 1.38 μM), does not inhibit PIM-1 kinase function, and decreases PIM-1 concentration under cellular conditions. Pim-1 kinase-IN-17 reduces tumor burden. Pim-1 kinase-IN-17 can be used for the research of triple-negative breast cancer.
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SGI-1776-amide-C6-acid
0 ImagesArt. -Nr.: HY-186147CAS. Nr.: 3013618-83-9
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Pim1/AAK1-IN-1
0 ImagesSynonyms: LKB1/AAK1 dual inhibitorPim1/AAK1-IN-1 is a potent multi-kinase inhibitor with Kd values of 35 nM/53 nM/75 nM/380 nM for Pim1/AAK1/MST2/LKB1 respectively, and also inhibits MPSK1 and TNIK.
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SMI-4a
0 ImagesSynonyms: TCS-PIM-1-4aSMI-4a (TCS-PIM-1-4a) is a poten, selective, cell-permeable and ATP-competitive Pim-1 inhibitor with an IC50 of 24 μM and a Ki of 0.6 μM. SMI-4a also inhibits Pim-2 (IC50 of 100 μM), and does not significantly inhibit the other serine/threonine- or tyrosine-kinases. SMI-4a has anticancer activity.
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RS47
0 ImagesRS47 is a selective RelB inhibitor with a Kd value of 1.1 μM. RS47 also acts as an inhibitor of HCV replication. RS47 can block the non-canonical NF-κB signaling pathway without affecting the canonical pathway. RS47 exerts anti-tumor effects of inhibiting proliferation and promoting apoptosis on colorectal cancer, B-cell lymphoma and other related tumors both in vitro and in vivo by disrupting the binding of RelB to target DNA. RS47 can be used for the research of tumors and infectious diseases.
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CRT0066101
0 ImagesCRT0066101 is a potent and orally active PKD inhibitor with IC50 values of 1 nM, 2.5 nM and 2 nM for PKD1, PKD2, and PKD3, respectively. CRT0066101 is also a potent PIM2 inhibitor with an IC50 of ~135.7 nM. CRT0066101 exhibits anti-inflammatory activity in mice LPS (HY-D1056)-induced lung injury models, and has anticancer effects.
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Quercetagetin
0 ImagesQuercetagetin (6-Hydroxyquercetin) is a flavonoid. Quercetagetin is a moderately potent and selective, cell-permeable pim-1 kinase inhibitor (IC50, 0.34 μM). Anti-inflammatory and anticancer properties.
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PIM-447 dihydrochloride
0 ImagesSynonyms: LGH447 dihydrochloridePIM447 dihydrochloride (LGH447 dihydrochloride) is a potent, orally available, and selective pan-PIM kinase inhibitor, with Ki values of 6, 18, and 9 pM for PIM1, PIM2, and PIM3, respectively. PIM447 dihydrochloride displays dual antimyeloma and bone-protective effects. PIM447 dihydrochloride induces apoptosis.
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CX-6258
0 ImagesCX-6258 is a potent and kinase selective pan-Pim kinases inhibitor, with IC50s of 5 nM, 25 nM and 16 nM for Pim-1, Pim-2 and Pim-3, respectively.
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TCS PIM-1 1
0 ImagesSynonyms: SC 204330TCS PIM-1 1 (SC 204330) is a potent, selective and ATP-competitive Pim-1 kianse inhibitor with an IC50 of 50 nM, displays good selectivity over Pim-2 and MEK1/MEK2 (IC50s >20000 nM).
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CK2/ERK8-IN-1
0 ImagesCK2/ERK8-IN-1 is a dual casein kinase 2 (CK2) (Ki of 0.25 µM) and ERK8 (MAPK15, ERK7) inhibitor with IC50s of 0.50 μM. CK2/ERK8-IN-1 also binds to PIM1, HIPK2 (homeodomain-interacting protein kinase 2), and DYRK1A with Kis of 8.65 µM, 15.25 µM, and 11.9 µM, respectively. CK2/ERK8-IN-1 has pro-apoptotic efficacy.
