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Pim-1kinase inhibitor 8 (compound 12) is a potent inhibitor of Pim-1kinase with an IC50 of 14.3 nM. Pim-1kinase inhibitor 8 has potent cytotoxicity against MCF-7 and HepG2 cells with IC50s of 0.5 and 5.27 μM, respectively. Pim-1kinase inhibitor 8 can used in study breast cancer .
Pim-1kinase inhibitor 9 (compound 8b) is a selective inhibitor against Pim-1kinase with IC50value of 0.24 µM. Pim-1kinase inhibitor 9 inhibits cell cycle of T47D at S phase. Pim-1kinase inhibitor 9 reveals antitumor activity .
Pim-1kinase inhibitor 2 (Compound 13) is a potent inhibitor of Pim-1kinase. Pim-1kinase inhibitor 2 induces apoptosis. Pim-1kinase inhibitor 2 has the potential for the research of cancer diseases .
Pim-1kinase inhibitor 1 is a Pim-1kinase inhibitor with an IC50 of 0.11 μM for Pim-1kinase. Pim-1kinase inhibitor 1 shows anticancer activity to several cancer cell lines by promotes cell apoptosis. Pim-1kinase inhibitor 1 can be used for the research of cancer .
Pim-1kinase inhibitor 4 (Compound 10f) is a Pim-1kinase inhibitor (IC50: 17.01 nM). Pim-1kinase inhibitor 4 also has antioxidant activity and inhibits DPPH. Pim-1kinase inhibitor 4 induces apoptosis in PC-3 cell, and inhibits PC-3 cell growth with an IC50 of 16 nM. Pim-1kinase inhibitor 4 can be used for research of prostate cancer .
Pim-1kinase inhibitor 10 (compound 13a) is a both competitive and non-competitive inhibitor of PIM-1/2 kinase. Pim-1kinase inhibitor 10 can induce cell apoptosis and exhibits anticancer activity. Pim-1kinase inhibitor 10 also induces caspase 3/7 activation .
Pim-1kinase inhibitor 6 (Compound 4d) is a potent Pim-1kinase inhibitor with IC50 value of 0.46 μM, and has significant cytotoxic effect on cancer cells .
Pim-1kinase inhibitor 5 (Compound 4c) is a Pim-1kinase inhibitor (IC50: 0.61 μM). Pim-1kinase inhibitor 5 shows cytotoxicity against cancer cells, with IC50s of 6.95-20.19 μM for HepG2, MCF-7, PC3, and HCT-116 cells .
Pim-1/2 kinase inhibitor 2 (compound 5b) is a competitive PIM-1 and PIM-2 kinase inhibitor with IC50s of 1.31 μM and 0.67 μM, respectively. Pim-1/2 kinase inhibitor 2 shows in-vitro low cytotoxicity against normal human lung fibroblast Wi-38 cell line and potent in-vitro anticancer activity against myeloid leukaemia (NFS-60), liver (HepG-2), prostate (PC-3), and colon (Caco-2) cancer cell lines .
NDBM is a probe and binds to tumor-specific Pim-1kinase, releases strong fluorescence, and produces cytotoxicity, thus achieving cell screening and killing effects. NDBM can specifically target lysosomes and sensitively respond to pH. NDBM can be used to track the pH changes in the intracellular environment under conditions of autophagy and external stimulation .
Pim-1/2 kinase inhibitor 1 is an orally active pim-1/2 kinase inhibitor. Pim-1/2 kinase inhibitor 1 blocks the ability of Pimkinases to phosphorylate peptides, and inhibits the pim protein kinase directed phosphorylation of 4E-BP1 and p27 Kip1. Pim-1/2 kinase inhibitor 1 can be used in study of cancer, especially prostate cancer .
PIM1-IN-2 is a potent and ATP competitive Pim-1 inhibitor with a Ki of 91 nM. PIM1-IN-2 targets the ATP-binding kinase hinge region not by forming classical hydrogen bonds .
CK2/PIM1-IN-1 is an inhibitor of CK2 and PIM1, with IC50s of 3.787 μM and 4.327 μM for CK2 and PIM1, respectively. CK2/PIM1-IN-1 is developed for the research of proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation, pain, vascular disorders, pathogenic infections and certain immunological disorders .
Pim1/AKK1-IN-1 is a potent multi-kinase inhibitor with Kd values of 35 nM/53 nM/75 nM/380 nM for Pim1/AKK1/MST2/LKB1 respectively, and also inhibits MPSK1 and TNIK.
CX-6258 hydrochloride hydrate is a potent and kinase selective pan-Pimkinases inhibitor, with IC50s of 5 nM, 25 nM and 16 nM for Pim-1, Pim-2 and Pim-3, respectively .
CX-6258 hydrochloride is a potent and kinase selective pan-Pimkinases inhibitor, with IC50s of 5 nM, 25 nM and 16 nM for Pim-1, Pim-2 and Pim-3, respectively .
Quercetagetin (6-Hydroxyquercetin) is a flavonoid . Quercetagetin is a moderately potent and selective, cell-permeable pim-1kinase inhibitor (IC50, 0.34 μM) . Anti-inflammatory and anticancer properties.
Quercetagetin (Standard) is the analytical standard of Quercetagetin. This product is intended for research and analytical applications. Quercetagetin (6-Hydroxyquercetin) is a flavonoid . Quercetagetin is a moderately potent and selective, cell-permeable pim-1kinase inhibitor (IC50, 0.34 μM) . Anti-inflammatory and anticancer properties.
SMI-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 .
M-110 is a highly selective, ATP-competitive inhibitor of PIMkinases with a preference for PIM-3 (IC50=47 nM). M-110 inhibits PIM-1 and PIM-2 with similar IC50s of 2.5 μM. M-110 inhibits the proliferation of prostate cancer cell lines with IC50s of 0.6 to 0.9 μM .
GDC-0339 is a potent, orally bioavailable and well tolerated pan-Pimkinase inhibitor, with Kis of 0.03 nM, 0.1 nM and 0.02 nM for Pim1, Pim2 and Pim3, respectively. GDC-0339 is discovered as a potential treatment of multiple myeloma .
PIM447 dihydrochloride (LGH447 dihydrochloride) is a potent, orally available, and selective pan-PIMkinase 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 .
PIM447 (LGH447) is a potent, orally available, and selective pan-PIMkinase inhibitor, with Ki values of 6, 18, and 9 pM for PIM1, PIM2, and PIM3, respectively. PIM447 displays dual antimyeloma and bone-protective effects. PIM447 induces apoptosis .
Uzansertib (INCB053914) phosphate is an orally active, ATP-competitive pan-PIMkinase 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 .
Uzansertib (INCB053914) is an orally active, ATP-competitive pan-PIMkinase inhibitor with IC50s of 0.24 nM, 30 nM, 0.12 nM for PIM1, PIM2, PIM3, respectively. Uzansertib has broad anti-proliferative activity against a variety of hematologic tumor cell lines .
HTH-01-091 is a potent and selective maternal embryonic leucine zipper kinase (MELK) inhibitor, with an IC50 of 10.5 nM. HTH-01-091 also inhibits PIM1/2/3, RIPK2, DYRK3, smMLCK and CLK2. HTH-01-091 can be uesd for breast cancer research .
HTH-01-091 TFA is a potent and selective maternal embryonic leucine zipper kinase (MELK) inhibitor, with an IC50 of 10.5 nM. HTH-01-091 TFA also inhibits PIM1/2/3, RIPK2, DYRK3, smMLCK and CLK2. HTH-01-091 TFA can be uesd for breast cancer research .
AZD1897 is a PIM1, PIM2, and PIM3 inhibitor with IC50 values of less than 3 nM for these three PIMkinases. AZD1897 exhibits anticancer activity and synergistically inhibits the activity of acute myeloid leukemia (AML) cells in combination with Capivasertib (HY-15431). This synergistic inhibitory effect is achieved through the inhibition of the mTOR and MCL1 pathways .
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 .
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 .
CK2/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 .
Quercetagetin (6-Hydroxyquercetin) is a flavonoid . Quercetagetin is a moderately potent and selective, cell-permeable pim-1kinase inhibitor (IC50, 0.34 μM) . Anti-inflammatory and anticancer properties.
Quercetagetin (Standard) is the analytical standard of Quercetagetin. This product is intended for research and analytical applications. Quercetagetin (6-Hydroxyquercetin) is a flavonoid . Quercetagetin is a moderately potent and selective, cell-permeable pim-1kinase inhibitor (IC50, 0.34 μM) . Anti-inflammatory and anticancer properties.
The PIM1 protein is a proto-oncogene with serine/threonine kinase activity that significantly promotes cell survival and proliferation, providing a selective advantage for tumorigenesis. It regulates MYC transcription, cell cycle progression, and inhibits pro-apoptotic proteins such as BAD, MAP3K5, and FOXO3 through phosphorylation. PIM1 Protein, Human is the recombinant human-derived PIM1 protein, expressed by E. coli , with tag free. The total length of PIM1 Protein, Human is 300 a.a., .
PIM1 Antibody (YA2502) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA2502), targeting PIM1, with a predicted molecular weight of 36 kDa (observed band size: 36 kDa). PIM1 Antibody (YA2502) can be used for WB, IHC-P experiment in human background.
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