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Catalog No.
Product Name
Application
Product Information
Citations
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PIM-1 Inhibitor
PIM1-IN-6 is a potent inhibitor of Pim-1 kinase, exhibiting an IC50 of 0.60 μM. This compound demonstrates significant cytotoxic activity in HCT-116 and MCF-7 cancer cell lines, with IC50 values of 1.51 μM and 15.2 μM, respectively. PIM1-IN-6 holds promise for research applications in cancer biology, particularly in studies aimed at elucidating the role of Pim-1 in tumor proliferation and survival. -
Pim-1 Kinase Inhibitor
10-DEBC is a selective inhibitor of Pim-1 kinase, demonstrating potent inhibitory activity with an IC50 of 1.28 μM. This compound plays a critical role in regulating cell proliferation and survival, making it a valuable tool for research in cancer biology and therapeutic interventions. Its specificity for Pim-1 kinase supports its use in studies exploring signal transduction pathways and the development of targeted cancer therapies. -
PIM1 Inhibitor
PIM1-IN-4 is a selective inhibitor of PIM1 kinase, demonstrating potent activity in blocking PIM1-mediated signaling. In addition to PIM1, PIM1-IN-4 exhibits significant inhibition of several other kinases, including SGK-1, PKA, CaMK-1, GSK3β, and MSK1. This compound is valuable for investigating its role in cancer biology and therapeutic strategies targeting PIM1-related pathways. -
Pim-1 Inhibitor
Pim-1 kinase inhibitor 3 (Compound H5) is a selective inhibitor of Pim-1 kinase, exhibiting an IC50 of 35.13 nM. This compound effectively modulates the activity of Pim-1, a serine/threonine kinase involved in cell growth and survival signaling pathways. It is valuable for studying the role of Pim-1 in cancer and other diseases where its dysregulation is implicated. -
Pim Inhibitor
MNK/PIM-IN-1 is a dual inhibitor targeting MNK and PIM kinases, showcasing a favorable pharmacokinetic profile. This reagent exhibits significant antitumor activity and is applicable in studying the roles of MNK and PIM signaling pathways in cancer biology. It is an essential tool for researchers investigating the mechanisms of cell proliferation and survival in various malignancies. -
PIM1 Inhibitor
NMS-P645 is a potent PIM1 inhibitor that exhibits anti-proliferative activity, particularly when used in combination with GDC-0941 in both TMPRSS2/ERG positive and negative prostate cancer cells. By reversing PIM1-induced pro-survival signals, NMS-P645 contributes valuable insights into the mechanisms underlying prostate cancer resistance and cell survival. This compound is suitable for research applications focused on prostate cancer treatment and the exploration of PIM1 signaling pathways. -
Pim-1 Kinase Inhibitor
Pim-1 kinase inhibitor 4 is a potent inhibitor of Pim-1 kinase, with an inhibitory concentration (IC50) of 17.01 nM. This compound exhibits antioxidant activity and inhibits DPPH, contributing to its biological profile. Additionally, Pim-1 kinase inhibitor 4 induces apoptosis in PC-3 prostate cancer cells, demonstrating an IC50 of 16 nM for growth inhibition. This reagent is valuable for research focused on prostate cancer and cellular apoptosis mechanisms. -
Pim-2 Inhibitor
PIM-IN-2 is a potent inhibitor of Pim-2 kinases, exhibiting an IC50 of 25 nM. This compound has demonstrated significant antiapoptotic properties and promotes cell survival, making it a valuable tool in cancer research. Its elevated expression in various human tumors positions PIM-IN-2 as a relevant reagent for studies on tumor biology and therapeutic strategies targeting the Pim kinase pathway. -
Pim-1 Inhibitor
Pim-1 kinase inhibitor 6 is a selective inhibitor of Pim-1 kinase, demonstrating an IC50 value of 0.46 μM. This compound exhibits significant cytotoxic activity against various cancer cell lines, making it a valuable tool for cancer research. Its ability to target and inhibit Pim-1 kinase contributes to its potential applications in investigating therapeutic strategies for malignancies. -
Pim Inhibitor
PIM-IN-4 is a potent inhibitor of Pim kinases, exhibiting Ki values of 2 nM, 3 nM, and 0.5 nM for Pim-1, Pim-2, and Pim-3, respectively. By inhibiting the phosphorylation of the pro-apoptotic protein Bad, PIM-IN-4 effectively induces apoptosis in leukemic cells. This compound is valuable for research into leukemia and related signaling pathways, contributing to the understanding of therapeutic strategies in hematological malignancies. -
PIM-1/PIM-2 Inhibitor
Pim-1/2 kinase inhibitor 2 is a selective competitive inhibitor of PIM-1 and PIM-2 kinases, with IC50 values of 1.31 μM and 0.67 μM, respectively. This compound exhibits low cytotoxicity in normal human lung fibroblast Wi-38 cells while demonstrating potent anticancer activity against various cancer cell lines, including myeloid leukemia (NFS-60), liver (HepG-2), prostate (PC-3), and colon (Caco-2). It serves as a valuable tool for studying the therapeutic potential of PIM inhibition in cancer research. -
EGFR Inhibitor
Afatinib N-Oxide is an oxidative degradation product of Afatinib dimaleate, an irreversible inhibitor of the epidermal growth factor receptor (EGFR) family. This compound serves as a valuable tool for characterizing the stability and degradation pathways of Afatinib in chemical research. It may also aid in understanding the mechanistic effects of EGFR inhibition in various biological contexts. -
JAK/STAT Inhibitor
Phenylpyropene C is a JAK/STAT pathway inhibitor known to effectively inhibit interferon-gamma (IFN-γ) mediated expression of reporter genes, with an IC50 range of 5.4 to 10.8 μM. Additionally, it serves as an inhibitor of acyl-CoA, exhibiting an IC50 of 16.0 μM. This compound is valuable for research applications focusing on the modulation of immune responses and the exploration of cytokine signaling pathways. -
EGFR inhibitor
CHMFL-EGFR-202 is a potent, irreversible inhibitor of epidermal growth factor receptor (EGFR) mutant kinase, with IC50s of 5.3 nM and 8.3 nM for drug-resistant mutant EGFR T790M and WT EGFR kinases, respectively. -
pan-JAK inhibitor
PF-06263276 (PF 6263276) is a potent and selective pan-JAK inhibitor, with IC50s of 2.2 nM, 23.1 nM, 59.9 nM and 29.7 nM for JAK1, JAK2, JAK3 and TYK2, respectively. -
PKC inhibitor
PKC 412 is a broad spectrum protein kinase inhibitor. Inhibits conventional PKC isoforms α/β/γ, PDFRβ, VEGFR2, Syk, Flk-1, Flt3, Cdk1/B, PKA, c-Kit, c-Fgr, c-Src, VEGFR1 and EGFR. Displays potent antitumor activity. -
ErbB inhibitor
ARRY-543 is a novel, oral ErbB family inhibitor that, unlike approved ErbB inhibitors, targets all members of the ErbB family, including ErbB3, either directly or indirectly, and has potential advantages in treating tumors that signal through multiple ErbB family members. -
Pdia3/ERp57 activator, STAT3 inhibitor
Diosgenin glucoside, a saponin compound extracted from Tritulus terrestris L., provides neuroprotection by regulating microglial M1 polarization. Diosgenin glucoside protects against spinal cord injury by regulating autophagy and alleviating apoptosis . -
EGFR inhibitor
CO-1686 is a novel, oral, targeted covalent (irreversible) inhibitor of the cancer-causing mutant forms of epidermal growth factor receptor (EGFR) currently being studied for the treatment of non-small cell lung cancer (NSCLC). -
EGFR inhibitor
CL-387785 is an irreversible inhibitor of EGFR with IC50 of 370+/-120 pM; is able to overcome resistance caused by the T790M mutation on a functional level. -
JAK2/HDAC dual inhibitor
JAK/HDAC-IN-1 is a potent JAK2/HDAC dual inhibitor, exhibits antiproliferative and proapoptotic activities in several hematological cell lines. -
JAK inhibitor
NVP-BSK805 is a potent and selective inhibition of polycythemia by the quinoxaline JAK2 inhibitor that potently suppressed recombinant human erythropoietin-induced polycythemia and extramedullary erythropoiesis in mice and rats.
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EGFR Inhibitor
BMS 599626 is an orally bioavailable inhibitor of the HER1, HER2 and HER4 tyrosine kinases (IC50=22, 32 and 190 nM, respectively) with potential antineoplastic activity. -
HER2/EGFR inhibitor
TAK-285 is an investigational HER2/EGFR inhibitor that penetrates the CNS in Rats with an Intact Blood Brain Barrier (BBB). TAK-285 has inhibitory activity against HER2 and EGFR kinases with IC50 values for HER2 and EGFR of 17 nmol/L (95% CI 12-24) and 23 nmol/L (95% CI 18-30), respectively.[1] -
JAK inhibitor
BMS-911543 is an orally available small molecule targeting a subset of Janus-associated kinase (JAK) with potential antineoplastic activity. -
multi-kinase inhibitor
Cenisertib (AS-703569) is a multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3. -
VEGFR/EGFR Inhibitor
BMS-690514 is a potent and selective inhibitor of epidermal growth factor receptor (EGFR), HER2, and HER4, as well as the VEGF receptor kinases. -
multi-kinase inhibitor
Lestaurtinib (CEP-701;KT-5555) is a multi-kinase inhibitor with potent activity against the Trk family of receptor tyrosine kinases. Lestaurtinib inhibits JAK2, FLT3 and TrkA with IC50s of 0.9, 3 and less than 25 nM, respectively. -
EGFR inhibitor
BIBX 1382 is a cell-permeable pyrimidopyrimidine compound that acts as a potent, reversible, ATP-competitive, and highly selective inhibitor of EGFR. -
EGFR inhibitor
Canertinib dihydrochloride (CI-1033 dihydrochloride) is a potent and irreversible EGFR inhibitor; inhibits cellular EGFR and ErbB2 autophosphorylation with IC50s of 7.4 and 9 nM. -
JAK1/2 inhibitor
Ruxolitinib sulfate (INCB018424 sulfate) is the first potent, selective JAK1/2 inhibitor to enter the clinic with IC50s of 3.3 nM/2.8 nM, and has > 130-fold selectivity for JAK1/2 versus JAK3. -
LKB1/AAK1 dual inhibitor
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. -
JAK inhibitor
Ruxolitinib Phosphate is the phosphate salt form of ruxolitinib, an orally bioavailable Janus-associated kinase (JAK) inhibitor with potential antineoplastic and immunomodulating activities. -
EGFR inhibitor
AG-17 is an inhibitor of EGF receptor kinase with an IC50 value of 460 μM in the human epidermoid carcinoma cell line A431. -
FLT3 inhibitor
TG-02 is a novel small molecule potent CDK/JAK2/FLT3 inhibitor. -
Pim inhibitor
TCS PIM-1 4a is a selective and ATP-competitive Pim kinase inhibitor (IC50 values = 24 and 100 nM for Pim-1 and Pim-2, respectively). -
CDK/JAK2/FLT3 inhibitor
SB1317 is a potent inhibitor of Cyclin dependent kinases (CDKs), FMS-like tyrosine kinase-3 (FLT3) and Janus kinase 2 (JAK2) with IC50 values of 13nM, 56nM and 73nM for CDK2, JAK2 and FLT3, respectively. -
STAT inhibitor
Napabucasin is an orally-administered small molecule which can block cancer stem cell (CSC) self-renewal and induces cell death in CSCs as well as non-stem cancer cells.
