About 27 results found for searched term "TIM-3-IN-2" (0.21 seconds)
Cat.No. | Name | Target |
---|---|---|
M42061 | TIM-3-IN-2 | Others |
TIM-3-IN-2 is a Tim3 inhibitor (KD: 0.61 μM). TIM-3-IN-2 inhibits the immunosuppressive function of TIM-3. TIM-3-IN-2 reverses the TIM-3-mediated blockade of the production of proinflammatory cytokines, and maximizes the T-cell antitumor activity against AML cell lines. | ||
M6127 | TD-4208 | AChR/AChE |
Revefenacin; GSK1160724 | ||
Revefenacin (TD-4208; GSK1160724) is a novel and potent muscarinic receptor antagonist that has a high affinity and long residence time at the M3 receptor, and demonstrates in vitro kinetic selectivity for M3 over M2 muscarinic receptor subtype and no meaningful off-target activity. | ||
M6161 | GSK369796 Dihydrochloride | Potassium Channel |
GSK369796 shows antimalerial activity with IC50 values of 11.2 nM for 3D7 strain, 12.6 nM for HB3 strain, 17.6 nM for K1 strain. | ||
M10734 | YKL-5-124 | CDK |
YKL-5-124 is a potent, selective, irreversible COVALENT inhibitor of CDK7 and CDK7/Mat1/CycH IC50 53.5 nM and 9.7 nM, respectively. YKL-5-124 is more than 100 times more selective to CDK7 than CDK9 and CDK2 and is inactive to CDK12 and CDK13. YKL-5-124 induces intense cell cycle arrest and inhibits E2F-driven gene expression with little effect on RNA polymerase II phosphorylation status. | ||
M10824 | GSK2245035 | TLR |
GSK2245035 is a highly potent, selective intranasal Toll-Like receptor 7 (TLR7) agonist with preferential stimulation of interferon type 1 (IFN). GSK2245035 for IFNα and TNFα pEC50 9.3 and 6.5, respectively. GSK2245035 effectively inhibits allergen-induced Th2 cytokine production in human peripheral blood cell cultures. GSK2245035 has the potential for asthma. | ||
M11418 | SAR-020106 | Checkpoint |
Sar-020106 is an ATP-competitive and selective CHK1 inhibitor with an IC50 of 13.3 nM. Sar-020106 has good selectivity to CHK2. Sar-020106 increased cell lethality of Gemcitabine and SN38 by 3.0 to 29 times in a p53-dependent manner in several colon cancer cell lines. Sar-020106 can enhance antitumor activity by selecting anticancer drugs. | ||
M14856 | Quercetin dihydrate | PI3K |
Quercetin dihydrate, a natural flavonoid, is a stimulator of recombinant SIRT1 and a PI3K inhibitor with IC50s of 2.4 μM, 3.0 μM and 5.4 μM for PI3K γ, PI3K δ and PI3K β, respectively. | ||
M21210 | Recombinant Mouse IL-3 (E. coli) | Cytokines and Growth Factors |
IL3; interleukin 3; IL-3; MCGF | ||
Interleukin-3 (IL-3) is a pleiotropic cytokine belonging to the interleukin family. IL-3 stimulates the development and colony formation of multiple lineages of hematopoietic cells by activating intracellular pathways such as Ras-Raf-ERK and JAK/STAT. IL-3 inhibits apoptosis and promotes cell survival by targeting the anti-apoptotic bcl-2 gene family. | ||
M21442 | Recombinant Mouse G-CSF (CHO) | Cytokines and Growth Factors |
CSF3; C17orf33; CSF3OS; GCSF | ||
Granulocyte Colony-Stimulating Factor (G-CSF), also known as CSF-3 and MGI-1G, is a cytokine and hormone belonging to the IL-6 superfamily. It is expressed by monocytes, macrophages, endothelial cells, fibroblasts and bone marrow stroma. ED50 < 0.02 ng/ml | ||
M21546 | Recombinant Mouse IL-3 (HEK293, C-6His) | Cytokines and Growth Factors |
IL3; interleukin 3; IL-3; MCGF; MULTI-CSF; Mast cell growth factor | ||
Interleukin-3 (IL-3) is a pleiotropic cytokine belonging to the interleukin family. IL-3 stimulates the development and colony formation of multiple lineages of hematopoietic cells by activating intracellular pathways such as Ras-Raf-ERK and JAK/STAT. IL-3 inhibits apoptosis and promotes cell survival by targeting the anti-apoptotic bcl-2 gene family. | ||
M21677 | Recombinant Human Follistatin 288 (HEK293, C-6His) | Cytokines and Growth Factors |
FST; follistatin isoform FST317 | ||
Follistatin 288 is a secreted glycoprotein that was first identified as a follicle-stimulating hormone inhibiting substance in ovarian follicular fluid . Human follistatin 288 cDNA encodes a 317 amino acid (aa) protein with a 29 aa signal sequence, and a 288 aa mature region. Recombinant Human Follistatin/FST is produced by Mammalian expression system and the target gene encoding Gly30-Asn317 is expressed with a 6His tag at the C-terminus. | ||
M24546 | Timolumab | Others |
BTT 1023; Anti-Human AOC3 Recombinant Antibody | ||
Timolumab (BTT1023 ), a recombinant fully human monoclonal antibody that specifically binds VAP-1. Timolumab (BTT1023 ) could be used in the study of chronic inflammatory diseases. | ||
M24621 | Margetuximab | EGFR/HER2 |
Margetuximab (MGAH22) is a chimeric anti-HER2 monoclonal antibody optimized Fc domain, with an EC50 value of 39.33 ng/mL. Margetuximab can be used for researching metastatic HER2-positive breast cancer. | ||
M27703 | Dagrocorat | GCR |
PF-00251802 | ||
Dagrocorat (PF-00251802) is an orally active and selective high-affinity partial agonist of the glucocorticoid receptor. Dagrocorat is also a time-dependent reversible inhibitor of CYP3A (IC50=1.3 μM in human liver microsomes) and CYP2D6 (Ki=0.57 μM in human liver microsomes). Dagrocorat can be used for the research of rheumatoid arthritis. | ||
M27705 | Dagrocorat hydrochloride | GCR |
PF-00251802 hydrochloride | ||
Dagrocorat (PF-00251802) hydrochloride is an orally active and selective high-affinity partial agonist of the glucocorticoid receptor. Dagrocorat hydrochloride is also a time-dependent reversible inhibitor of CYP3A (IC50=1.3 μM in human liver microsomes) and CYP2D6 (Ki=0.57 μM in human liver microsomes). Dagrocorat hydrochloride can be used for the research of rheumatoid arthritis. | ||
M27824 | Dynole 34-2 | Dynamin |
Dynole 34-2 is a dynamin GTPase inhibitor (IC50s=6.9 and 14.2 µM for dynamin1 and dynamin2 GTPase activity, respectively) with antimitotic effect. Dynole 34-2 induces apoptosis, as revealed by cell blebbing, DNA fragmentation, and PARP cleavage. Dynole 34-2 also potently inhibits receptor mediated endocytosis (RME). | ||
M28998 | Pactimibe | Transferase |
CS-505 free base | ||
Pactimibe (CS-505) free base is a dual ACAT1/2 inhibitor with IC50s of 4.9 μM and 3.0 μM, respectively. Pactimibe (CS-505) free base inhibits ACAT with IC50s of 2.0 μM, 2.7 μM, 4.7 μM in the liver, macrophages and THP-1 cells, respectively. Pactimibe (CS-505) free base noncompetitively inhibits oleoyl-CoA with a Ki value of 5.6 μM. | ||
M29603 | FAK inhibitor 6 | FAK |
Compound 26F not only optimized the effective inhibitory enzyme (ic50= 28.2 nm), but also showed relatively less cytotoxicity (ic50= 3.32 μ M) And induced MDA-MB-231 cell apoptosis in a dose-dependent manner, effectively blocking MDA-MB-231 cells in g0/g1 phase. | ||
M29668 | YS-370 | P-glycoprotein |
YS-370 (compound 44) is a potent, high selective, and orally active inhibitor of P-glycoprotein (P-gp). YS-370 stimulates the P-gp ATPase activity and has moderate inhibition against CYP3A4. YS-370 effectively reverses multidrug resistance (MDR) to paclitaxel and colchicine in SW620/AD300 and HEK293T-ABCB1 cells. YS-370 in combination with paclitaxel achieves much stronger antitumor activity. | ||
M30242 | Methoxy-PEPy | GluR |
Methoxy-PEPy is a potent and highly selective mGlu5 receptor antagonist with IC50 of 1 nM. IC50 value: 1 nM [1] Target: mGlu5R inhibitor Administration of [3H]methoxy-PEPy (50 microCi/kg i.v.) to mGlu5 receptor-deficient mice revealed binding at background levels in forebrain, whereas wild-type mice exhibited 14-fold higher binding in forebrain relative to cerebellum . The calcium transients stimulated by these agonists were potently inhibited by reference allosteric mGlu5 antagonists - 2-methyl-6-(phenylethynyl)pyridine (MPEP), 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine (MTEP) and 3-methoxy-5-(pyridine-2-ylethynyl)pyridine (methoxy-PEPy) (IC(50) ranges: 0.8-66 nM) . | ||
M30357 | Pactimibe sulfate | Transferase |
CS-505 | ||
Pactimibe sulfate (CS-505) is a dual ACAT1/2 inhibitor with IC50s of 4.9 μM and 3.0 μM, respectively. Pactimibe sulfate (CS-505) inhibits ACAT with IC50s of 2.0 μM, 2.7 μM, 4.7 μM in the liver, macrophages and THP-1 cells, respectively. Pactimibe sulfate (CS-505) noncompetitively inhibits oleoyl-CoA with a Ki value of 5.6 μM. | ||
M30649 | C188 | STAT |
CPD188 | ||
C188 is a STAT3 inhibitor that inhibits IL-6-stimulated STAT3 phosphorylation and nuclear translocation in HepG2 cells by targeting STAT3 SH2 domain peptide-binding pocket. C188, in particular, was highly active in inducing apoptosis of the breast cancer cell line MB-MDA-468 in vitro (EC50= 0.7 μM). | ||
M38782 | Antimalarial agent 12 | Parasite |
Antimalarial agent 12 is a potent antimalarial agent. Antimalarial agent 12 shows growth inhibition on P. falciparum Dd2 Strain (EC50=155 nM), 3D7 strain (EC50=136 nM). Antimalarial agent 12 has CC50 values of 10,000 to 50,000 nM for HEK-293 and hPHep cell lines. | ||
M40653 | A2AR-antagonist-1 | Adenosine Receptor |
A2AR-antagonist-1 is an orally active adenosine receptor A2AR antagonist with an IC50 value of 29 nM.A2AR-antagonist-1 is also a T-cell activator that acts by inhibiting immunosuppressive molecules (LAG-3 and TIM-3) and potentiating effector molecules (GZMB, IFNG and IL-2). It has antitumor activity and is metabolically stable in mouse liver microsomes. | ||
M45092 | (R)-GSK-3685032 | DNA Methyltransferase |
(R)-GSK-3685032 is the R-isomer of GSK-3685032.GSK-3685032 is a non-time-dependent, non-covalent, first-in-class, reversible selective inhibitor of DNMT1 with an IC50 value of 0.036 μM.GSK-3685032 induces DNA GSK-3685032 induces loss of DNA methylation, transcriptional activation and cancer cell growth inhibition. | ||
M45093 | (S)-GSK-3685032 | DNA Methyltransferase |
(S)-GSK-3685032 is the inactive isomer of GSK-3685032.GSK-3685032 is a non-time-dependent, non-covalent, first-in-class, reversible selective inhibitor of DNMT1 with an IC50 value of 0.036 μM.GSK-3685032 induces DNA GSK-3685032 induces loss of DNA methylation, transcriptional activation and cancer cell growth inhibition. | ||
M54722 | Fluoflavine | NADPH Oxidase |
ML-090 | ||
Fluoflavine is a selective NOX1 inhibitor with an IC50 value of 90 nM.Fluoflavine is >100 times more selective for NOX1 than NOX2, NOX3, NOX4, and has an IC50 >10 μM for all of them.Fluoflavine was shown to be a selective inhibitor of NOX1 with an IC50 of 360 nM in HEK293 cells. |
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