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 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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