About 34 results found for searched term "TS-IN-2" (0.224 seconds)
| Cat.No. | Name | Target |
|---|---|---|
| M4067 | Ginsenoside-Rg2 | NF-κB |
| Chikusetsusaponin I; Panaxoside Rg2; Prosapogenin C2 | ||
| Ginsenoside-Rg2 is one of the major active components of ginseng, acts as a NF-κB inhibitor. | ||
| M21451 | Recombinant Human Cathepsin K protein (E.coli) | Cytokines and Growth Factors |
| CTSK；Cathepsin K；Cathepsin O；Cathepsin O2 | ||
| Protein construction: The DNA sequence encoding human CTSK (Ala115-Met329) is fused with His tag. Accession #P43235. | ||
| M41372 | TS-IN-2 | Others |
| TS-IN-2 is a thymidylate synthase (TS) inhibitor with an IC50 of 0.81 μM. | ||
| M51402 | KWKHGAEIVYKSPVV-{S(GlcNAc-β-D)}-GDTSPRHLSNVK-{K(biotinyl)}-NH2 | Others |
| KWKHGAEIVYKSPVV-{S(GlcNAc-β-D)}-GDTSPRHLSNVK-{K(biotinyl)}-NH2 is a polypeptide that can be found by peptide screening. | ||
| M1676 | BIBR1532 | Checkpoint |
| BIBR-1532 | ||
| BIBR1532 is a potent and selective telomerase inhibitor with IC50 of 100 nM. BIBR 1532 inhibits the proliferation of JVM13 leukemia cells with an IC50 of 52 μM, and similar effect also occurs in other leukemia cell lines such as Nalm-1, HL-60, and Jurkat. BIBR1532 is also an inhibitor of TERT, the rate-limiting enzyme in the regulation of telomerase activity. | ||
| M1717 | GSK1904529A | IGF-1R |
| GSK1904529A selectively inhibits IGF-IR and IR with IC50s of 27 and 25 nmol/L, respectively. GSK1904529A shows poor activity (IC50>1 μM) in 45 other serine/threonine and tyrosine kinases. GSK1904529A exhibits anti-tumor activity. | ||
| M1757 | XL-184 | c-Met |
| Cabozantinib; BMS-907351 | ||
| Cabozantinib (XL184, BMS-907351) is a small molecule inhibits multiple receptor tyrosine kinases, specifically MET and VEGFR2 with IC50 values of 0.035 and 1.8 nM for VEGFR2 and Met respectively. | ||
| M1784 | Icotinib | EGFR/HER2 |
| BPI-2009H | ||
| Icotinib (BPI-2009H) is a potent and novel epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) with an IC50 of 5 nM. Iconitib inhibits the proliferation of A431 and BGC-823 A549, H460 and KB cell lines with IC50s of 1, 4.06, 12.16, 16.08, 40.71 μM. | ||
| M1861 | Silmitasertib (CX-4945) | Casein Kinase |
| Silmitasertib; CX-4945 | ||
| CX-4945 (Silmitasertib) is a potent small molecule protein kinase inhibitor that selectively binds to and inhibits the enzyme casein kinase II (CK2). | ||
| M1923 | Lonidamine | CFTR |
| AF 1890；Diclondazolic Acid; DICA | ||
| Lonidamine (AF-1890) is a novel CFTR open channel blocker with an IC50 of 0.85 mM, which inhibits aerobic glycolysis in cancer cells. Lonidamine (AF-1890) is a hexokinase and mitochondrial pyruvate carrier inhibitor (Ki=2.5 μM). | ||
| M1932 | GSK1838705A | ALK |
| GSK1838705A is a small-molecule kinase inhibitor that inhibits IGF-IR and the insulin receptor with IC50s of 2.0 and 1.6 nmol/L, respectively. | ||
| M2022 | Torin 2 | mTOR |
| Torin 2 is a potent and selective mTOR inhibitor with IC50 of 2.1 nM. Torin 2 also inhibits DNA-PK with an IC50 of 0.5 nM in the cell free assay. Torin 2 can suppress both mTORC1 and mTORC2. | ||
| M2027 | Tenovin-1 | p53 |
| Tenovin-1 is a small molecule activator of p53 transcriptional activity. Tenovin-1 acts through inhibition of the protein-deacetylating activities of SirT1 and SirT2. Tenovin-1 is also a dihydroorotate dehydrogenase (DHODH) inhibitor. | ||
| M2028 | Fludarabine | STAT |
| Fludara; NSC 118218; Fludarabinum; F-ara-A | ||
| Fludarabine (NSC 118218) is a STAT1 activation inhibitor and a DNA synthesis inhibitor. Fludarabine inhibits DNA synthesis by interfering with ribonucleotide reductase and DNA polymerase. Fludarabine markedly inhibited VSMC proliferation in cell culture. Fludarabine also induces significant reduction of STAT-1 phosphorylation, whereas it does not change JAK2 activation. Fludarabine exhibits antiproliferative activity (IC50 = 1.54 μM in RPMI cells) and triggers apoptosis through increasing Bax and decreasing Bid, XIAP and survivin expression. | ||
| M2031 | SU5416 (Semaxinib) | VEGFR/PDGFR |
| Semaxanib | ||
| Semaxinib (SU5416) is a novel small molecule multi-targeted kinase inhibitor of VEGF receptors, c-kit and FLT3. Semaxinib reversibly inhibits ATP binding to the tyrosine kinase domain of VEGFR2, potentially inhibiting VEGF-stimulated endothelial cell migration and proliferation, thereby reducing tumor microvasculature. | ||
| M2040 | BAY 11-7082 | IκB/IKK |
| BAY 11-7821; NF-κB inhibitor 13 | ||
| BAY 11-7082 is an inhibitor of cytokine-induced IκB-α phosphorylation (IC50 ~ 10 μM). BAY 11-7082 inhibits ubiquitin-specific protease USP7 and USP21 (IC50=0.19, 0.96 μM, respectively). | ||
| M2056 | PJ34 hydrochloride | PARP |
| PJ34 hcl | ||
| PJ34 hydrochloride is the hydrochloride form of PJ34, a PARP inhibitor, and inhibits PARP-1-dependent cell death (parthanatos) with an EC50 of 20 nM, acting equally effectively on PARP1/2. | ||
| M2090 | MLN2480 | Raf |
| BIIB-024; Tovorafenib | ||
| MLN2480 is an orally active, CNS-permeable, highly selective inhibitor of type II RAF kinase that inhibits both monomeric (class I mutant) and dimeric forms of RAF and does not cause aberrant activation of the MAPK pathway caused by type I RAF inhibitors. In addition, MLN2480 inhibits the growth of tumors harboring BRAF fusions or BRAF V600 mutations and can be used in studies related to gliomas. | ||
| M2122 | MLN9708 | Proteasome |
| ixazomib citrate | ||
| MLN9708 is a novel orally bioactive proteasome inhibitor, inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with an IC50 value of 3.4 nM. | ||
| M2126 | Fluvastatin sodium | HMG-CoA Reductase |
| XU 62-320 | ||
| Fluvastatin sodium is an orally active, potent and competitive HMG-CoA reductase inhibitor with IC50 value between 40 and 100 nM at human liver microsomes. Fluvastatin sodium protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway. | ||
| M2153 | Orantinib | VEGFR/PDGFR |
| SU6668; TSU-68 | ||
| Orantinib (SU6668; TSU-68) is a protein kinase inhibitor of PDGF-Rβ, VEGF-R2 and FGF-R1 with IC50 of 0.06, 2.4 and 3.0 μM, respectively. | ||
| M2192 | BMS-754807 | IGF-1R |
| Bms-754807 is a potent igf-1r /InsR reversible inhibitor with an IC50 of 1.8 nM/1.7 nM and also inhibits the activity of Met, RON, TrkA, TrkB, AurA and AurB with an IC50 value of 6,44,7,4, respectively. At 9 and 25 nM, it has almost no inhibitory activity against Flt3, Lck, MK2, PKA and PKC. | ||
| M2198 | Curcumin | Histone Acetyltransferase |
| Indian Saffron; Turmeric yellow; Natural Yellow 3; Diferuloylmethane | ||
| Curcumin (Diferuloyl), a natural phenolic compound, is a p300/CREB binding protein specific inhibitor that inhibits histone/non-histone acetylation and histone acetyltransferase-dependent chromatin transcription. Curcumin inhibited NF-κ B and MAPKs, and had anti-inflammatory, antioxidant, anti-proliferation and anti-angiogenesis effects. Curcumin induces Nrf2 protein stabilization through Keap1 cysteine modification. | ||
| M2225 | Thalidomide | Ligand for E3 Ligase |
| Thalomid | ||
| Thalidomide is a sedative and immunomodulator used to study the symptoms of many cancers, it has immunomodulatory, anti-inflammatory and anti-angiogenic cancer properties. Thalidomide inhibits cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, with a Kd of ∼250 nM. | ||
| M2238 | Dorsomorphin dihydrochloride | AMPK |
| BML-275 2HCl; Compound C 2HCl | ||
| Dorsomorphin (BML-275; Compound C) dihydrochloride is a potent inhibitor of AMP-activated protein kinase (AMPK), with a Ki of 109 nM. Dorsomorphin dihydrochloride inhibits BMP pathway by targeting the type I receptors ALK2, ALK3, and ALK6. Dorsomorphin dihydrochloride induces autophagy. | ||
| M2285 | MLN2238 | Proteasome |
| Ixazomib | ||
| MLN2238 inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with IC50 and Ki of 3.4 nM and 0.93 nM, respectively. | ||
| M2327 | Daunorubicin hydrochloride | DNA/RNA Synthesis |
| Daunomycin hydrochloride; RP 13057 hydrochloride; Rubidomycin hydrochloride | ||
| Daunorubicin (Daunomycin) HCl is a topoisomerase II inhibitor, inhibits both DNA and RNA synthesis and inhibits DNA synthesis with Ki of 0.02 μM. Daunorubicin hydrochloride is a cytotoxin that inhibits cancer cell viability and induces apoptosis and necrosis. Daunorubicin hydrochloride is also an anthracycline antibiotic. | ||
| M2328 | Pirfenidone | TGF-beta/Smad |
| AMR69; S-7701 | ||
| Pirfenidone (AMR69) is an antifibrotic agent that attenuates CCL2 and CCL12 production in fibrocyte cells. Pirfenidone inhibits TGF-β bioactivity by affecting TGF-β2 mRNA expression and processing of pro-TGF-β in CCL-64 cells. Pirfenidone (AMR69) attenuates CCL2 and CCL12 production in fibrocyte cells. | ||
| M2360 | 4E1RCat | Eukaryotic Initiation Factor |
| 4E1RCat is a dual inhibitor of eIF4E:eIF4G and eIF4E:4E-BP1 interaction, and inhibits the binding of eIF4G to eIF4E with IC50 of 3.2 μM. | ||
| M2381 | AMD3465 hexahydrobromide (AMD3465 ) | CXCR |
| GENZ-644494 hexahydrobromide | ||
| AMD3465 hexahydrobromide（AMD3465 ) is an effective CXCR4 antagonist that inhibits 12G5 mAb in SupT1 cells. The IC50 values of CXCL12AF647 and CXCR4 were 0.75 nM and 18 nM, respectively. AMD 3465 also effectively inhibited X4 HIV replication (IC50, 1-10 nM), but not R5 HIV replication. | ||
| M2388 | Amitriptyline hydrochloride | 5-HT Receptor |
| Amitriptyline inhibits serotonin receptor, norepinephrine receptor, 5-HT4, 5-HT2 and sigma 1 receptor with IC50 of 3.45 nM, 13.3 nM, 7.31 nM, 235 nM and 287 nM, respectively. | ||
| M2389 | Amoxapine | Others |
| CL-67772 | ||
| Amoxapine is a tricyclic dibenzoxazepine (an N-aryl piperazine) which acts similarly to several other tricyclic antidepressants, amoxapine inhibits GLYT2a transport activity with IC50 of 92 μM. | ||
| M2425 | Azelnidipine | Calcium Channel |
| UR-12592; CS 905 | ||
| Azelnidipine is a novel dihydropyridine derivative, a L-type calcium channel blocker, and an antihypertensive. Azelnidipine inhibits the intracellular calcium ion flow and lower blood pressure by selectively blocking L-type calcium channel on the membrane of vascular smooth muscle. Azelnidipine inhibits esophageal squamous cell carcinoma proliferation by targeting MEK1/2. Azelnidipine also has anti-inflammatory, antioxidant and neuroprotective effects. | ||
| M2458 | Bismuth Subsalicylate | Others |
| Bismuth oxysalicylate; Bismuth(III) salicylate basic | ||
| Bismuth Subsalicylate is the active ingredient in Pepto-Bismol and inhibits prostaglandin G/H Synthase 1/2. | ||
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