About 32 results found for searched term "TR100" (0.089 seconds)
| Cat.No. | Name | Target |
|---|---|---|
| M8430 | TR100 | Myosin |
| TR-100 | ||
| TR100 is a specific anti-tropomyosin agent that preferentially disrupts the actin cytoskeleton of tumor cells. TR100 selectively disrupts Tm5NM1/2 containing actin filaments. | ||
| M21464 | FITC-Dextran (MW 10000) | Fluorescent Dye |
| FITC-Dextran (MW 10000) is a fluorescent probe for fluorescein isothiocyanate (FITC) dextran (Ex=495 nm; Em=525 nm). | ||
| M25117 | Galegenimab | Serine/Threonine Protease |
| FHTR 2163; RG 6147; RO 7171009 | ||
| Galegenimab (FHTR 2163; RG 6147; RO 7171009), an anti-High-temperature requirement A1 (HTRA1) antibody fragment. Galegenimab can be used for age-related macular degeneration (AMD) research. | ||
| M1710 | Flavopiridol | CDK |
| HMR-1275; Alvocidib; L86-8275 | ||
| Flavopiridol (Alvocidib) is a competitive broad-spectrum CDK inhibitor with IC50 of 30,170,100 nM against CDK1, CDK2 and CDK4, respectively. | ||
| M1755 | WYE-354 | mTOR |
| WYE-354 is a cell-permeable pyrazolopyrimidine compound that acts as a potent and ATP-competitive mTOR inhibitor (IC50 = 5 nM with S6K as the substrate and 100 µM ATP). | ||
| M1854 | VX-770 (Ivacaftor) | CFTR |
| Ivacaftor | ||
| VX-770 (Ivacaftor) is a first-in-class potentiator of CFTR, which targeting G551D-CFTR and F508del-CFTR with EC50 of 100 nM and 25 nM, respectively. | ||
| M2048 | Sumatriptan succinate | 5-HT Receptor |
| GR-43175 | ||
| Sumatriptan succinate (GR 43175) is an orally active 5-HT1 receptor agonist with Kis of 17 nM, 27 nM and 100 nM for 5-HT1D, 5-HT1B and 5-HT1A receptors, respectively. Sumatriptan succinate can be used for the research of migraine headache. | ||
| M3481 | WAY-100635 Maleate | 5-HT Receptor |
| WAY-100635 maleate is a potent, selective 5-HT1A receptor antagonist with an IC50 value of 0.91 nM, a Ki value of 0.39 nM, and a pIC50 of 8.87, which is more than 100-fold more selective than for use at the other 5-HT receptor subtypes and major neurotransmitter receptors. In addition, WAY-100635 maleate is a potent dopamine D4 receptor agonist. | ||
| M3516 | MK-5108 | Aurora Kinase |
| VX-689 | ||
| MK-5108 (VX-689) is a highly selective Aurora A inhibitor with IC50 of 0.064 nM and is 220- and 190-fold more selective for Aurora A than Aurora B/C, while it inhibits TrkA with less than 100-fold selectivity. | ||
| M3616 | Tofacitinib citrate | JAK |
| CP-690550 citrate | ||
| Tofacitinib (CP-690550) Citrate is a novel inhibitor of JAK3 with IC50 of 1 nM, 20- to 100-fold less potent against JAK2 and JAK1. | ||
| M4985 | VR23 | Proteasome |
| VR23 is a small molecule that potently inhibited the activities of trypsin-like proteasomes (IC50 = 1 nM), chymotrypsin-like proteasomes (IC50 = 50-100 nM), and caspase-like proteasomes (IC50 = 3 μM). | ||
| M5128 | PFI-2 | Histone Methyltransferase |
| (R)-PFI-2 | ||
| PFI-2 is a potent, selective, and cell-active lysine methyltransferase SETD7 inhibitor with Ki (app) and IC50 of 0.33 nM and 2 nM, 1000-fold selectivity over other methyltransferases and other non-epigenetic targets. | ||
| M5207 | Bempedoic acid (ETC-1002) | AMPK |
| ESP-55016; Bempedoic acid | ||
| Bempedoic acid (ETC-1002) is a novel, first-in-class, orally available ATP-citrate lyase (ACL) inhibitor, Bempedoic acid (ETC-1002) can activate AMPK. | ||
| M6151 | Larotrectinib (LOXO-101) | Trk |
| ARRY-470, larotrectinib | ||
| Larotrectinib (LOXO-101) is a potent, ATP competitive TRK inhibitor with IC50s in low nanomolar range for inhibition of all TRK family members in binding and cellular assays, with 100x selectivity over other kinases, with 2 to 20 nM cellular potency against the TRKA, TRKB, and TRKC kinases. | ||
| M6175 | Serabelisib | PI3K |
| INK-1117,MLN-1117,TAK-117 | ||
| Serabelisib (INK-1117,MLN-1117,TAK-117) is a potent and selective oral PI3Kα isoform inhibitor (IC50 of 21 nmol/L against PI3Kα) that has demonstrated > 100-fold selectivity relative to other class I PI3K family members (PI3Kβ/γ/δ) and mTOR, and a high degree of selectivity against many other kinase. | ||
| M6177 | SGC2085 | PRMTs |
| SGC2085 is a potent and selective Coactivator Associated Arginine Methyltransferase 1 (CARM1) inhibitor with an IC50 value of 50 nM and >100-fold selective over other PRMTs. | ||
| M6198 | Verucerfont | CRFR |
| GSK561679 | ||
| Verucerfont is a corticotropin-releasing factor receptor 1 (CRF1) antagonist with IC50s of ~6.1, >1000 and >1000 nM for CRF1, CRF2, and CRF-BP, respectively. | ||
| M6303 | JNJ-31020028 | Neuropeptide Receptor |
| JNJ-31020028 is a selective brain penetrant antagonist of neuropeptide Y2 receptor with high affinity(pIC50=8.07, human; pIC50=8.22 rat); >100-fold selective versus human Y1/Y4/Y5 receptors. | ||
| M6312 | LLY-283 | PRMTs |
| LLY-283 is the potent and selective SAM-competitive chemical probe for PRMT5. It inhibits PRMT5 enzyme activity with IC50 of 20 nM for methylation of an H4R3 derived peptide substrate, and shows greater than 100-fold selectivity over other histone methyltransferases and non-epigenetic targets. | ||
| M6746 | Sobetirome | Thyroid Hormone Receptor |
| GC-1; QRX-431 | ||
| Sobetirome is a thyroxine mimetic and a high affinity agonist for the thyroid hormone receptors THR-β and THR-α (KD values 67 and 440 pM, respectively). The in vitro effects on TRα1 and TRβ1 receptors are 5 and 100 times stronger than those of the endogenous agonist T3, respectively. | ||
| M7177 | Quinine hydrochloride | Potassium Channel |
| Quinine hydrochloride is the hydrochloride form of Quinine, an alkaloid extracted from the bark of the cinchona tree, with antimalarial and antitumor activities, and an IC50 value of 60 ng/mL against P. falciparum strains passou and 107.8 ng/mL against P. falciparum strain 3CD7, respectively, and an inhibitor of potassium channels. Quinine hydrochloride is also a potassium channel inhibitor that inhibits voltage pulse-induced MT mSlo3 (KCa5.1) channel +100 mV currents, with an IC50 value of 169 μM. In addition, Quinine hydrochloride binds to purine nucleoside phosphorylase (PfNP) and PfNP with low nanomolar affinity. nucleoside phosphorylase (PfPNP) with low nanomolar affinity. | ||
| M7886 | LY255283 | Leukotriene Receptor |
| LY255283 is a competitive leukotriene B4 receptor antagonist, with an IC50 of about 100 nM. | ||
| M8294 | Indazole-Cl | Others |
| Indazole-Cl is a selective estrogen receptor modifier (SERM), a selective ERβ agonist with > 100-fold selectivity for ERβ over Erα. | ||
| M9016 | Ezutromid | Cytochrome P450 (e.g. CYP17) |
| BMN-195; SMT C1100 | ||
| Ezutromid (BMN-195, SMT C1100) is a first-in-class oral bioavailable utrophin translational modulator with an EC50 value of 0.4 uM. | ||
| M9561 | A-485 | Histone Acetyltransferase |
| A-485 is a potent and selective HAT inhibitor of p300/CBP in vitro with an IC50 of 10 nM in a p300 TR-FRET assay and 3 nM in a CBP TR-FRET assay with selectivity > 1000-fold over closely related HATs. | ||
| M9745 | DIDS sodium salt | VDAC |
| MDL101114ZA | ||
| DIDS sodium salt (MDL101114ZA) is a dual ABCA1 and VDAC1 inhibitor. DIDS sodium salt is also an anion transport inhibitor, which inhibits the ClC-Ka chloride channel and the bacterial ClC-ec1Cl-/H+ exchanger with IC50s of 100 μM and ~300 μM, respectively. | ||
| M10822 | GNE-781 | Epigenetic Reader Domain |
| GNE-781 (compound 19) is a highly potent, orally active, selective bromodomain inhibitor against cyclic adenosine monophosphate response element binding protein (CBP). The IC50 value is 0.94 nM (in TR-FRET assay). GNE-781 also suppresses BRET and BRD4(1), with IC50s of 6.2 nM and 5100 nM, respectively. GNE-781 has antitumor activity. | ||
| M11286 | NXT629 | PPAR |
| NXT629 is an effective, selective and competitive PPAR-α antagonist. The IC50 value of HUMAN PPARα is 77 nM, which is higher than that of other nuclear hormone receptors, such as PPARδ, PPARγ, Erβ, GR and TRβ, with IC50 value of 6.0, 15, respectively. 15.2, 32.5 and >100 μM. | ||
| M11391 | Recombinant Human 4-1BB Ligand Protein (HEK293) | Recombinant Proteins |
| Recombinant Human 4-1BB Ligand Protein (HEK293) Protein sequence: DNA sequence encoding human 4-1BB Ligand (NP_003802.1) expressed with Fc tag at c-terminal Bioactivity: Fixed human 4-1BB (His tag) at a concentration of 1ug/mL (100 μL/ well) can bind 4-1BB ligands (Fc tag) in a linear range of 1.25-20ug/mL | ||
| M15039 | Recombinant Rat Leptin (E. coli) | Recombinant Proteins |
| Obesity protein; OB; LEP; LEPD; OBS; leptin | ||
| Leptin is a cytokine belonging to the Interleukin 6 family, and has a four-helix bundle structure. Leptin also has effects on reproduction and immunity. ED50 < 10.0 µg/ml, measured by a cell proliferation assay using LoVo cells, corresponding to a specific activity of > 100.0 units/mg. | ||
| M13827 | Butyrolactone 3 | Histone Acetyltransferase |
| MB-3 | ||
| Butyrolactone 3 (MB-3) is a specifical small-molecule inhibitor of the histone acetyltransferase Gcn5 (IC50=100 μM), which has a high affinity to the Gcn5 enzyme comparable to that of its natural substrate, histone H3. | ||
| M13877 | Tandospirone citrate | 5-HT Receptor |
| SM-3997 citrate | ||
| Tandospirone citrate is a potent and selective 5-HT1A receptor partial agonist (Ki = 27 nM) that displays selectivity over SR-2, SR-1C, α1, α2, D1 and D2 receptors (Ki values ranging from 1300-41000 nM). | ||
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