About 32 results found for searched term "PAI-1" (0.091 seconds)
| Cat.No. | Name | Target |
|---|---|---|
| M51696 | Calpain-1 substrate, fluorogenic | Fluorescent Dye |
| Calpain-1 substrate, fluorogenic serves as a sensitive and specific substrate for calpain-1 that cleaves Tyr-Gly bond and results in enhanced fluorescence.(Ex/Em = 490 nm/518 nm). | ||
| M52777 | SPAI-1 | ATPase |
| SPAI-1 is a specific inhibitor for monovalent cation transporting ATPases. | ||
| M3636 | Leupeptin hemisulfate | Cathepsin |
| Leupeptin hemisulfate hemisulfate is the reversible inhibitor of lysosomal serine and cysteine proteinases; Leupeptin; inhibition of cathepsin B(Ki=6 nM), calpain(Ki=10 nM), trypsin (Ki=35 nM), plasmin (Ki=3.4 μM) and kallikrein (Ki=19 μM) had no effect on chymotrypsin, elastase, renin, or pepsin. | ||
| M3787 | PAI-039 | PAI-1 |
| Tiplaxtinin | ||
| PAI-039 is an inhibitor of plasminogen activator inhibitor-1 (PAI-1). | ||
| M3826 | Papain | Animal Modeling |
| arbuz; caroid; nematolyt | ||
| Papain is a cysteine protease of the peptidase C1 family. | ||
| M3950 | APD668 | GPR/FFAR |
| APD668 is a potent GPR119 agonist with EC50 of 2.7 nM and 33 nM for hGPR119 and ratGPR119 respectively. APD668 pairs are divided by CYP2C9 (KiNone of the five major CYP subtypes other than =0.1 μM) had no significant inhibitory effect. APD668 can be used for research on steatohepatitis and diabetes. | ||
| M4676 | Loureirin B | PAI-1 |
| Loureirin B is a flavonoid isolated from The blood tree of Pterygophyllum SPP. It is an inhibitor of PAI-1 with IC50 value of 26.10 μM. Loureirin B can inhibit the phosphorylation of KATP, ERK and JNK at the same time, showing an anti-diabetes effect. | ||
| M5221 | MG-101 | Proteasome |
| Calpain inhibitor I; Ac-LLnL-CHO; ALLN | ||
| MG-101 is a potent inhibitor of cysteine proteases including calpain I (Ki = 190 nM), calpain II (Ki = 220 nM), cathepsin B (Ki = 150 nM), and cathepsin L (Ki = 500 pM). IC50 value: 150 nM (Ki) | ||
| M5349 | (+)-Camphor | TRP Channel |
| D-(+)-Camphor; (1R)-(+)-Camphor | ||
| Camphor is a waxy, flammable, white or transparent solid with a strong aroma, often used to relieve pain, reduce itching and treat fungal infections. It can activate TRPV1 and TRPV3. | ||
| M6221 | Pertuzumab | EGFR/HER2 |
| Omnitarg, 2C4 | ||
| Pertuzumab, a humanized monoclonal antibody and the first in the class of agents called the HER2 dimerization inhibitors, impairs the ability of HER2 to bind to other members of the HER family, MW: 148 KD. | ||
| M6704 | EHT 1864 2HCl | Ras |
| EHT1864 | ||
| EHT 1864 is a potent inhibitor of Rac family GTPases. EHT 1864 directly binds and impairs the ability of this small GTPase to engage critical downstream effectors required for growth transformation. The Kd values are 40, 50, 60, and 230 nM for Rac1, Rac1b, Rac2 and Rac3, respectively. | ||
| M7764 | PD 150606 | Others |
| PD 150606 is a selective, cellular permeable non-peptide calpain inhibitor with Ki of 0.21 μ m and 0.37 μ m on μ-calpains and M-calpains, respectively, and has neuroprotective activity. | ||
| M7934 | MDL 28170 | Gamma-secretase/Beta-secretase |
| Calpain Inhibitor III | ||
| Mdl-28170 (Calpain Inhibitor III) is a potent, selective, membrane-permeable Inhibitor of cysteine protease (Calpain Inhibitor III) that can quickly cross the blood-brain barrier after systemic administration. Mdl-28170 also blocks gamma-secretase. | ||
| M8524 | TM5275 sodium salt | PAI-1 |
| TMS5275 is an orally available, potent and selective inhibitor of PAI-1 that delivers antithrombotic benefits devoid of bleeding effect in nonhuman primates. | ||
| M8783 | Lys05 | Autophagy |
| Lys01 trihydrochloride | ||
| Lys05 (Lys01 trihydrochloride) is a dimeric chloroquine (CQ) that deacidifies the lysosome and causes impairment of lysosomal enzymes, exhibiting more than 10-fold higher autophagy inhibitory potency than hydroxychloroquine (HCQ) and CQ (LC3II/LC3I ratio = 15. | ||
| M9677 | TM5441 | PAI-1 |
| TM-5441 | ||
| TM5441 is an orally bioavailable inhibitor of plasminogen activator inhibitor-1 (PAI-1), with IC50 values between 13.9 and 51.1 μM against several human cancer cell lines. | ||
| M10877 | QCA570 | Others |
| QCA570 is made up of Cereblon ligands and BET ligands connected to PROTAC, which is paired with the BRD4 BD1 protein IC50 The value is 10 nM. | ||
| M11294 | Alicapistat | Proteasome |
| ABT-957 | ||
| Alicapistat (ABT-957) is an orally active, selective inhibitor of human calpains 1 and 2 that can be used in alzheimer's disease (AD) studies. | ||
| M11420 | MYCi975 | c-Myc |
| NUCC-0200975 | ||
| MYCi975 (Nuc-0200975) is an orally active MYC inhibitor that disrupts MYC/MAX interactions, promotes MYC T58 phosphorylation and MYC degradation, and impairs myC-driven gene expression. MYCi975 (NUC-0200975) has strong anti-tumor effect and good tolerance, increasing tumor immune cell infiltration and enhancing tumor sensitivity against PD1 immune studies. | ||
| M13366 | (R)-MG-132 | Proteasome |
| Z-Leu-Leu-Leu-al | ||
| (R)-MG-132 (Z-LEu-LEu-Al) is a cellular permeable proteasome and Calpain inhibitor with IC50 of 100 nM and 1.2 μM, respectively. | ||
| M13499 | Bacopaside II | AQP |
| Bacopaside II, an extract from the medicinal herb Bacopa monnieri, blocks the Aquaporin-1 (AQP1) water channel and impairs migration of cells that express AQP1. Bacopaside II induces cell cycle arrest and apoptosis. | ||
| M14193 | Cav 2.2 blocker 1 | Calcium Channel |
| Cav 2.2 blocker 1 (compound 9) is a N-type calcium channel (Cav 2.2) blocker for the treatment of pain, with an IC50 of 1 nM. | ||
| M14480 | Toddalolactone | PAI-1 |
| Toddalolactone, a main component of Toddalia asiatica, inhibits the activity of recombinant human plasminogen activator inhibitor-1 (PAI-1), with an IC50 value of 37.31 μM. | ||
| M14600 | DCZ0415 | NF-κB |
| DCZ0415, a potent TRIP13 inhibitor, impairs nonhomologous end joining repair and inhibits NF-κB activity. DCZ0415 induces anti-myeloma activity in vitro, in vivo, and in primary cells derived from drug-resistant myeloma patients. | ||
| M20575 | Lucanthone | Autophagy |
| Lucanthone is a novel autophagic inhibitor and also an orally available thioxanthone-based DNA intercalator and inhibitor of the DNA repair enzyme apurinic-apyrimidinic endonuclease 1. | ||
| M20729 | MYCi361 | c-Myc |
| NUCC-0196361 | ||
| MYCi361 is a MYC inhibitor that engages MYC inside cells, disrupts MYC/MAX dimers, and impairs MYC-driven gene expression. MYCi361 binds to MYC with Kd of 3.2 μM. MYCi361 suppresses in vivo tumor growth, increases tumor immune cell infiltration, upregulates PD-L1 on tumors, and sensitizes tumors to anti-PD1 immunotherapy. | ||
| M20775 | SEC inhibitor KL-1 | Others |
| KL-1 | ||
| SEC inhibitor KL-1 (KL-1) is a potent and selective inhibitor of super elongation complex (SEC) that disrupts the interaction between the SEC scaffolding protein AFF4 and P-TEFb, resulting in impaired release of Pol II from promoter-proximal pause sites and a reduced average rate of processive transcription elongation. KL-1 exhibits an dose-dependent inhibitory effect on AFF4-CCNT1 interaction with Ki of 3.48 μM. | ||
| M20800 | ASLAN003 | DHODH |
| LAS 186323; Farudodstat | ||
ASLAN003 (LAS 186323) is a potent and orally active inhibitor of DHODH (Dihydroorotate dehydrogenase) with IC50 of 35 nM for human DHODH enzyme activity. ASLAN003 impairs protein synthesis and induces the differentiation and apoptosis transcriptional program in acute myeloid leukemia (AML) cells via activation of AP-1 transcription factors. |
||
| M20954 | Zucapsaicin | TRP Channel |
| Zucapsaicin, the cis-isomer of capsaicin, is a topical analgesic used to treat osteoarthritis of the knee and other neuropathic pain. It is also a TRPV-1 modulator. | ||
| M25000 | TSR-033 | Others |
| TSR-033 is a high affinity human IgG4 antibody targeting LAG-3 (lymphocyte activation gene-3), a co-receptor associated with impaired T cell function and often co-expressed with PD-1, that enhances T cell function and PD-1 blocking activity in vitro and in vivo. TSR-033 has anti-tumor activity. | ||
| M27646 | VCP171 | Adenosine Receptor |
| VCP171 is a potent adenosine A1 receptor (A1R) positive allosteric modulator (PAM). VCP171 is effective at decreasing excitatory synaptic currents in Lamina II of neuropathic pain model. VCP171 can be used for researching neuropathic pain. | ||
| M27678 | KS15 | Others |
| KS15 is an inhibitor of the interactions between cryptochromes (CRYs: CRY1 and CRY2) and the CLOCK:BMAL1 heterodimer. KS15 impairs the feedback actions of CRYs on E-box-dependent transcription (EC50=4.9 μM) by CLOCK:BMAL1 heterodimer, an indispensable transcriptional regulator of the mammalian circadian clock. Anti-proliferative activity. | ||
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