About 32 results found for searched term "50-76-0" (0.089 seconds)
| Cat.No. | Name | Target |
|---|---|---|
| M11187 | Eclitasertib | RIPK |
| DNL-758; SAR-443122 | ||
| Eclitasertib (DNL-758) is a receptor interaction protein kinase 1 (RIPK1) inhibitor, with IC50 value of <1 μΜ. | ||
| M50323 | Peptidylprolyl isomerase | Enzymes & Coenzymes |
| Peptidylprolyl isomerase is a biochemical reagent that can be used as a biological material or organic compound for life science related research. | ||
| M1770 | PIK-75 Hydrochloride | PI3K |
| PIK-75 HCl | ||
| PIK-75 Hydrochloride is a PI3K p110α specific inhibitor with IC50s of 6,1300,76,510 nM for p110α,p110β,p110γ, p110δrespectively. | ||
| M1875 | PD173074 | FGFR |
| PD173074 is a selective FGFR1 and FGFR3 inhibitor with IC50 values of 5, 21.5, ~100, 17600 and 19800 nM for FGFR3, FGFR1, VEGFR2, PDGFR and c-Src respectively. | ||
| M1908 | VER-82576 | HSP |
| NVP-BEP800; VER82576 | ||
| VER-82576 (NVP-BEP800) is a potent, orally available and selective inhibitor of Hsp90β with an IC50 of 58 nM. VER-82576 also slightly blocks Grp94 and Trap-1, with IC50s of 4.1 and 5.5 μM, respectively. | ||
| M2383 | AMG-517 | TRP Channel |
| AMG 517 is a potent and selective TRPV1 antagonist, antagonizes capsaicin, proton, and heat activation of TRPV1 with IC50 of 0.76 nM, 0.62 nM and 1.3 nM. | ||
| M2911 | Riviciclib hydrochloride (P276-00) | CDK |
| Riviciclib hydrochloride | ||
| Riviciclib hydrochloride (P276-00) is an effective CDK inhibitor, inhibiting CDK9-CyclinT1, CDK4-cyclin D1, CDK1-Cyclinb with IC50 values of 20 nM, 63 nM, respectively. 79 nM. Riviciclib hydrochloride (P276-00) has anti-tumor activity against Cisplatin resistant cells. | ||
| M3230 | D-87503 | PI3K |
| D-87503 inhibits PI3K and Erk2 with IC50 of 62 nM and 760 nM, respectively. | ||
| M4532 | Rhodionin | AChR/AChE |
| Rhodionin was isolated from the roots of Rhodiola crenulata and is a specific non-competitive cytochrome P450 2D6 inhibitor with IC50 of 0.761 μM and Ki of 0.769 μM. Rhodionin effectively inhibited acetylcholinesterase (AChE) in a dose-dependent manner with an IC50 range of 57.50 to 2.43 μg/mL. Rhodionin had effective DPPH radical scavenging activity with IC50 of 19.49 μM. | ||
| M5043 | 4-Chloro-7H-pyrrolo[2,3-d]pyrimidine | Others |
| 4-Chloro-7H-pyrrolo[2,3-d] pyrimidine is an important pharmaceutical intermediate, which is widely used in the synthesis of many pharmaceutical intermediates at home and abroad. Including CP690550, CGP76030 and so on, 4-Chloro-7H-pyrrolo[2,3-d] pyrimidine was the scaffold for many commercially available drugs. Also, 4-Chloro-7H-pyrrolo[2,3-d] pyrimidine was the intermediate of the bulk drug, Tofatinib, which was widely used in treatment of adult patients with moderate to severe rheumatoid arthritis with inadequate or intolerant methotrexate response. | ||
| M5254 | Ipragliflozin | SGLT |
| ASP 1941 | ||
| Ipragliflozin (ASP1941) is an orally active and selective SGLT2 inhibitor with IC50s of 7.38 and 1876 nM, 6.73 and 1166 nM, 5.64 and 1380 nM for human SGLT2 and SGLT1, rat SGLT2 and SGLT1, mouse SGLT2 and SGLT1, respectively. | ||
| M6649 | CZC-25146 | LRRK2 |
| CZC25146 | ||
| CZC 25146 is a potent and orally active LRRK2 inhibitor with IC50 values of 4.76 nM and 6.87 nM for wild-type LRRK2 and G2019S LRRK2, respectively. CZC-25146 inhibits PLK4, GAK, TNK1, CAMKK2 and PIP4K2C as well. | ||
| M7374 | TC-H 106 | HDAC |
| Pimelic Diphenylamide 106; RGFA-8; Histone Deacetylase Inhibitor VII | ||
| TC-H 106 is a class I histone deacetylase inhibitor, with IC50 values of 150 nM , 760 nM and 370 nM for HDAC 1, 2, and 3, respectively. | ||
| M8432 | CYM50769 | Neuropeptide Receptor |
| CYM50769 is a potent, specific antagonist of the Neuropeptide B and Neuropeptide W receptor, NPBWR1 (IC50 = 120 nM). | ||
| M8624 | HPB | Others |
| HPB is a cell-permeable, non-cytotoxic N-hydroxybenzamide derivative that acts as a HDAC6-selective deacetylase inhibitor (IC50 = 31/376/677/842/1133 nM against HDAC6/8/10/1/7, >2 μM against HDAC2/3/4/11/9/5). | ||
| M9743 | TMRE | Fluorescent Dye |
| Tetramethylrhodamine ethyl ester perchlorate | ||
| Tetramethylrhodamine ethyl ester (TMRE) can bind to mitochondria and produce orange fluorescence with a maximum excitation/emission wavelength of 550nm/576nm, which is often used to observe mitochondria. Store in refrigerator (-5 to -30°C) away from light. | ||
| M10595 | MLi-2 | LRRK2 |
| MLi2 | ||
| MLi-2 is a highly potent, and selective LRRK2 kinase inhibitor with central nervous system activity. MLi-2 exhibits exceptional potency in a purified LRRK2 kinase assay in vitro (IC50 = 0.76 nM), a cellular assay monitoring dephosphorylation of LRRK2 pSer935 LRRK2 (IC50 = 1.4 nM), and a radioligand competition binding assay (IC50 = 3.4 nM). | ||
| M10848 | LP-922761 | Others |
| LP-922761 is a potent, selective, orally active AAK1 inhibitor in enzymatic and cell analysis IC50 4.8 nM and 7.6 nM, respectively. LP-922761 also inhibits BMP-2-induced protein kinase (BIKE),IC50 24 nM. LP-922761 has no significant activity against cell GAK, opioids, epinephrine alpha2, or GABAa receptors. | ||
| M11524 | TMRM | Fluorescent Dye |
| Tetramethylrhodamine methyl ester (TMRM) is a cell permeable, cationic fluorescent dye with a maximum excitation/emission wavelength of 550nm/576nm. It emits red fluorescence and can easily adsorb active mitochondria. Store in refrigerator (-5 to -30°C) away from light. | ||
| M20060 | WAY-296818 | Casein Kinase |
| Casein kinase 1δ-IN-3 | ||
| WAY-296818 is a casein kinase 1δ (CK1d) inhibitor with a pIC50 of 6.5376 M. It is a casein kinase 1δ (CK1d) inhibitor with a pIC50 of 6.5376 M. | ||
| M22486 | AH-7614 | GPR/FFAR |
| AH7614 | ||
| AH-7614 is a potent and selective FFA4 (GPR120) antagonist, with pIC50s of 7.1, 8.1, and 8.1 for human, mouse, and rat FFA4, respectively. AH-7614 has selectivity for FFA4 over FFA1 (pIC50<4.6). AH-7614 is able to block effects of both the polyunsaturated ω-6 fatty acid linoleic acid and the synthetic FFA4 agonist. | ||
| M27999 | TASP0376377 | Prostaglandin Receptor |
| TASP0376377 is a potent and selective CRTH2 antagonist (IC50: 13 nM). TASP0376377 has binding affinity for CRTH2 (IC50: 19 nM). | ||
| M28380 | AZ3976 | PAI-1 |
| AZ3976 is a potent plasminogen activator inhibitor type 1 (PAI-1) inhibitor with an IC50 value of 26 μM in an enzymatic chromogenic assay. AZ3976 is active with an IC50 of 16 μM in a plasma clot lysis assay. AZ3976 does not bind to active PAI-1 but bound reversibly to latent PAI-1. AZ3976 inhibits PAI-1 by enhancing the latency transition of active PAI-1. AZ3976 displays profibrinolytic activities in a human plasma clot lysis assay. | ||
| M28535 | GDC-0276 | Sodium Channel |
| GDC-0276 is a potent, selective, reversible and orally active NaV1.7 inhibitor with an IC50 value of 0.4 nM. GDC-0276 is well tolerated and exhibits a good pharmacokinetic profile. GDC-0276 has the potential for the treatment of pain and to address shortcomings of existing pain medications, such as addiction and off-target side effects. | ||
| M28540 | Talabostat | Dipeptidyl Peptidase |
| Val-boroPro; PT100 | ||
| Talabostat (Val-boroPro; PT100) is an orally active and nonselective dipeptidyl peptidase IV (DPP-IV) inhibitor (IC50 < 4 nM; Ki = 0.18 nM) and the first clinical inhibitor of fibroblast activation protein (FAP) (IC50 = 560 nM), inhibits DPP8/9 (IC50 = 4/11 nM; Ki = 1.5/0.76 nM), quiescent cell proline dipeptidase (QPP) (IC50 = 310 nM), DPP2, and some other DASH family enzymes. Antineoplastic and hematopoiesis- stimulating activities. | ||
| M28603 | PS10 | PDHK |
| PS10 is a novel, potent and ATP-competitive pan-PDK inhibitor, inhibits all PDK isoforms with IC50 of 0.8 μM, 0.76 μM, 2.1 μM and 21.3 μM for PDK2, PDK4, PDK1, and PDK3, respectively. PS10 shows high affinity for PDK2 (Kd= 239 nM) than for Hsp90 (Kd= 47 μM). PS10 improves glucose tolerance, stimulates myocardial carbohydrate oxidation in diet-induced obesity. PS10 has the potential for the investigation of diabetic cardiomyopathy.PDK: pyruvate dehydrogenase kinase | ||
| M28706 | SF0166 | Integrin |
| SF0166 is a potent and selective αvβ3 antagonist with IC50 values of 0.6 nM, 8 nM, and 13 nM for αvβ3, αvβ6, and αvβ8, respectively. SF0166 inhibits cellular adhesion to vitronectin across human, rat, rabbit, and dog cell lines with IC50 values of 7.6 pM to 76 nM. SF0166 decreases neovascularization in the oxygen-induced retinopathy mouse model. | ||
| M28832 | GGTI-286 | Ras |
| GGTI-286, a potent and cell-permeable GGTase I inhibitor, is 25-fold more potent (IC50=2 μM) than the corresponding methyl ester of FTI-276. GGTI-286 selectively inhibits geranylgeranylation of Rap1A over farnesylation of H-Ras in NIH3T3 cells (IC50s=2 and >30 μM, respectively). GGTI-286 also potently inhibits oncogenic K-Ras4B stimulation with an IC50 of 1 μM. | ||
| M28863 | PD-089828 | FGFR |
| PD-089828 is an ATP competitive inhibitor of FGFR-1, PDGFR-β and EGFR (IC50s=0.15, 1.76, and 5.47 µM, respectively) and a noncompetitive inhibitor of c-Src tyrosine kinase (IC50=0.18 µM). PD-089828 also inhibits MAPK with an IC50 of 7.1 µM. PD-089828 inhibits PDGF-, EGF- and bFGF-mediated tyrosine kinase receptor autophosphorylation in vitro. PD-089828 has a long-lasting cellular activity. | ||
| M28909 | GGTI-286 hydrochloride | Ras |
| GGTI-286 hydrochloride, a potent GGTase I inhibitor, is 25-fold more potent (IC50=2 μM) than the corresponding methyl ester of FTI-276. GGTI-286 hydrochloride selectively inhibits geranylgeranylation of Rap1A over farnesylation of H-Ras in NIH3T3 cells (IC50s =2 and >30 μM, respectively). GGTI-286 hydrochloride also potently inhibits oncogenic K-Ras4B stimulation with an IC50 of 1 μM. | ||
| M29386 | CCT367766 | PROTAC |
| CCT367766 is a potent and the third generation heterobifunctional and Cereblon-based pirin targeting protein degradation probe (PDP, or PROTAC), depletes pirin protein expression at low concentration. CCT367766 exhibits a moderate affinity for the CRBN-DDB1 complex with an IC50 value of 490 nM. CCT367766 reveals a good affinity for the recombinant pirin and CRBN with Kd values of 55 nM and 120 nM, respectively. CCT367766 provides a potential chemical tool to study a largely unexplored protein. | ||
| M29712 | TH1760 | Others |
| TH1760 is an inhibitor of NUDIX-type 15 (NUDT15) with an IC50 value of 25 nM. TH1760 sensitizes cells to 6-thioguanine by enhancing the accumulation of 6-thio- (d) GTP in nucleic acids. TH1760 enhances the anti-leukemia effect of thiopurine. | ||
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