About 21 results found for searched term "DO34" (0.123 seconds)
| Cat.No. | Name | Target |
|---|---|---|
| M2411 | Picropodophyllin (AXL1717) | IGF-1R |
| Picropodophyllotoxin; CAS# 17434-18-3; PPP | ||
| AXL1717 (picropodophyllin, Picropodophyllotoxin, PPP) is a non-competitive, potent, and specific inhibitor of IGF-1Rα/β with IC50 of 1 nM. | ||
| M9647 | Orludodstat (BAY-2402234) | DHODH |
| BAY-2402234 is a potent and selective dihydroorotate dehydrogenase (DHODH) inhibitor for the treatment of myeloid malignancies, with an IC50 of 1.2 nM. | ||
| M14690 | DO34 | Others |
| DO34 is a highly potent, selective and centrally active diacylglycerol lipase (DAGL) inhibitor, with an IC50 of 6 nM for DAGLα conversion of SAG to 2-AG, and an IC50 for DAGLβ. | ||
| M3484 | Dolutegravir | Integrase |
| GSK1349572 | ||
| Dolutegravir (GSK1349572) is a two-metal-binding HIV integrase inhibitor with IC50 of 2.7 nM, modest activity against raltegravir-resistant signature mutants Y143R, Q148K, N155H, and G140S/Q148H. | ||
| M5511 | Chlormadinone acetate | Estrogen Receptor |
| Chlormadinone acetate is a steroidal progestin with additional antiandrogen and antigonadotropic effects, used often in combinations as an oral contraceptive. Its half-life is about 34-38 hours. | ||
| M5916 | Radotinib | Src-bcr-Abl |
| IY-5511 | ||
| Radotinib is a selective BCR-ABL1 tyrosine kinase inhibitor with IC50 of 34 nM, used to treat Chronic Myeloid Leukemia. | ||
| M7137 | Phosphoramidon disodium salt | Neprilysin (NEP) |
| Phosphoramidon disodium salt is a microbial metabolite and an inhibitor of the specific metalloproteases thermolysin, endothelin-converting enzyme (ECE), neutralizing peptidase (NEP) and angiotensin-converting enzyme (ACE), with IC50s of 0.4 μg/mL, 3.5 μM, 0.034 μM and 78 μM, respectively. Phosphoramidon disodium salt also prevented the degradation of amyloid β-peptide and increased Aβ levels in rodents. | ||
| M8733 | K67 | Keap1-Nrf2 |
| K-67 | ||
| K67 is a specific inhibitor against the interaction between KEAP1 (Kelch-like ECH-associated protein 1) DC (double glycine repeat and C-terminal region) domain and S349-phosphorylated (human Ser349, mouse Ser351) KIR (Keap1-interacting region) of p62/SQSTM1, thereby preventing phospho-p62 from blocking KEAP1-DC and NRF2 (nuclear factor erythroid 2-related factor 2) DLGex motif association. | ||
| M10198 | Zabedosertib | IRAK |
| BAY1834845 | ||
| Zabedosertib (BAY 1834845) is a selective, orally potent IRAK4 inhibitor with immunomodulatory and anti-inflammatory activity and an IC50 value of 3.55 nM. Zabedosertib (BAY 1834845) exhibits anti-inflammatory property against IL-β, LPS and Imiquimod induced inflammation. | ||
| M11261 | CDDO-Im | Keap1-Nrf2 |
| RTA-403; TP-235; CDDO-Imidazolide | ||
| CDDO Im (RTA-403) is the activator of Nrf2 and PPAR with Ki of 232 nM and 344 nM for PPARα and PPARγ, respectively. | ||
| M13826 | TPOP146 | Epigenetic Reader Domain |
| TPOP146 is a selective CBP/P300 benzoxazepine bromodomain inhibitor with Kd values of 134 nM and 5.02 μM for CBP and BRD4. | ||
| M13870 | Lurasidone | 5-HT Receptor |
| SM-13496 | ||
| Lurasidone (SM-13496) is an antagonist of both dopamine D2 and 5-HT7 with IC50s of 1.68 and 0.495 nM, respectively. | ||
| M28707 | VPC-14449 | Androgen Receptor |
| VPC-14449 is a potent and selective inhibitor of the DNA-binding domain of the androgen receptor (AR-DBD), with IC50 of 0.34 μM for full-length human AR. VPC-14449 reduces the ability of full-length AR as well as AR variants to interact with chromatin. VPC-14449 can be used for the research of prostate cancer. | ||
| M28808 | Dyrk1A-IN-5 | DYRK |
| Dyrk1A-IN-5 (compound 5j) is a potent and selective DYRK1A inhibitor, with an IC50 of 6 nM. Dyrk1A-IN-5 dose-dependently reduces the phosphorylation of Thr434 in SF3B1, with an IC50 of 0.5 μM. Dyrk1A-IN-5 inhibits phosphorylation of tau at Thr212, with an IC50 of 2.1 μM. Dyrk1A-IN-5 can be used for Down syndrome research. | ||
| M29173 | GSK3494245 | Parasite |
| DDD01305143 | ||
| GSK3494245 (DDD01305143) is a potent, orally active, and selective inhibitor of the chymotrypsin-like activity of the parasite proteasome binding in a site sandwiched between the β4 and β5 subunits (IC50=0.16 μM for WT L. donovani proteasomes). GSK3494245 moderately inhibits chymotrypsin-like activity of human proteasome (IC50: purified 26S=13 µM; enriched THP-1 extracts IC50=40µM). GSK3494245 exhibits attractive biological and biosafety properties. | ||
| M29317 | UT-34 | Androgen Receptor |
| UT-34 is a potent, selective and orally active second-generation pan-androgen receptor (AR) antagonist and degrader with IC50s of 211.7 nM, 262.4 nM and 215.7 nM for wild-type, F876L and W741L AR, respectively. UT-34 binds to ligand-binding domain (LBD) and function-1 (AF-1) domains and requires ubiquitin proteasome pathway to degrade the AR. UT-34 has anti-prostate cancer efficacy. | ||
| M29542 | HaloPROTAC-E | SGK |
| HaloPROTAC-E is a novel HaloPROTAC potent degrader, inducing reversible degradation of two endosomally localized proteins, SGK3 and VPS34, with a DC50 of 3-10 nM, remarkably selective inducing only degradation of the Halo tagged endogenous VPS34 complex (VPS34, VPS15, Beclin1, and ATG14). | ||
| M30133 | FAUC 365 | Dopamine Receptor |
| FAUC 365 is a highly dopamine D3 receptor-selective antagonist with Ki values of 0.5 nM, 340, 2600, and 3600 nM at D3, D4.4, D2short, and D2Long receptors, respectively. FAUC 365 can be used for the research of schizophrenia, and Parkinson's disease. | ||
| M30559 | Rubone | MicroRNA (miRNA) |
| Rubone, a chalcone analog, is a modulator of miR-34a. Rubone upregulates miR-34a expression in a p53 dependent manner, downregulates the downstream target Bcl-2 and Cyclin D1 expression, and suppresses hepatocellular carcinoma (HCC) growth in vivo. Rubone enhanced the anticancer effect of Paclitaxel (PTX) in PTX-resistant prostate cancer cell lines by reversing the expression of miR-34a downstream targets. | ||
| M45130 | NNC0385-0434 | PCSK9 |
| NNC0385-0434 is a peptide based on the epidermal growth-factor-like domain A of the human LDLR peptide. NNC0385-0434 competitively binds free PCSK9 and subsequently prevents PCSK9 binding to the LDLR. NNC0385-0434 is an orally active peptide small molecule PCSK9 inhibitor for atherosclerosis-related studies. | ||
| M50435 | Adropin (34-76) (human, mouse, rat) | Akt |
| Adropin (34-76) (human, mouse, rat) is a secretory domain of Adropin. Adropin (34-76) can inhibit cAMP level and glucose production in hepatocytes, and has a hypoglycemic effect. Adropin (34-76) plays an antifibrotic role by inhibiting the GLI1 signaling pathway. | ||
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