About 30 results found for searched term "AS-99" (0.195 seconds)
| Cat.No. | Name | Target |
|---|---|---|
| M7539 | AS1517499 | STAT |
| AS1517499 is a novel and potent STAT6 inhibitor with an IC50 value of 21 nM. | ||
| M21504 | AS-99 free base | Histone Methyltransferase |
| AS-99 is the first-in-class, effective and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 µM, Kd= 0.89 µM) with anti-leukemia activity. | ||
| M21505 | AS-99 | Histone Methyltransferase |
| AS-99 is a first-in-class, potent and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 µM, Kd= 0.89 µM) with antileukemic activity. | ||
| M21507 | AS-99 TFA | Histone Methyltransferase |
| AS-99 TFA is the first-in-class, effective and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 µM, Kd= 0.89 µM) with anti-leukemia activity. In vivo, AS-99 TFA blocked cell proliferation, induced apoptosis and apoptosis, down-regulated MLL fusion target genes, and alleviated leukaemia. | ||
| M1827 | Sorafenib Tosylate | VEGFR/PDGFR |
| BAY 43-9006,Nexavar | ||
| Sorafenib (BAY 43-9006) Tosylate is an orally active multikinase inhibitor of tyrosine protein kinases VEGFR/PDGFR and RAF/MEK/ERK with IC50 values of 6, 22, 38 nM for Raf-1, wt BRAF and V599E mutant BRAF. | ||
| M4333 | Calceolarioside-B | Aldose Reductase |
| Calceolarioside B is a natural product isolated from the Stauntonia hexaphylla leaf. Calceolarioside B showed significant inhibitory activity against aldose reductase (RLAR) in rat lens with IC50 value of 23.99 μM. Calceolarioside B could effectively inhibit DPPH radical scavenging activity with IC50 value of 94.60 μM. | ||
| M7561 | GSK-2881078 | Androgen Receptor |
| GSK-2881078 is an orally active and nonsteroidal selective androgen receptor modulator (SARM) which act as partial AR agonists in androgenic tissues while mainly as complete AR agonists in synthetic metabolic tissues,induces AR-mediated transcriptional activation in PC3(AR)2 cells (EC50 = 3.99 nM). | ||
| M8939 | Firategrast | Integrin |
| SB-683699; T-0047 | ||
| Firategrast (SB-683699) is an orally bioavailable alpha4 beta1/alpha4 beta7 integrin antagonist. | ||
| M9205 | Glasdegib | Smo |
| PF-04449913 | ||
| Glasdegib (PF-04449913) is a potent, orally bioavailable Smoothened (Smo) inhibitor with an IC50 of 4 nM. | ||
| M9646 | Decoglurant | GluR |
| RG-1578; RO4995819 | ||
| Decoglurant (also known as RO4995819) is a negative allosteric modulator of the mGlu2 and mGlu3 receptors. | ||
| M9875 | ACT-389949 | FPR |
| ACT389949 | ||
| ACT-389949 is a first-in-class, potent, selective formyl peptide receptor 2/lipoprotein A4 receptor (FPR2)/(ALX) agonist with an EC50 value of 3 nM for FPR2/ALX entry into monocytes.Additionally, ACT-389949 is an excellent tool compound for in vitro and in vivo to further analyze FPR2-regulated activity, which could be used in the development of next-generation FPR signaling-regulated anti-inflammatory therapies. | ||
| M10259 | Spastazoline | Others |
| Spastazoline is a potent and selective, cell permeable inhibitor for aaa+ (atpases associated with diverse cellular activities) proteins, inhibiting the microtubule-severing aaa+ protein spastin, with IC50 of 99 nM for human spastin. | ||
| M10608 | NLX-101 (F-15599) | 5-HT Receptor |
| NLX101 | ||
| NLX-101 (F-15599) is a highly selective G-protein biased 5-HT1A receptor agonist, with Ki of 3.4 nM. NLX-101 (F-15599) mediates antidepressant-like activity in rats via prefrontal cortex 5-HT 1A receptors. NLX-101 (F-15599) has over 1000-fold higher affinity for this target over other receptors. | ||
| M13676 | NKL 22 | HDAC |
| NKL 22 (compound 4b) is a potent and selective inhibitor of histone deacetylases (HDAC), with an IC50 of 199 and 69 nM for HDAC1 and HDAC3, respectively. | ||
| M13908 | AVE 0991 sodium salt | Angiotensin Receptor |
| AVE 0991 sodium salt is a nonpeptide and orally active Ang-(1-7) receptor Mas agonist. AVE 0991 competes for high-affinity binding of [125I]-Ang-(1-7) to bovine aortic endothelial cell membranes with IC50 of 21 nM. | ||
| M14117 | YKL-05-099 | Salt-inducible Kinase |
| YKL-05-099 is a salt-inducible kinase (SIK) inhibitor. YKL-05-099 binds to SIK1 and SIK3 with IC50s of ~10 and ~30 nM, respectively. YKL-05-099 has slightly less potent SIK2-inhibitory (IC50=40 nM). | ||
| M15035 | Recombinant Human IL-8/CXCL8 (77aa, CHO) | Cytokines and Growth Factors |
| IL8; CXCL8; monocyte-derived neutrophil chemotactic factor | ||
| Interleukin-8 (IL-8), also known as CXCL8, GCP-1 and NAP-1, is one of the first discovered chemokines and belongs to the CXCL family, in which the first two conserved cysteines are separated by one residue. Protein Construction: IL-8 (Ala23-Ser99). Accession # P10145. | ||
| M14472 | Luteolin 7-O-glucuronide | MMP |
| Luteolin 7-glucuronide | ||
| Luteolin 7-O-glucuronide could inhibit Matrix Metalloproteinases (MMP) activities, with IC50s of 17.63, 7.99, 11.42, 12.85, 0.03 μM for MMP-1, MMP-3, MMP-8, MMP-9, MMP-13, respectively. | ||
| M14579 | AZ-23 | Trk |
| AZ23; AZ 23 | ||
| AZ-23 is an ATP-competitive and orally bioavailable Trk kinase A/B/C inhibitor with IC50s of 2 nM (TrkA), 8 nM (TrkB), 24 nM (FGFR1), 52 nM (Flt3), 55 nM (Ret), 84 nM (MuSk), 99 nM (Lck), respectively. | ||
| M20705 | AS2863619 | CDK |
| AS2863619 is a small-molecule cyclin-dependent kinase CDK8/19 inhibitor with IC50 of 0.6099 nM and 4.277 nM, respectively. AS2863619 is a potent Foxp3 inducer in Tconv cells. | ||
| M20734 | (E/Z)-BCI | Phosphatase |
| BCI, NSC 150117 | ||
| (E/Z)-BCI (BCI, NSC 150117) is an inhibitor of dual specific phosphatase 1/6 (DUSP1/DUSP6) and mitogen-activated protein kinase with EC50 of 13.3 μM and 8.0 μM for DUSP6 and DUSP1 in cells, respectively. (E)-BCI induces apoptosis via generation of reactive oxygen species (ROS) and activation of intrinsic mitochondrial pathway in H1299 lung cancer cells. | ||
| M21035 | LCH-7749944 | PAK |
| GNF-PF-2356 | ||
| LCH-7749944 (GNF-PF-2356) is a novel and potent p21-activated kinase 4 (PAK4) inhibitor with an IC50 of 14.93 μM and has less potently inhibitory effect against PAK1, PAK5 and PAK6. LCH-7749944 causes successful inhibition of EGFR activity due to its inhibitory effect on PAK4. | ||
| M21353 | Golcadomide | Ligand for E3 Ligase |
| CC-99282 | ||
| Golcadomide (CC-99282) is a potent and orally active CRBN E3 ligase modulator (CELMoD).CC-99282 co-induces effective and targeted degradation of Ikaros and Aiolos with CRBN.CC-99282 can be used in studies of non-Hodgkin's lymphoma. | ||
| M25072 | Mipasetamab uzoptirine | TAM Receptor |
| ADCT-601 | ||
| Mipasetamab uzoptirine (ADCT-601) is an AXL-targeted antibody-drug conjugates (ADCs). Mipasetamab uzoptirine consists of a humanized anti-AXL antibody, a cleavable linker and the potent pyrrolobenzodiazepine (PBD) dimer cytotoxin SG3199. Mipasetamab uzoptirine can be used for the research of cancers. | ||
| M27620 | AKB-6899 | HIF |
| AKB-6899, a prolyl hydroxylase domain 3 (PHD3) inhibitor, is a selective HIF-2α stabilizer. AKB-6899 also increases soluble form of the VEGF receptor (sVEGFR-1) production from GM-CSF-treated macrophages, and has antitumor and antiangiogenic effects. | ||
| M27718 | AUTEN-99 hydrobromide | Others |
| Autophagy enhancer-99 hydrobromide | ||
| AUTEN-99 (hydrobromide) is a novel inhibitor of the myotubularin phosphatase Jumpy (also called MTMR14). AUTEN-99 (hydrobromide) crosses the blood-brain barrier and exerts potent neuroprotective effects. | ||
| M27808 | AZ12799734 | TGF-β Receptor |
| AZ12799734 is a selective, orally active TGFBR1 kinase inhibitor with an IC50 of 47 nM. AZ12799734 is also a pan BMP and TGFβ inhibitor. | ||
| M28065 | PTC299 | VEGFR/PDGFR |
| PTC299 is an orally active inhibitor of VEGFA mRNA translation that selectively inhibits VEGF protein synthesis at the post-transcriptional level. PTC299 is also a potent inhibitor of dihydroorotate dehydrogenase (DHODH). PTC299 shows good oral bioavailability and lack of off-target kinase inhibition and myelosuppression. PTC299 can be useful for the research of hematologic malignancies. | ||
| M28228 | UNC9994 | Dopamine Receptor |
| UNC9994, an analog of Aripiprazole, is a functionally selective β-arrestin-biased dopamine D2 receptor (D2R) agonist with EC50 <10 nM for β-arrestin-2 recruitment to D2 receptors. UNC9994 is simultaneously partial agonists of β-arrestin-2 translocation and antagonists of Gi-regulated cAMP production. Antipsychotic Activity. | ||
| M28298 | NCGC00249987 | Phosphatase |
| NCGC00249987 is a highly selective and allosteric Tyr phosphatase activity of Eya2 inhibitor with IC50s of 3 μM and 6.9 μM for Eya2 ED and MBP-Eya2 FL. NCGC00249987 specifically targets migration, invadopodia formation, and invasion of lung cancer cells. | ||
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