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BMP signaling inhibitor
LDN193189 HCl (DM-3189) is the hydrochloride salt of LDN193189, which is a selective BMP signaling inhibitor, and inhibits the transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 of 5 nM and 30 nM in C2C12 cell lines, respectively, 200-fold selectivity for BMP versus TGF-β.
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uPA inhibitor
UK-371804 is a potent and selective urokinase-type plasmogen activator (uPA) inhibitor with excellent enzyme potency (Ki=10 nM) and selectivity profile (4000-fold versus tPA and 2700-fold versus plasmin).
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Polymyxin B nonapeptide is a cyclic peptide obtained from Polymyxin B by proteolytic removal of its terminal amino acyl residue. Polymyxin B nonapeptide is less toxic, lacks bactericidal activity, and retains its ability to render gram-negative bacteria susceptible to several antibiotics by permeabilizing their outer membranes.
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P2X3R antagonist
Gefapixant is an orally active P2X3 receptor (P2X3R) antagonist with IC50s of ~30 nM versus recombinant hP2X3 homotrimers and 100-250 nM at hP2X2/3 heterotrimeric receptors.
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JAK1/JAK2 inhibitor
Momelotinib Mesylate (CYT387 Mesylate) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, appr 10-fold selectivity versus JAK3.
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- Ghazal Nabil, .et al. CD44 Targeted Nanomaterials for Treatment of Triple-Negative Breast Cancer, Cancers (Basel), 2021, Feb 20;13(4):898 PMID: 33672756
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CDK9 inhibitor
CDKI-73 is a potent CDK9 inhibitor with Ki of 4 nM; shows selective toxicity to CLL cells(LD50=80 nM) versus normal B cell and normal CD34+ cell(LD50>20 uM).
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GSK-3α/β inhibitor
CHIR-99021 monohydrochloride (CT99021 monohydrochloride) is a GSK-3α/β inhibitor with IC50 of 10 nM/6.7 nM; > 500-fold selectivity for GSK-3 versus its closest homologs CDC2 and ERK2, as well as other protein kinases.
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adenosine A1 receptor antagonist
Tonapofylline (BG 9928) is an orally active and selective adenosine A1 receptor antagonist with a Ki of 7.4 nM for human adenosine A1 receptor (hA1), which displays 915-fold selectivity versus human adenosine A2A receptor and 12-fold selectivity versus human adenosine A2B receptor and is used in development for the treatment of heart failure.
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steroid sulfatase inhibitor
Irosustat is a potent steroid sulfatase inhibitor, with an IC50 of 8 nM, and exhibits anti-breast cancer activity.
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11β-HSD1 inhibitor
AZD8329 is a potent 11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with an IC50 of 9 nM for human 11β-HSD1, displays excellent selectivity versus 11β-HSD2, 17β-HSD1 and 17β-HSD3.
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JAK1/2 inhibitor
Ruxolitinib sulfate (INCB018424 sulfate) is the first potent, selective JAK1/2 inhibitor to enter the clinic with IC50s of 3.3 nM/2.8 nM, and has > 130-fold selectivity for JAK1/2 versus JAK3.
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Vancomycin hydrochloride is an antibiotic for the treatment of bacterial infections. It acts by inhibiting the second stage of cell wall synthesis of susceptible bacteria.
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DNA topoisomerase I inhibitor
MAC glucuronide phenol-linked SN-38 is a pH-susceptible lactone MAC glucuronide phenol-linked SN-38 (DNA topoisomerase I inhibitor) drug linker. MAC glucuronide phenol-linked SN-38 is cytotoxic across L540cy cells and Ramos cells with IC50 values of 113 and 67 ng/mL, respectively.
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NaV 1.7 inhibitor
NaV1.7 inhibitor-1 is an efficacious voltage-gated sodium channel (NaV) 1.7 inhibitor with an IC50 of 0.6 nM for hNaV1.7, exhibits 80-fold selectivity versus hNaV1.5.
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SIRT1 activator
SRT 1460, a potent Sirtuin-1 (SIRT1) activator with an EC1.5 value of 2.9 μM, shows good selectivity for activation of SIRT1 versus SIRT2 and SIRT3 (EC1.5>300 μM), and is more potent than Resveratrol and the closest sirtuin homologues.
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broad-spectrum penicillin antibiotic
Penicillin V potassium is a broad-spectrum penicillin antibiotic used orally in the treatment of mild to moderate infections by susceptible gram-positive organisms.
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anticataract drug
Bendazac, also known as Bendazolic acid and AF-983, is an anticataract drug. It has been reported that Bendazac acts by preventing protein denaturation.
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CDK9 inhibitor
AZD4573 is a potent and selective inhibitor of CDK9, with fast-off binding kinetics and high selectivity versus other kinases, including other CDK family kinases.
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Rantes Rhesus Macaque Recombinant (CCL5)
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IP-10 Rhesus macaque Recombinant (CXCL10)
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Interleukin-8 Rhesus Macaque Recombinant
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Eotaxin Rhesus Macaque Recombinant (CCL11)
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Tumor Necrosis Factor-Alpha Rhesus Macaque Recombinant
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Serum Amyloid A (APO-SAA1) Rhesus Macaque Recombinant
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Interleukin-1 alpha Rhesus Macaque Recombinant
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Interleukin-5 Rhesus Macaque Recombinant
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Interleukin-1 beta Rhesus Macaque Recombinant
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Interleukin-13 Rhesus Macaque Recombinant
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Interleukin-6 Rhesus Macaque Recombinant
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Interleukin-4 Rhesus Macaque Recombinant
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Interleukin-3 Rhesus Macaque Recombinant
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Interleukin-16 Rhesus Macaque Recombinant
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Flt3-Ligand Rhesus Macaque Recombinant
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Thermostable dUTPase Pyrococcus Fruriosus Recombinant
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Granulocyte Macrophage-Colony Stimulating Factor Rhesus Macaque Recombinant
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Procalcitonin Rhesus Recombinant
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Tumor Susceptibility Gene 101 Human Recombinant
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S100 Calcium Binding Protein B Rhesus Macaque Recombinant
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Ciwujianoside B是从Eleutherococcus senticosus 叶中分离出来的,口服后能够渗透并在大脑中起作用。Ciwujianoside B显着增强识别记忆的能力。
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Dopamine Receptor 拮抗剂
Paliperidone (Invega)是一种非典型的抗精神病药。
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- Reiko Watanabe, .et al. Development of an In Silico Prediction Model for P-glycoprotein Efflux Potential in Brain Capillary Endothelial Cells toward the Prediction of Brain Penetration, J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967