About 32 results found for searched term "Wee1" (0.076 seconds)
|WEE1-IN-4 is a potent checkpoint Wee1 kinase inhibitor with an IC50 of 0.011 μM.
|WEE1-IN-5 is a potent WEE1 inhibitor with an IC50 value of 0.8 nM. WEE1-IN-5 inhibits phospho-CDC2. WEE1-IN-5 abrogates the G2 check point, increasing sensitivity to DNA damaging agents in cancer cells.
|BSI-201, NSC-746045, IND-71677
|Iniparib is an irreversible, noncompetitive inhibitor of PARP1 that disrupts binding between PARP1 and DNA by interacting with the DNA binding domain.
|Fluvastatin sodium is an orally active, potent and competitive HMG-CoA reductase inhibitor with IC50 value between 40 and 100 nM at human liver microsomes.
|Adavosertib (AZD1775, MK-1775) is a small pyrazolacil derivative, an effective ATP competitive specific inhibitor of WEE1 kinase, with IC50 of 5.2 nM. It can inhibit G2 phase DNA damage test sites.
|YYA-021 is a CD4-mimic HIV entry inhibitor, competitively inhibiting the interaction between gp120 and CD4.
|Tyrphostin AG 1024
|AG-1024 (Tyrphostin) inhibits IGF-1R autophosphorylation with IC50 of 7 μM, is less potent to IR with IC50 of 57 μM and specifically distinguishes between InsR and IGF-1R (as compared to other tyrphostins).
|NVP-TAE684 is a highly potent and selective small-molecule ALK inhibitor, which blocked the growth of ALCL-derived and ALK-dependent cell lines with IC(50) values between 2 and 10 nM.
|11-Oxo-Mogroside V is a natural sweetener with strong antioxidant activity. 11-OXo-Mogroside V had a significant inhibitory effect on reactive oxygen species, and the EC50 of O2-, H2O2 and *OH were 4.79, 16.52 and 146.17 μg/mL, respectively.
|Eupalinolide A, isolated from Eupatorium lindleyanum, induces the expression of HSP70 via the activation of HSF1 by inhibiting the interaction between HSF1 and HSP90.
|LDC4297 is a novel CDK7 inhibitor (IC50=0.13±0.06 nM for CDK7 versus IC50s between 10 nM and 10,000 nM for all other analyzed CDKs).
|Epigenetic Reader Domain
|Mi-538 is an inhibitor of the interaction between MENin and MLL fusion protein with an IC50 value of 21 nM.
|Entrectinib (RXDX-101) is an orally bioavailable pan-TrkA/B/C, ROS1 and ALK inhibitor with IC50 ranging between 0.1 and 1.7 nM.
|SAR 1118; Xiidra
|Lifitegrast is an antagonist of integrin lymphocyte function associated antigen-1 (LFA-1). The IC50 of Jurkat T cells to icAM-1 was 2.98nM. Lifitegrast blocks the interaction between LFA-1 and ICAM-1, thereby reducing T cell activity and cytokine secretion.
|ASTX660 is a potent, non-peptidomimetic antagonist of cIAP1/2 and XIAP, it potently inhibited the interactions between a SMAC-derived peptide and the BIR3 domains of XIAP (BIR3-XIAP) and cIAP1 (BIR3-cIAP1) with IC50 values less than 40 and 12 nmol/L, respectively.
|Pembrolizumab (pembrolizumab) is a humanized anti-PD-1 monoclonal antibody that blocks the interaction between PD-1 and its ligands PD-L1 and PD-L2. It has immune checkpoint inhibitory activity and antitumor activity. MW: 146.286 KD.(Pembrolizumab does not recognize murine PD-1 protein, humanized mice or mice expressing human PD-1 gene are required).
|Emodin is an anti-SARS-CoV compound that blocks the interaction between the SARS-coronavirus spike protein and angiotensin converting enzyme 2 (ACE2). Emodin inhibited casein kinase 2 (CK2) and 11β-HSD1. Emodin can also induce necrotic apoptosis of glioma U251 cells and inhibit U251 cell proliferation by targeting the TNF/RIPK1/RIPK3 signaling pathway.
|PD-407824 is a Wee1/Chk1 inhibitor.
|CU-CPT22 is the first probe for the complex between toll-like receptors TLR1 and TLR2. CU-CPT22 shows dose-dependent inhibitory effects blocking Pam3CSK4-induced TLR1/2 activation with an IC50 of 0.58 ± 0.09 µM.
|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.
|PD0166285 is a potent Wee1 inhibitor and Chk1 inhibitor with IC50s of 24 nM and 72 nM, respectively.
|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.
|ZN-c3 is a potentially first-in-class and best-in-class orally active, potent and selective Wee1 inhibitor (IC50=3.9 nM). zN-c3 can be used in cancer research.
|Deoxynyboquinone is a potent inducer of cancer cell death with IC(50) values between 16 and 210 nM.
|TK216 is an orally active and potent E26 transformation specific (ETS) inhibitor. TK216 directly binds EWS-FLI1 and inhibits EWS-FLI1 protein interactions. TK216 blocks the binding between EWS-FLI1 and RNA helicase A. TK216 has anticancer activity.
|TMPyP4 tosylate (TMP 1363) is a quadruplex-specific ligand, which inhibits the interaction between G-quadruplexes and IGF-1. TMPyP4 tosylate (TMP 1363) is a telomerase inhibitor with antitumor effects in osteosarcoma cell lines.
|RBPJ Inhibitor-1 (RIN1) is a first-in-class RBPJ inhibitor that blocks the interaction between RBPJ and SHARP.RBPJ Inhibitor-1 (RIN1) inhibits the proliferation of Notch-dependent tumor cells.
|ABX464 is a reverse transcriptase (RT) inhibitor with anti-HIV activity that inhibits HIV-1 replication in stimulated peripheral blood mononuclear cells (PBMCs) from five different donors, with IC50 values between 0.1 μM and 0.5 μM, and can be used in studies related to ulcerative colitis.
|SEC inhibitor 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.
|K-975 is a potent, selective and orally active TEAD inhibitor that strongly inhibits protein-protein interactions between YAP1/TAZ and TEAD.
|ARV471; 2229711-08-2; PF-07850327
|Vepdegestrant (ARV-471) is an oral estrogen receptor PROTAC protein degrader for breast cancer.ARV-471 is a heterobifunctional molecule that promotes the interaction between estrogen receptor alpha and intracellular E3 ligase complexes.ARV-471 causes ubiquitination and subsequent degradation of the estrogen receptor via the proteasome.ARV-471 potently degrades ER-positive The ER in breast cancer cell lines is potently degraded by ARV-471 with a DC50 value of approximately 2 nM.
|ASP2453 is a potent, selective and covalent inhibitor of KRAS G12C. ASP2453 inhibits Son of Sevenless (SOS)-mediated interactions between KRAS G12C and Raf with an IC50 value of 40 nM.
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