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VNPP433-3β is a molecular glue degrader, which degrades androgen receptor (AR) and its splice variants (AR-Vs) and MAP kinase-interacting serine/threonine protein kinase Mnk1/2. VNPP433-3β inhibits proliferation of cancer cell LNCaP, C4-2B and CWR22Rv1 with GI50 of 0.2, 0.3 and 0.31 μM. VNPP433-3β exhibits good pharmacokinetic characters in CD-1mouse and inhibits tumor growth in the CWR22Rv1 xenograft mouse model .
D-Dopa is a non-competitive, allosteric inhibitor for glutamate carboxypeptidase II (GCPII) with an IC50 of 200 nM. D-Dopa exhibits good pharmacokinetic characteristics, and low blood-brain barrier permeability in mouse model .
Influenza A virus-IN-14 (Compound 37) is an inhibitor for influenza virus type A (IAV), which inhibits H1N1 with an EC50 of 23 nM. Influenza A virus-IN-14 exhibits low cytotoxicity with CC50 of more than 100 μM. Influenza A virus-IN-14 inhibits cytopathic effect and improves the survival rates of cell Calu3. Influenza A virus-IN-14 exhibits synergistic activity with the neuraminidase inhibitor Oseltamivir (HY-13317). Influenza A virus-IN-14 exhibits poor pharmacokinetic properties in CD-1mouse .
GZNL-P36 is an orally active inhibitor for SARS-CoV-2 papain-like protease (PL pro), with an IC50 of 6.45 nM. GZNL-P36 inhibits SARS-CoV and its variants with EC50 range from 58.2 nM to 2.66 μM. GZNL-P36 exhibits a peak plasma concentration Cmax of 549 ng/mL, a half-life T1/2 of 1.45 h and a bioavailability of 74.7% in CD-1mouse. GZNL-P36 exhibits antiviral activity in SARS-CoV-2 XXB.1 infection in mouse .
Bfl-1-IN-5 (Compound (R,R,S)-26) is a selective inhibitor for Bfl-1 with an IC50 of 0.022 μM. Bfl-1-IN-5 promotes the caspase-3/7 activity with an EC50 of 0.37 μM, and inhibits the cell viability of SU-DHL-1 with an EC50 of 1.3 μM .
Methyl-4-oxoretinoate is a derivative of Retinoic acid (HY-14649). Methyl-4-oxoretinoate inhibits TPA (HY-18739)-induced ornithine decarboxylase (ODC) activity, and carcinogen-induced papillomas in mouse skin .
PRMT5-MTA-IN-1 (Compound A9a) is an inhibitor for protein arginine methyltransferase PRMT5-MTA. PRMT5-MTA-IN-1 inhibits the proliferation of colorectal cancer cell HCT116 wildtype and MTAP del mutant, with an IC50 of 16 nM and 2.47 μM. PRMT5-MTA-IN-1 exhibits good liver microsomal stability and film permeability. PRMT5-MTA-IN-1 exhibits good pharmacokinetic characteristics in CD-1 mice .
LQ-38 is an orally active inhibitor for soluble epoxide hydrolase (sEH) with an IC50 of 5.2 nM. LQ-38 exhibits anti-inflammatory activity in rat foot edema model and mouse acute pancreatitis model, exhibits analgesic effect in Acetic acid (HY-Y0319)-induced writhing mouse model .
Antiproliferative agent-53-d3 (Compound C1) is an inhibitor for theta-mediated end joining (TMEJ) in HEK293 cell with an IC50 of 0.14 µM. Antiproliferative agent-53-d3 is the inhibitor for CYP2C19 and CYP2C9 with IC50 of 0.77 and 3.1 µM. Antiproliferative agent-53-d3 inhibits the proliferation of DNA repair-compromised cells, with IC50 of 8.1 µM for BRCA2 -/- DLD-1. Antiproliferative agent-53-d3 exhibits good pharmacokinetic characteristics in CD-1 mice .
G-631 is a selective inhibitor for tankyrase. G-631 inhibits tankyrase auto-PARsylation (poly ADP ribosylation) with an IC50 of 7 nM, and inhibits Wnt signaling pathway. G-631 exhibits good pharmacokinetic characteristics in mice .
GPR17 modulator-1 (Compound 2-046) is a modulator for G protein-coupled receptor 17 GPR17, with an IC50<10 nM for hGPR17 in CHO. GPR17 modulator-1 exhibits moderate pharmacokinetic characteristics in mice. GPR17 modulator-1 ix blood-brain barrier (BBB) permeable .
WRN inhibitor 10 (Compound P24) is an inhibitor for the Werner helicase WRN with an IC50 of 1.1 nM. WRN inhibitor 10 inhibits the proliferation of cancer cell SW48 with IC50 of 39 nM. WRN inhibitor 10 exhibits good liver microsomal stability and film permeability. WRN inhibitor 10 exhibits good pharmacokinetic characteristics in CD-1 mice .
Androgen receptor-IN-6 (compound 16) is an orally available androgen receptor (Androgen Receptor) potent inhibitor (IC50=0.12 μM in vitro), targeting the disordered N-terminal domain (NTD). Androgen receptor-IN-6 has good Caco2 cell membrane permeability and has an oral activity (F/%) of 16% in male CD-1 mice .
SI-2 (EPH 116) is an inhibitor for steroid receptor coactivator-3 (SRC-3), which reduces the transcriptional activity and protein concentration of SRC-3 in cells, exhibits cytotoxicity in cancer cell, with IC50s ranging from 3-20 nM, inhibits migration of MDA-MB-468, induces apoptosis of MDA-MB-468. SI-2 inhibits the tumor growth in mouse models, without significant toxicity for heart and other major organs (20 mg/kg) .
SCH 57790 is a selective antegonist for muscarinic M2 receptor, which increases acetylcholine release, and thus improves cognitive performance. SCH 57790 reverses Scopolamine (HY-N0296)-induced memory deficits in mice, without significant toxicity (100 mg/kg).
D3S-001 is an orally active inhibitor for KRAS. D3S-001 inhibits the proliferation of KRAS G12C mutant H358 and MIA-PA-CA-2 with an IC50 of 0.6 and 0.44 nM. D3S-001 exhibits good metabolic stability in hepatocytes, liver microsomes, plasma and whole blood in various species. D3S-001 exhibits good pharmacokinetic characteristics and antitumor efficacy in mice .
Genz-669178 is an inhibitor for dihydroorotate dehydrogenase (DHODH) with IC50 of 0.015-0.05 μM in Plasmodium spp.. Genz-669178 inhibits P. berghei, P. falciparum strains 3D7 and Dd2 with IC50 of 0.068, 0.008 and 0.01 μM, respectively. Genz-669178 exhibits anti-malarial efficacy in P. berghei-infected mice with ED50 of 13-21 mg/kg/day. Genz-669178 exhibits good pharmacokinetic characteristics in mice .
SUN-1334H free base is an orally active inhibitor for histamine H1 receptor, with an IC50 of 20.3 nM and Ki of 9.7 nM. SUN-1334H free base inhibits histamine-induced contractions of isolated guinea-pig ileum with an IC50 of 0.198 μM. SUN-1334H free base inhibits histamine-induced bronchoconstriction in guinea pigs, histamine-induced skin wheals in beagle dogs, and ovalbumin-induced rhinitis in guinea pigs .
Endo CNTinh-03 is inhibitor for the elevation of cAMP and cGMP induced by agonist, such as G protein-coupled receptors, adenylate cyclase, and guanylate cyclase (IC50 is 4 μM). Endo CNTinh-03 inhibits cholera toxin- and Escherichia coli (STa) toxin- induced CFTR chloride current, ameliorates secretory diarrhea in mouse models, and prevents cyst growth in polycystic kidney disease model .
Ocifisertib hydrochloride (CFI-400945 hydrochloride) is the hydrochloride salt form of Ocifisertib (HY-12300). Ocifisertib hydrochloride is an orally active PLK4 inhibitor with a Ki and an IC50 of 0.26 nM and 2.8 nM. Ocifisertib hydrochloride inhibits growth of various cancer cells, arrests cell cycles at G2/M phase, and induces apoptosis. Ocifisertib hydrochloride exhibits antitumor efficacy in mouse model .
EGFR-IN-48 is a potent and orally active EGFR inhibitor with IC50s of 0.193 nM, 0.251 nM, 10.4 nM for EGFR d19/TM/CS, EGFR LR/TM/CS, EGFR WT, respectively. EGFR-IN-48 inhibits the proliferation of BaF3 EGFR del19/T790M/C797S and PC-9 EGFR del19/T790M/C797S cells with IC50s of 1.526, 66.7 nM, respectively .
D-Dopa is a non-competitive, allosteric inhibitor for glutamate carboxypeptidase II (GCPII) with an IC50 of 200 nM. D-Dopa exhibits good pharmacokinetic characteristics, and low blood-brain barrier permeability in mouse model .
Cd1a is a β-toxin derived from the African spider Ceratogyrus darlingi. Cd1a can regulate calcium ion channels. Cd1a inhibits human calcium ion channels (Cav2.2)(IC502.6 μM) and mouse sodium ion channels (Nav1.7). Cd1a can be used in the development of peripheral pain treatment drugs .
Anti-MouseCD1d Antibody (20H2 (HB323)) is a kind of rat IgG1 kappa in vivomouse antibody, targeting to CD1d. The recommend isotype control of Anti-MouseCD1d Antibody (20H2 (HB323)): Rat IgG1 kappa, Isotype Control (HY-P99979).
Anti-CD1a Antibody (OKT-6) is a kind of mouse IgG1 chimeric antibody, targeting to human CD1a. The recommend isotype control of Anti-CD1a Antibody (OKT-6): Mouse IgG1 kappa, Isotype Control (HY-P99977).
CD1D protein, in partnership with B2M, functions as an antigen-presenting protein, binding self and non-self glycolipids. It presents these molecules to T-cell receptors on natural killer T-cells, playing a pivotal role in immune responses. CD1D also interacts with MHC II and CD74, contributing to the coordination of the adaptive immune system. CD1D Protein, Mouse (HEK293, His) is the recombinant mouse-derived CD1D protein, expressed by HEK293 , with C-His labeled tag. The total length of CD1D Protein, Mouse (HEK293, His) is 305 a.a., with molecular weight of 45-50 kDa.
CD1D protein, in partnership with B2M, functions as an antigen-presenting protein, binding self and non-self glycolipids. It presents these molecules to T-cell receptors on natural killer T-cells, playing a pivotal role in immune responses. CD1D also interacts with MHC II and CD74, contributing to the coordination of the adaptive immune system. CD1D Protein, Mouse (HEK293, His-Fc) is the recombinant mouse-derived CD1D protein, expressed by HEK293 , with C-hFc, C-His labeled tag. The total length of CD1D Protein, Mouse (HEK293, His-Fc) is 305 a.a., with molecular weight of ~60.4 kDa.
CD1D protein, in partnership with B2M, functions as an antigen-presenting protein, binding self and non-self glycolipids. It presents these molecules to T-cell receptors on natural killer T-cells, playing a pivotal role in immune responses. CD1D also interacts with MHC II and CD74, contributing to the coordination of the adaptive immune system. CD1D1-B2M Heterodimer Protein, Mouse (HEK293, His) is a recombinant protein dimer complex containing mouse-derived CD1D1-B2M Heterodimer protein, expressed by HEK293 , with C-His labeled tag. CD1D1-B2M Heterodimer Protein, Mouse (HEK293, His), has molecular weight of ~40-50 & 12 KDa, respectively.
The CD1D2 protein plays a crucial role as an antigen-presenting molecule, binding self and non-self glycolipids and presenting them to T-cell receptors on natural killer T-cells. In partnership with B2M, it mediates immune responses, and its interactions with MHC II and CD74 highlight its significance in the complex network of immune system regulation. CD1D2-B2M Heterodimer Protein, Mouse (HEK293, His) is a recombinant protein dimer complex containing mouse-derived CD1D2-B2M Heterodimer protein, expressed by HEK293 , with C-His labeled tag.
Antiproliferative agent-53-d3 (Compound C1) is an inhibitor for theta-mediated end joining (TMEJ) in HEK293 cell with an IC50 of 0.14 µM. Antiproliferative agent-53-d3 is the inhibitor for CYP2C19 and CYP2C9 with IC50 of 0.77 and 3.1 µM. Antiproliferative agent-53-d3 inhibits the proliferation of DNA repair-compromised cells, with IC50 of 8.1 µM for BRCA2 -/- DLD-1. Antiproliferative agent-53-d3 exhibits good pharmacokinetic characteristics in CD-1 mice .
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