| DC74550 |
EOS789 tosylate |
EOS789 tosylate is a potent, pan-phosphate transporter (NaPi-2b, PiT-1, PiT-2) inhibitor, inhibits phosphate uptake in a noncompetitive manner for human NaPi-IIb, PiT-1, and PiT-2 with IC50 of 6.8, 1.5 and 1.7 uM, respectively. |
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| DC74551 |
LY3358966 |
LY3358966 is a potent, selective inhibitor of the intestinal sodium-dependent phosphate cotransporter NPT2b (NaPi-2b, SLC34A2), inhibits phosphate uptake in human NPT2b expressed in CHO cells with IC50 of 32.4 nM. |
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| DC74552 |
TY-2136 |
TY-2136 is a next generation ROS1/TRK/ALK inhibitor with IC50 of 1.6 nM and 460.1 nM for ROS1 G2032R and TRKA G595R, respectively, inhibits ROS1/TRK/ALK mutations and overcomes drug resistance due to acquired solvent-front mutations. |
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| DC74553 |
1D-142 |
1D-142 is a novel small molecule RHO family of GTPase RAC1 inhibitor, inhibits Rac1-GEF interaction and reduces Rac1-mediated TNFα-induced NF-κB nuclear translocation during cell proliferation and migration. |
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| DC74554 |
CS7171 |
CS7171 is an effective, blood-brain barrier (BBB) permeable small molecule inhibitor of hippocampal Rac1 activity, rescues learning deficits in APP/PS1 mice. |
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| DC74555 |
GYS32661
Featured
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GYS32661 (GYS 32661) is a potent Rac inhibitor capable of inhibiting both Rac1 and Rac1b, inhibited activated Rac1 with IC50 of 1.18 uM in in vitro pull-down assays. |
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| DC74556 |
JKF-034 |
JKF-034 is an effective,blood-brain barrier (BBB) permeable small molecule inhibitor of hippocampal Rac1 activity, rescues learning deficits in APP/PS1 mice. |
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| DC74557 |
PREX-in1
Featured
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PREX-in1 is a specific small-molecule inhibitor of P-Rex1 and P-Rex2 Rac-GEF activity with IC50 of 4.5 uM (P-Rex1 DHPH Rac-GEF activity) in liposome-based GEF assay, inhibits P-Rex1 and P-Rex2 through their catalytic DH domain. |
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| DC74558 |
BAY 2686013 |
BAY 2686013 is a selective, allosteric antagonist of human pituitary adenylate cyclase activating polypeptide receptor (hPAC1-R) with IC50 of 0.92 and 0.4 uM in cAMP HTRF and Ca2+ release assays, respectively. |
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| DC74559 |
PA-915 |
PA-915 (PA915) is a small-molecule, non-peptide antagonist of the PACAP type I (PAC1) receptor, inhibits PACAP (1 nM)-induced phosphorylation of CREB in PAC1/CHO cells with IC50 of <10 pM. |
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| DC74560 |
Ro 25-1553 |
Ro 25-1553 is a potent, selective VIPR2 agonist and a cyclic peptide analog of vasoactive intestinal peptide (VIP), displaces the radioligand 125I-VIP from rat forebrain membranes with IC50 of 4.98 nM. |
|
| DC74229 |
Zenuzolac |
Zenuzolac (GLS1027, VGX-1027) is a small molecule immunosuppressant and an orally available isoxazole compound, inhibits toll-like receptor 4 (TLR4) activity, has shown promise for the treatment of several neuroinflammatory disorders. |
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| DC74630 |
Antiviral agent 17 |
Antiviral agent 17 is an anti-infection agent. |
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| DC74631 |
JAK-IN-21 |
JAK-IN-21 (Example 4) is a selective and potent JAK inhibitor. |
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| DC74632 |
Dimethylamiloride |
Dimethylamiloride is a Na(+)-H+ exchange inhibitor. |
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| DC74633 |
TCMDC-137332 |
TCMDC-137332 is a compound that exhibits antimalarial activity against Plasmodium falciparum with an IC50 value of 7 nM. |
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| DC74634 |
Seladelpar free acid |
Seladelpar, also known as MBX-8025 and RWJ-800025, is a selective peroxisome proliferator-activated receptor (SPPAR) -δ receptor agonist. MBX-8025 may have potential use for the treatment of dyslipidemia, metabolic syndrome, type 2 diabetes, and non-alcoholic steatohepatitis. |
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| DC74635 |
ATH434 mesylate |
ATH434, also known as PBT434, is a novel, brain-penetrant, inhibitor of α-synuclein aggregation. In transgenic animal models of Parkinson disease (A53T) and MSA (PLP-α-Syn), PBT434 reduced α-synuclein aggregation, preserved neurons and improved motor function. Glial cell inclusions were also reduced in a murine MSA model. PBT434 is thought to act by redistributing reactive iron across membranes, thereby blocking intracellular protein aggregation and oxidative stress. The affinity of PBT434 for iron is greater than that of α-synuclein but lower than that of iron trafficking proteins, e.g., ferritin. |
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| DC74636 |
Bromo-PADAP |
Bromo-PADAP is a dye agent for research use. Bromo-PADAP was reported for the spectrophotometric determination of uranium(VI). Bromo-PADAP is highly sensitive towards uranium, the uranyl complex having a molar absorptivity of 74,000 at 578 nm and pH 7.6. In the presence of a mixed masking solution only a few ions interfere seriously, and the method can be made specific for uranium by a preliminary extraction of uranium into tri-n-octylphosphine oxide, and direct development of the bromo-PADAP colour in the organic phase. Details are given for the determination of uranium in waters, ores, phosphoric acid and phosphate rocks, thorium oxide, and zirconium oxide. |
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| DC74637 |
Deuremidevir free base |
Deuremidevir, also known as VV116, JT001, and mindeudesivir, is a chemically-modified version of the antiviral remdesivir with oral bioavailability and potent activity against SARS-CoV-2. VV116 is a deuterated, tri-isobutyrate ester prodrug of the RDV parent nucleoside, and is rapidly metabolized into the parent nucleoside (116-N1) in the body. 116-N1 is intracellularly converted to the nucleoside triphosphate active form, which would interfere with the function of RNA-dependent RNA polymerase of SARS-CoV-2, thus exerting antiviral effects. VV116 showed potent activity against a panel of SARS-CoV-2 variants (alpha, beta, delta, and omicron) and excellent therapeutic efficacy in the mice model. Note: the non-labeled analog is called GS621763 (Cat#465727). |
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| DC74638 |
GLPG3667 |
GLPG3667 is an oral, reversible, and selective tyrosine kinase 2 (TYK2) inhibitor. It is being developed to treat inflammatory and auto-immune diseases. Biochemical assays showed that GLPG3667 displayed nanomolar potency on TYK2 with a selectivity over other JAK kinases >3-fold. In human PBMC, GLPG3667 showed comparable potency on the IFNα and IL-23 pathways (around 50 nM). Selectivity for TYK2 on the IFNα pathway was >14-fold and >19-fold toward the IL-2 and GM-CSF pathways in human PBMC and whole blood, respectively. Dermal ear inflammation in a mouse model of psoriasis driven by IL-23 was prevented by GLPG3667 with a minimal effective dose of 3 mg/kg given orally once daily. This effect was associated with a decrease in neutrophil infiltration and STAT3 phosphorylation at sites of inflammation. In healthy HV, GLPG3667 completely inhibited IFNα-induced STAT1 and STAT3 phosphorylation but did not impact IL-2- and GM-CSF-induced STAT5 phosphorylation. |
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| DC74639 |
Oligopeptide-10 |
Oligopeptide-10, also known as granactive oligopeptide-10, is a synthetic bio-active peptide composed of 15 amino acids. it can help manage acne-causing bacteria, both on its own and in conjunction with anti-acne superstar exfoliant salicylic acid. |
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| DC74640 |
Ganirelix acetate |
Ganirelix is is an antagonist of GnRH that competitively antagonizes the gonadotropic GnRH receptor, thereby mutating the pathway and causing rapid and reversible inhibition of gonadotropin (luteinizing hormone LH and follicle stimulating hormone FSH) secretion. Ganirelix Acetate acts by competitively blocking the GnRH receptors on the pituitary gonadotroph and subsequent transduction pathway. It induces a rapid, reversible suppression of gonadotropin secretion. The suppression of pituitary LH secretion by Ganirelix Acetate is more pronounced than that of FSH. |
|
| DC74641 |
HC-258 |
HC-258 is a Covalent Acrylamide TEAD Inhibitor That Reduces Gene Expression and Cell Migration. HC-258 reduces the CTGF, CYR61, AXL, and NF2 transcript levels and inhibits the migration of MDA-MB-231 breast cancer cells. Co-crystallization with hTEAD2 confirmed that HC-258 binds within TEAD’s PA pocket, where it forms a covalent bond with its cysteine. |
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| DC74642 |
Mtb ATP synthase-IN-1 |
Mtb ATP synthase-IN-1 is a potent Mycobacterium tuberculosis (Mtb) ATP synthase inhibitor, with MIC of 0.452-0.499 μg/mL against Mtb. |
|
| DC74643 |
PSMA I＆T |
PSMA I＆T is a ligand for making 177Lu-PSMA-I&T for Treatment of Metastatic Castration-Resistant Prostate Cancer. |
|
| DC74644 |
PSMA-I&F |
PSMA-I&F is a ligand for making 68Ga/177Lu-PSMA-I&F, which is a PSMA-Targeted Hybrid Tracer. PSMA-I&F is a useful agent for Nuclear and Fluorescence Imaging of Prostate Cancer. |
|
| DC74645 |
OXA-06 HCl |
OXA-06 is a potent ROCK inhibitor(IC50 = 10 nM). OXA-06 suppresses pMYPT1 and pCofilin levels in non-small cell lung carcinoma (NSCLC) cell lines. OXA-06 also inhibits anchorage-independent growth of NSCLC cell lines in vitro. |
|
| DC74646 |
EB-PSMA-617 |
EB-PSMA-617 is an Evans blue-modified prostate-specific membrane antigen (PSMA) 617 ligand for making 177Lu-EB-PSMA, which is potential useful for Metastatic Castration-Resistant Prostate Cancer. |
|
| DC74647 |
Neladalkib |
Neladalkib, also known as NVL-655, and NUV-655, is a selective, brain-penetrant ALK inhibitor with antitumor activity against the lorlatinib-resistant G1202R/L1196M compound mutation. NUV-655 (NVL-655) inhibited the kinase activity of ALK and ALK G1202R/L1196M with Kiapp < 5 nM in the presence of 1 mM ATP and with selectivity over TRKB. Across a panel of 335 wild-type kinases, NUV-655 (NVL-655) inhibited only 5 other kinases by >50% within 10-fold of its IC50 for ALK. NUV-655 (NVL-655) also selectively inhibited ALK in cells. It inhibited the growth of Ba/F3 cells driven by expression of EML4-ALK variant 1 (v1) with either wild-type kinase domain or drug-resistance mutations G1202R, G1202R/L1196M, or G1202R/G1269A at IC50 values < 10 nM and with selectivity over TRKB. In vivo, NUV-655 (NVL-655) induced regression at well-tolerated doses in a Ba/F3 EML4-ALKv1 G1202R/L1196M xenograft model. Furthermore, NUV-655 (NVL-655) demonstrated brain penetrance in rodent pharmacokinetic studies. |
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