Z-VRPR-FMK is an irreversible MALT1 protein inhibitor. Z-VRPR-FMK inhibits the growth and invasion of diffuse large B-cell lymphoma by inhibiting MALT1-induced NF-κB activation and MMP expression[1].
Glenzocimab (ACT017) is a Fab fragment of humanized anti-GPVI monoclonal antibody. Glenzocimab inhibits collagen-induced platelet aggregation. Glenzocimab has the potential for the research of acute ischemic stroke[1][2].
Sulfamonomethoxine sodium is a long acting sulfonamide?antibacterial?agent, used in blood kinetic studies,and blocks the synthesis of folic acid by inhibiting synthetase of dihydropteroate[1].
Desglymidodrine (ST 1059), the active metabolite of midodrine, is a selective α1-adrenoceptor agonist. Desglymidodrine is an effective arterial and venous vasoconstrictor and can be used to regulate blood pressure[1][2].
Flindokalner (BMS-204352) is a potassium channel modulator. Flindokalner is a positive modulator of all neuronal Kv7 channel subtypes expressed in HEK293 cells. Flindokalner is also a large conductance calcium-activated K channel (BKca) positive modulator. Flindokalner shows a negative modulatory activity at Kv7.1 channels (Ki=3.7 μM), and acts as a negative modulator of GABAA receptors. Flindokalner shows anxiolytic efficacy in vivo[1][2].
Caffeic acid-pYEEIE, a non-phosphopeptide inhibitor, exhibits potent binding affinity for the GST-Lck-SH2 domain[1].
D359-0396 is an orally active NLRP3 inflammasome inhibitor. D359-0396 inhibits pyroptosis and IL-1β release in macrophages. D359-0396 also inhibits the oligomerization of NLRP3, ASC and the cleavage of GSDMD. D359-0396 alleviates EAE, and also improves survival after septic shock in mice[1].
Ala-Ala-Pro-pNA is a tripeptide, including chromophoric amino acids Pro-pNA. Ala-Ala-Pro-pNA is targeted by tripeptidyl aminopeptidase (SM-TAP)[1].
Irigenin is a is a lead compound, and mediates its anti-metastatic effect by specifically and selectively blocking α9β1 and α4β1 integrins binding sites on C-C loop of Extra Domain A (EDA). Irigenin shows anti-cancer properties. It sensitizes TRAIL-induced apoptosis via enhancing pro-apoptotic molecules in gastric cancer cells[1].
5-Azidomethyl-2’-beta-methyl uridine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
(R)-Necrocide 1 (compound (R)-38) a potent anticancer agent. (R)-Necrocide 1 has antiproliferative activity[1].
Urolithin B is one of the gut microbial metabolites of ellagitannins, and has anti-inflammatory and antioxidant effects. Urolithin B inhibits NF-κB activity by reducing the phosphorylation and degradation of IκBα, and suppresses the phosphorylation of JNK, ERK, and Akt, and enhances the phosphorylation of AMPK. Urolithin B is also a regulator of skeletal muscle mass[1][2].
Globotriaosylsphingosine (lyso-Gb3) inhibits the growth of fibroblasts, as well as their differentiation into myofibroblasts, and collagen expression. Globotriaosylsphingosine can be used for Fabry disease research[1].
Ucasareotide dasaroxetan (SarTATE) is diagnostic agent with antineoplastic effect[1].
A potent and selective 5-HT2C receptor agonist with EC50 of 190 nM, with excellent selectivity for 5-HT2C over 5-HT2A; has minimal activation at either the 5-HT(2A) or 5-HT(2B) receptors, demonstrates robust efficacy in preclinical canine model of stress urinary incontinence (SUI) and attractive pharmacokinetic and safety properties.
Hydroxy-PEG4-C2-nitrile is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
L-Proline β-naphthylamide (hydrochloride) is a proline derivative[1].
Bromo-PEG4-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
DC-CPin7 is a potent inhibitor of CREB-binding protein (CBP) bromodomain with an IC50 of 2.5 μM[1].
Seclidemstat (SP-2577) mesylate is a potent noncompetitive and reversible KDM1A (LSD1) inhibitor (Ki=31 nM, IC50=13 nM). Seclidemstat mesylate promotes antitumor immunity in switch/sucrose nonfermentable (SWI/SNF) complex mutated ovarian cancer, as well as inhibit virus production, viral DNA replication, and late gene expression. Seclidemstat mesylate can be used for the research of Ewing Sarcoma[1][2].
BPH-715 is a bisphosphonate, inhibits Plasmodium liver-stage growth, with an IC50 of 10 μM for Plasmodium exoerythrocytic forms in HepG2 cells[1].
Bz-DTPA is a bifunctional chelator. Bz-DTPA can be used for preparing immunoconjugate of monoclonal antibody 2G3 labeled with indium-111[1].
LRRK2-IN-7 is a potent, selective, and CNS-penetrant LRRK2 kinase inhibitor with an IC50 of 0.9 nM. LRRK2-IN-7 shows >1000-fold selectivity over other kinases, ion channels, and CYP enzymes[1].
Methyldopate is an ethyl ester prodrug of α-Methyldopa (α-MD; HY-B0225). Methyldopa (L-(-)-α-Methyldopa) is an α-adrenergic agonist (selective for α2-adrenergic receptors). Methyldopate has the potential for severe hypertension research [1].
Gly-Gly-Phe-Gly-NH-CH2-O-CH2COOH is an ADC Linker that can be used to synthesize Drug-Linker Conjugates for ADC. Especially for the synthesis of Deruxtecan (HY-13631E), a toxic drug-linker conjugate[1].
3',4'-Dihydroxyacetophenone (3,4-DHAP), isolated from Picea Schrenkiana Needles exhibits a strong suppressive action against tyrosinase activity, with an IC50 of 10 μM. 3',4'-Dihydroxyacetophenone (3,4-DHAP) is a vasoactive agent and antioxidant[1][2].
ML375 (VU-0483253) is a potent, highly selective M5 NAM with submicromolar potency (human M5 IC50=300 nM, rat M5 IC50=790 nM, M1-M4 IC50> 30 uM), exhibts excellent multispecies PK, high CNS penetration, and enantiospecific inhibition.
Dapagliflozin impurity A (Compound A) is a dapagliflozin peroxide, a genotoxic impurity, can cause damage to human genetic material at very low concentrations, leading to genetic mutations and possibly tumorigenesis[1].
Rhodblock 6 is a Rho kinase (ROCK) inhibitor that inhibits phospho-MRLC (myosin regulatory light chain) localization[1].
SWS1 is a d-(+)-biotin-conjugated PD-L1 inhibitor (IC50: 1.8 nM) with anticancer activity. SWS1 can increase the number of tumor-infiltrating lymphocytes and exhibit anti-tumor efficacy in the B16-F10 mouse model (TGI=66.1%)[1].