NAV 26 (compound 26) is a selective voltage-gated sodium channel Nav1.7 blocker with an IC50 of 0.37 μM. NAV 26 can be used for pain research[1].
GBT 440 (Voxelotor) is an orally bioavailable modulator of sickle cell hemoglobin.
Abz-GIVRAK(Dnp) is the most efficient substrate for cathepsin B and is highly selective for this enzyme among lysosomal cysteine proteases. After Abz-GIVRAK(Dnp) is hydrolyzed, aminoacylbenziminosulfosuccinic acid (Abz-SAS) is released, and dinitrobenzoyl (Dnp) is also released. The product of this hydrolysis reaction, Abz-SAS, is fluorescent under ultraviolet light and can emit a fluorescent signal[1].
Lamprey LH-RH I is a gonadotropin-releasing hormone, elevates plasma steroid levels and stimulates ovulation in the lamprey without biological activity in other animal models[1].
ML327 is a blocker of MYC which can also de-repress E-cadherin transcription and reverse Epithelial-to-Mesenchymal Transition (EMT).
Parvisoflavanone is an isoflavanone that can be isolated from Mucuna pruriens[1].
Octenidine dihydrochloride is an effective antiseptic compound for skin mucous membranes and wounds.
EGFR/HER2/CDK9-IN-2 (Compound 9) is a potent inhibitor of EGFR/HER2/CDK9 with IC50s of 145.35, 129.07, and 117.13 nM, respectively. EGFR/HER2/CDK9-IN-2 exhibits remarkable antitumor activity[1].
Hirsutanonol 5-O-glucoside is a diarylheptanoid derivatives that can be isolated from Alnus hirsuta. Hirsutanonol 5-O-glucoside exhibits significant hepatoprotective effects against t-BHP-induced toxicity in HepG2 cells with 42.8% protection[1].
BPHA is a potent and orally active MMP-2, MMP-9 and MMP-14 inhibitor with 50s of 12 nM, 16 nM and 17 nM, respectively. BPHA does not inhibit MMP-1, -3, and -7 (the IC50s are 974, >1000, and 795 nM, respectively). BPHA has antiangiogenic and antitumor effects[1].
Khellin, a naturally occurring furochromone, is an EGFR inhibitor with an IC50 of 0.15 µM. Khelline has anti-proliferative activity in vitro. Khellin has antispasmodic and coronary vasodilator effects[1][2].
m-PEG4-C6-phosphonic acid ethyl ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
SHP2 IN-1 (compound 13) is an allergic inhibitor of SHP2 (PTPN11), with an IC50 of 3 nM.
(R)-SCH 42495 is the less active enantiomer of SCH 42495[1]. SCH 42495 is an orally active neutral metalloendopeptidase (NEP) inhibitor with antihypertensive effect. SCH 42495 is the orally active ethylester prodrug of SCH 42354[2].
AMG0347 is a transient receptor potential type V1 receptor antagonist. AMG0347 inhibits activation of the rat TRPV1 channel by heat (IC50 = 0.2 nm), protons (IC50= 0.8 nm), or capsaicin (IC50 = 0.7 nm)[1].
Tetramethyl-ammonium Bromide-d12 is the deuterium labeled TMAB[1].
Tepoditamab (MCLA-117) is a bispecific monoclonal antibody that binds to CLEC12A of myeloid cells and CD3 of cytotoxic T cells. Among others, CLEC12A is a myeloid differentiation antigen. Tepoditamab (MCLA-117) kills AML leukaemia mother cells and AML leukaemia stem cells, induces T cell-mediated proliferative lysis of AML cells and can be used in acute myeloid leukaemia (AML) research[1].
ATL 1102 is a novel second-generation antisense oligonucleotide to CD49d mRNA
Syringetin-3-O-rutinoside is an antioxidant compound[1]. Syringetin-3-O-rutinoside can be used for the synthesis of syringetin-O-glycoside derivatives[2].
Autocamtide-2-related inhibitory peptide, myristoylated is the myristoylated Autocamtide-2-related inhibitory peptide. Autocamtide-2-related inhibitory peptide is a highly specific and potent inhibitor of CaMKII with an IC50 of 40 nM[1].
DMH4 is a potent and selective inhibitor of VEGFR2 with an IC50 of 0.16 µM[1].
YK 4-279 is an inhibitor of RNA Helicase A (RHA) binding to the oncogenic transciption factor EWS-FLI1. YK-4-279 inhibits Ewing's sarcoma family tumor (ESFT) cell growth; YK-4-279 induces apoptosis. IC50 value:Target: RNA Helicase AES-FLI1 is an oncogenic fusion protein found in Ewing’s sarcoma, a family of undifferentiated tumors that occur throughout the body. The binding of RNA helicase A (RHA) to ES-FLI1 promotes its oncogenic function. YK-4-279 is an inhibitor of protein-protein interactions between ES-FLI1 and RHA. At 10 μM, YK-4-279 blocks RHA binding to ES-FLI1 and induces apoptosis of a panel of Ewing’s sarcoma tumor cell lines with IC50 values ranging from 0.5-2 μM. At 1.5 mg per dose, YK-4-279 reduces the growth of Ewing’s sarcoma orthotopic xenografts in mice after treatment with the inhibitor for two weeks.
NAAA-IN-3 (Compound 17a) is a potent and selective inhibitor of NAAA with an IC50 of 50 nM. NAAA is a cysteine amidase which preferentially hydrolyzes the endogenous biolipids palmitoylethanolamide (PEA) and oleoylethanolamide (OEA). NAAA-IN-3 has the potential for the research of inflammation and pain[1].
Tetraethylene glycol monotosylate is a cleavable and acylhydrazone-based ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
BCL6-IN-3 (example 20a) is a B-cell lymphoma 6 (BCL6) inhibitor with anti-tumor activity, extracted from patent WO2018215801A1. BCL6-IN-3 (example 20a) exhibits a GI50 of 70 nM in SU-DHL4 cells[1].
μ opioid receptor agonist 2 （Compound H-3）is an optically pure oxaspiro ring substituted pyrrolopyrazole derivative, acts as a MOR receptor agonist and can be used for the research of pain and pain related diseases[1].
Monoethyl phthalate-d4 is the deuterium labeled Monoethyl phthalate[1]. Monoethyl phthalate is a metabolite of diethyl phthalate. Monoethyl phthalate acts as a urinary biomarker of phthalates exposure indicating the risks of thyroid cancer and benign nodule[2][3].
Ascochlorin (Ilicicolin D), an isoprenoid antibiotic, mediates its anti-tumor effects predominantly through the suppression of STAT3 signaling cascade. Ascochlorin induces apoptosis. Anti-inflammatory activity[1][2][3].
Menin-MLL inhibitor 24 (compound A) is a menin-mixed-lineage leukemia 1 (menin-MLL) inhibitor. Menin-MLL inhibitor 24 can be used for the research of cancer[1].
Sutimlimab, a first-in-class complement protein component 1, s subcomponent (C1s) inhibitor, can be used for the research of cold agglutinin disease. C1s is a serine protease which cleaves C4 and C2 to form the C3 convertase[1].