(D-Leu6,Pro-NHEt9)-LHRH (4-9) is a biologically active peptide.
IMM-H007 is a potent TGFβ1 (transforming growth factor β1) antagonist. IMM-H007 has protective effects in cardiovascular diseases via activation of AMPK (AMP-activated protein kinase). IMM-H007 negatively regulates endothelium inflammation through inactivating NF-κB and JNK/AP1 signaling. IMM-H007 inhibits ABCA1 degradation. IMM-H007 resolves hepatic steatosis in HFD-fed hamsters by the regulation of lipid metabolism. IMM-H007 can be used for the research of nonalcoholic fatty liver disease (NAFLD) and inflammatory atherosclerosis[1][2][3].
CRF1 receptor antagonist-1 (Compound 2) is a CRF1 receptor antagonist. CRF1 receptor antagonist-1 can be used for research of congenital adrenal hyperplasia (CAH)[1].
ZD-7114 hydrochloride is a potent and selective agonist of β3-adrenergic. ZD-7114 hydrochloride is a selective thermogenic agent in vivo. ZD-7114 hydrochloride can be used in study obesity and diabetes[1].
DAPI dihydrochloride (4',6-diamidino-2-phenylindole) is a fluorescent stain by binding in the minor grove of A-T rich sequences of DNA.
Tamoxifen-d3 is the deuterium labeled Tamoxifen[1]. Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells[2][3][4]. Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively[6]. Tamoxifen activates autophagy and induces apoptosis[5]. Tamoxifen also can induce gene knockout of CreER(T2) transgenic mouse[7].
Nikethamide, one of the respiratory central stimulants, is used to treat respiratory failure in clinical practice.
3-Acetylpinobanksin-7-methyl ether is a natural product that can be isolated from propolis[1].
CaLL is an antimicrobial peptide. CaLL has antibacterial activity against B. anthracis, B. anthracis (vegetative), and B. cepacia (MIC: 7.8, 31.3, 31.3 μg/mL)[1].
KRAS G12C inhibitor 55 (Compound 1) is a KRAS G12C inhibitor[1].
Azide-PEG12-alcohol is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Laurycolactone B is a natural product from Eurycoma longifolia Jack[1].
Huangjiangsu A, pseudoprotodioscin, methyl protobioside, protodioscin, and protodeltonin, isolated from D. villosa. Huangjiangsu A has hepatoprotective potential against H2O2-induced cytotoxicity and ROS generation and could be promising as potential therapeutic agents for liver diseases[1].
Fraxidin is a class of coumarin isolated from the roots of Jatropha podagrica, exhibits antibacterial activity against Bacillus subtilis with an inhibition zone of 12 mm at a concentration of 20 µg/disk[1][2].
TAK-659 hydrochloride is a potent, selective and orally available spleen tyrosine kinase (Syk) inhibitor with an IC50 of 3.2 nM.
HBV-IN-39-d3 (Example 14) is a deuterated HBV-IN-39 (Example 13). HBV-IN-39 is an HBV inhibitor. HBV-IN-39-d3 has better oral bioavailability than HBV-IN-39[1].
ML-097 (CID-2160985) is a pan Ras-related GTPases activator that can activate Rac1, cell division cycle 42, Ras, and Rab7[1].
INSCoV-614(1B) is a potent inhibitor of Mpro (3CLpro). Proteases (PL pro and 3CL pro) are involved with transcription and replication of the virus. INSCoV-614(1B) has the potential for the research of SARS-CoV-2 infection (extracted from patent WO2021219089A1)[1].
NPS ALX Compound 4a is a potent and selective 5-hydroxytryptamine6 (5-HT6) receptor antagonist with an IC50 of 7.2 nM, which also has a great binding affinity with Ki of 0.2 nM[1].
ODN 24987 is a Guanine-modified inhibitory oligonucleotides (ODN), targeting TLR9. ODN 24987 can inhibit IL-6 and IFN-α release. ODN 24987 can be used for research immune disorders. ODN 24987 sequence: 5’-C-C-T-G-G-C-c7G-G-G-G-3’[1].
Ro19-4603 is a benzodiazepine inverse agonist. Ro19-4603 antagonizes ethanol (EtOH) intake in alcohol-preferring rats[1].
N2,2'-O-Dimethylguanosine 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].
Pomalidomide-C3-adavosertib is a rapid and selective Wee1 degrader (IC50=3.58 nM). Pomalidomide-C3-adavosertib shows anti-cancer cell proliferation activity, and induces apoptosis[1].
PROTAC Linker 8 (Compound 15b) is a PROTAC linker can be used in the synthesis of a series of SNIPER(ER)s. SNIPER(ER)s contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. SNIPER(ER)s induce polyubiquitylation and proteasomal degradation of the target proteins in the cells[1].
Monomethyl auristatin E intermediate-9 is an intermediate reagent in the synthesis of Monomethyl auristatin E (HY-15162). Monomethyl auristatin E (MMAE) is a microtubule/tubulin inhibitor with anticancer activity. MMAE is widely used as the cytotoxic component (ADC Cytotoxin) of antibody-drug conjugates (ADCs)[1].
LCB 03-0110 is a potent, ATP-competitive inhibitor of Discoidin domain receptor (DDR) family and c-Src tyrosine kinase family, as well as Btk and Syk; potently inhibits the activated tyrosine kinase activity of DDR2 (IC50=6 nM), and nonactivated form of DDR2 (IC50=145 nM); suppresses collagen-induced autophosphorylation of DDR1 and DDR2 with IC50 of 164 and 171 nM in cell-based assays; inhibits all eight Src family kinases with IC50 of 2-20 nM; suppresses the proliferation and migration of primary dermal fibroblasts induced by TGF β1 and type I collagen (IC50=194 nM), inhibits cell migration and nitric oxide, iNOS, COX2, and TNF-α synthesis in LPS-activated J774A.1 macrophage cells; suppresses hypertrophic scar formation in wound healing models.
2,3′,4′,5-Tetrachlorobiphenyl-3,4,6-d3 is the deuterium labeled 2,3′,4′,5-Tetrachlorobiphenyl[1].
Cytarabine triphosphate (Ara-CTP), an active metabolite of Cytarabine, is a competitive inhibitor of DNA synthesis. Intracellular Cytarabine triphosphate levels can be used to predict chemosensitivity of leukemic blasts to Cytarabine[1].