ShK-Dap22 is a potent Kv1.3-specific immunosuppressive Polypeptide. ShK-Dap22 is a selective Kv1.3 channel blocker with IC50s of 23 pM, 1.8 nM, 10.5 nM, 37 nM, and 39 nM for mKv1.3, mKv1.1, hKv1.6, mKv1.4, and rKv1.2 channels, respectively[1].
Vitexolide E is a diterpenoid compound isolated from the leaves of the Malaysian species Vitex vestita. Vitexolide E shows cytotoxic activities against the HCT-116 cancer cell line and human fetal lung fibroblast MRC5 cell line[1].
Tet-213 is a antimicrobial peptide. Tet-213 has broad spectrum antibacterial activity. Tet-213 can promote infected wound repair[1].
Orlistat is a lipase inhibitor for obesity management that acts by inhibiting the absorption of dietary fats.
D-Biphenylalanine is a phenylalanine derivative[1].
Temsirolimus is an inhibitor of mTOR with an IC50 of 1.76 μM.
IL-1β-IN-1, cannabidiol derivative, is a potent IL-1β inhibitor. IL-1β-IN-1 has anti-inflammatory and pain-resolving properties[1].
CSF1R-IN-13 is a potent inhibitor of CSF1R. Colony stimulating factor 1 (CSF-1, also known as macrophage colony stimulating factor, M-CSF) is an important growth factor that controls bone marrow progenitor cells, monocytes, macrophages, and giants. CSF1R-IN-13 has the potential for the research of cancer diseases (extracted from patent WO2019134661A1, compound 32)[1].
CEP-9722, the prodrug of CEP-8983, is a selective and orally active PARP-1 and PARP-2 inhibitor with IC50s of 20 nM and 6 nM, respectively. CEP-9722 has anticancer effects[1][2].
AV-153, a 1,4-dihydropyridine (1,4-DHP) derivative, is an antimutagenic. AV-153 intercalates to DNA in a single strand break and reduces DNA damage, stimulates DNA repair in human cells in vitro. AV-153 interacts with thymine and cytosine and has an influence on poly(ADP)ribosylation. AV-153 has anti-cancer activity[1][2][3].
BI-2493 is a non-covalent and pan KRAS inhibitor. BI-2493 inhibits the interaction of GDP-bound KRAS with SOS1 in a biochemical assay using recombinant proteins with IC50s < 11nM. BI-2493 can be used in studies about KRAS-driven cancers.
SU5208 inhibits vascular endothelial growth factor receptor-2 (VEGFR2)[1].
α-Lapachone shows trypanocidal activity[1].
HG-7-85-01 is a type II ATP competitive inhibitor of wild-type and gatekeeper mutations forms of Bcr-Abl, PDGFRα, Kit, and Src kinases. HG-7-85-01 inhibits T315I mutant Bcr-Abl kinase, KDR and RET with IC50s of 3 nM, 20 nM and 30 nM, and is only weak or no inhibition of other kinases (IC50>2 μM). HG-7-85-01 inhibits the cell proliferation, which is mediated by the induction of apoptosis, and inhibition of cell-cycle progression[1].
Fmoc-D-Phe(2-CN)-OH is a phenylalanine derivative[1].
Butafenacil (WC-9717; CGA-276854) is an herbicide that inhibits protoporphyrinogen oxidase[1].
Tecarfarin sodium (ATI-5923 sodium) is a novel orally active non-competitive vitamin K epoxide reductase (VKOR) antagonist, impairs the activation of the vitamin K-dependent clotting factors II, VII, IX and X[1]. Tecarfarin sodium has the antithrombotic activity, attenuates venous and arterial thrombus formation in animal models by reducing the levels of the vitamin K-dependent coagulation factors[2].
Sibiromycin is a naturally produced glycosylated pyrrolobenzodiazepines (PBDs). Sibiromycin is also a potent antitumor antibiotic that binds covalently to DNA in the minor groove at the NH2 of guanine[1][2].
Beta-D-Glucopyranosyl nitromethane, as a salt of a strongly basic anion exchanger in the OH cycle, is a glycosyl derivative of nitromethane[1].
Piceatannol is a selective inhibitor of protein tyrosine kinase Syk. It could inhibit ICa,L, Ito, IKr, Ca2+ transients and Na+-Ca2+ exchange except IK1. Shows multiple biological activities such as anti-inflammatory, antiproliferative and immunomodulatory effects.In vitro: The treatment of human myeloid cells with piceatannol suppressed TNF-induced DNA binding activity of NF-κB. The effect of piceatannol was not restricted to myeloid cells, as TNF-induced NF-κB activation was also suppressed in lymphocyte and epithelial cells. Piceatannol also inhibited NF-κB activated by H2O2, PMA, LPS, okadaic acid, and ceramide. [1]
Nav1.7-IN-2 is an inhibitor of voltage-gated sodium channels (Nav), in particular Nav 1.7, with IC50 of 80 nM.IC50 value: 80 nMTarget: Nav 1.7Nav1.7-IN-2 is useful for the treatment of diseases treatable by inhibition of these channels, in particular, chronic pain disorder. The more detailed information please refer to WO 2011103196 A1. Nav1.7-IN-2 is a Nav1.7 channel inhibitor extracted from patent WO/2011103196 A1, compound example J, has an IC50 of 80 nM.
2-(Biotin-amido)-13-bis(carboxylethoxy)propane is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
S-(1-Hydroxy-2-methylpropan-2-yl) methanesulfonothioate is a glutathione cleavable ADC linker used for the antibody-drug conjugates (ADCs) and refers to the Alkyl-Chain composition. S-(1-Hydroxy-2-methylpropan-2-yl) methanesulfonothioate is the linker portions of the molecules employed for mAb attachment purposes[1].
DSPE-PEG5-propargyl is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Cypate, a cyanine dye, is a near infrared (NIR) fluorescent probe for in vivo tumor imaging[1][2].
ALK-IN-9 (compound 40) is a potent ALK inhibitor. ALK-IN-9 inhibits cell proliferation with IC50s of <0.2 nM, <0.2 nM, 0.2 nM for Ba/F3-EML4-ALK, KM 12 (TPM3-TRKA), KG-l cell (OP2-FGFR1), respectively[1].
Antitubercular agent-17 (Compound 8a) is an antitubercular agent with MIC values of 2, 2, 2 and 128 µg/ml against M. tuberculosis H37Rv, Spec. 192, Spec 210 and Spec. 800, respectively. Antitubercular agent-17 shows highly selective antimycobacterial effects[1].
Chlorobutanol is a pharmaceutical preservative with sedative-hypnotic actions. Chlorobutanol is active against a wide variety of Gram-positive and Gram-negative bacteria, and several mold spores and fungi[1][2].
Henatinib is an orally active small-molecule multikinase inhibitor that has demonstrated broad and potent antitumor activities. Henatinib inhibits the activity of VEGFR-2, c-kit, PDGFR with IC50 values of 0.6 nM, 3.3 nM and 41.5 nM, respectively. Henatinib significantly inhibits VEGFR-2 phosphorylation and its downstream signal pathway in human umbilical vein endothelial cells (HUVECs)[1].
N-Arachidonyldopamine is a potent and selective endogenous CB1 receptor agonist with a Ki of 250 nM[1]. N-Arachidonyldopamine is also a potent and selective TRPV1 agonist an with EC50 of ~ 50 nM[2].