(-)-Sparteine (sulfate) is a quinolizidine alkaloid that can be extracted from Lupinus. (-)-Sparteine (sulfate) inhibits the release of acetylcholine and has anticonvulsant effects[1].
BETd-260 is a potent BET degrader based on PROTAC technology, with an IC50 of 30 pM against BRD4 protein in RS4;11 leukemia cell line.
Fmoc-Met-OPfp is a Methionine (HY-13694) derivative[1].
Bestatin is a natural, broad-spectrum, and competitive aminopeptidase inhibitor.
HPGDS inhibitor 3 is an orally active and highly potent peripherally restricted hematopoietic prostaglandin D synthase (H-PGDS) inhibitor with IC50 value of 9.4 nM and EC50 of 42 nM. HPGDS inhibitor 3 exhibits good selectivity, good pharmacokinetic parameters in mouse, rat, and dog, and no CNS toxicity. HPGDS inhibitor 3 has anti-inflammatory activity[1].
Chlormadinone is an antiandrogen drug. Chlormadinone combined with Tamsulosin shows greater improvement in subjective symptoms of BPH[1].
Riddelline, a pyrrolizidine alkaloid, is a potent genotoxic agent. Riddelline induces significant elevations in unscheduled DNA synthesis and S-phase synthesis in rat liver[1].
O-allylvanillin is O-allylchalcone derivative with anti-cancer effects[1]. O-allylvanillin inhibits THP-1, HL60, Hep-G2, MCF-7 cells growth with IC50 values of 74.76 μM, 63.52 μM, 90.99 μM, and 90.11 μM, respectively[1].
Anticancer agent 101 is a derivative of tetracaine. Anticancer agent 101 has anti-cancer activity[1].
MMP3 inhibitor 1 is a potent and highly selective MMP-3 inhibitor with an IC50 of 1 nM[1].
Trovafloxacin mesylate is a broad-spectrum quinolone antibiotic with potent activity against Gram-positive, Gram-negative and anaerobic organisms. Trovafloxacin mesylate blocks the DNA gyrase and topoisomerase IV activity. Trovafloxacin mesylate is also a potent, selective and orally active pannexin 1 channel (PANX1) inhibitor with an IC50 of 4 μM for PANX1 inward current. Trovafloxacin mesylate does not inhibit connexin 43 gap junction or PANX2. Trovafloxacin mesylate leads to dysregulated fragmentation of apoptotic cells by inhibiting PANX1[1][2][3].
Arnicolide D is a sesquiterpene lactone isolated from Centipeda minima. Arnicolide D modulates the cell cycle, activates the caspase signaling pathway and inhibits the PI3K/AKT/mTOR and STAT3 signaling pathways. Arnicolide D inhibits Nasopharyngeal carcinoma (NPC) cell viability in a concentration- and time-dependent manner[1].
Phenazine ethosulfate is a cationic dye (Ex=390 nm, Em=530 nm) and an electron acceptor that can be used in dye-linked enzyme assays. Phenazine ethosulfate is an intermediate for detecting nitric oxide reducatase (Nors) activity with the presence of ascorbic acid[1][2][3].
7-Iodo-2',3'-dideoxy-7-deaza-guanosine is a dideoxynucleoside that can be used in DNA synthesis and sequencing reactions[1].
AMG-337 is a potent and highly selective small molecule ATP-competitive MET kinase inhibitor. AMG 337 inhibits MET kinase activity with an IC50 of < 5nM in enzymatic assays.IC50 value: < 5nM [1]Target: METin vitro: AMG-337 demonstrates exquisite selectivity for MET when profiled against a diverse panel of over 400 protein and lipid kinases in a competitive binding assay. In cellular assays, AMG 337 inhibits HGF-dependent MET phosphorylation with an IC50 of < 10 nM. [1] AMG 337 is a selective inhibitor of Met, which inhibits multiple mechanisms of Met activation. [2]in vivo: AMG-337 demonstrates robust activity in MET-dependent cancer models. Oral administration of AMG 337 results in robust dose-dependent anti-tumor efficacy in MET amplified gastric cancer xenograft models, with inhibition of tumor growth consistent with the pharmacodynamic modulation of MET signaling.[1]
Phenylbutazone-13C12 is the 13C12 labeled Phenylbutazone. Phenylbutazone is an efficient reducing cofactor for the peroxidase activity of prostaglandin H synthase (PHS). Phenylbutazone, a hepatotoxin, is a nonsteroidal anti-inflammatory drug (NSAID). Phenylbutazone induces muscle blind-like protein 1 (MBNL1) expression and has the potential for ankylosing spondylitis research.
Collagens are extracellular matrix proteins and show many applications in food, cosmetic, pharmaceutical and biomedical industries. Collagens play an important role in the structure and function of skin, cartilage, bone and connective tissue[1].
Bis-PEG17-NHS ester is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
Prolylserine, a dipeptide, is an inhibitor of melanogenesis production in Mel-Ab cells. Prolylserine decreases expression of microphthalmia-associated transcription factor (MITF) and tyrosinase, induces phorphosylation of ERK, but not cAMP response element binding protein (CREB)[1].
DI-87 is an orally active and selective deoxycytidine kinase (dCK) inhibitor with an EC50 of 10.2 nM. DI-87 has antitumor activity and is used in combination therapy against tumors expressing dCK[1].
Salicylic acid-13C6 is the 13C-labeled Salicylic acid (HY-B0167). Salicylic acid is a precursor to and a metabolite of Aspirin (HY-14654), can inhibit cyclo-oxygenase-2 (COX-2) activity[1][2].
PF-CBP1 hydrochloride is a highly selective inhibitor of the CREB binding protein bromodomain.Target: CREBin vitro: PF-CBP1 modulates key inflammatory genes in primary macrophages. PF-CBP1 downregulates RGS4 in neurons, a target linked to Parkinson's disease. PF-CBP1 is 139-fold selective over BRD4 in the biochemical assays and >105-fold selective by ITC. F-CBP1 is also a potent inhibitor of EP300 (a result observed for other CBP inhibitors. [1]
(S)-Trolox is a water-soluble analogue of vitamin E, in which the phytyl chain is replaced with a carboxyl group. (S)-Trolox is frequently used as a model compound for studies of structural features, as well as a standard for evaluation of antioxidant activity. (S)-Trolox has potent and specific neuroprotective and antioxidant effects[1][2].
(S)-Salsolidine is a weak monoamine oxidase (MAO) inhibitor (Ki=63 μM). The R enantiomer of Salsolidine is more potent than the S form (Ki=26 μM)[1].
N-(Amino-PEG5)-N-bis(PEG4-acid) is a PEG-based PROTAC linker used in the synthesis of PROTACs. N-(Amino-PEG5)-N-bis(PEG4-acid) contains an amino group with two terminal carboxylic acids[1].
USP1-IN-3 is a selective USPI inhibitor. USP1-IN-3 inhibits USPI-UAFI with an IC50 value of ＜30 nM. USP1-IN-3 can be used for the research of cancer[1].
Deoxyarbutin is a new effective lighten ingredient, can effectively inhibit tyrosinase activity and melanin synthesis to get significant and lasting lightening effect.
Z-L-Aha-OH is a click chemistry reagent containing azide group[1].
EB-47 dihydrochloride, a potent and selective PARP-1/ARTD-1 inhibitor with an IC50 value of 45 nM, shows modest potency against ARTD5 with an IC50 value of 410 nM. EB-47 mimics the substrate NAD+ and extends from the nicotinamide to the adenosine subsite[1].
(S)-Metolachor, a derivative of aniline, is a major pesticide in use.