Usaramine N-oxide, a flavonoid isolated from Crotalaria pallida, possesses anti-inflammatory activities[1].
Enapotamab is an anti-AXL/UFO reference antibody. Enapotamab can be used to synthesis Bcl-xl inhibitor antibody-drug conjugates[1].
KAAD-Cyclopamine, a hedgehog signaling inhibitor, is a smoothened antagonist[1].
Ginisortamab (UCB6114) is a fully human IgG4P antiGremlin-1 monoclonal antibody. Ginisortamab has the potential for the research of gastrointestinal (GI) tumors[1].
SC-26196 is a potent, orally active Delta6 desaturase (D6D) inhibitor (IC50=0.2 µM in a rat liver microsomal assay). Antiinflammatory properties[1].
Sulbactam-d5 sodium (CP45899-d5) sodium is the deuterium labeled Sulbactam sodium. Sulbactam (CP45899) sodium is a competitive, irreversible beta-lactamase inhibitor. Sulbactam sodium shows antimicrobial activity against multidrug-resistant (MDR) acinetobacter calcoaceticus--Acinetobacter baumannii (Acb) complex[1][2].
(S,R,S)-AHPC-C5-COOH (VH032-C5-COOH) is a synthesized E3 ligase ligand-linker conjugate, contains the VH032 VHL-based ligand and a linker to form PROTACs. VH-032 is a selective and potent inhibitor of VHL/HIF-1α interaction with a Kd of 185 nM, has the potential for the study of anemia and ischemic diseases[1].
SIS3 is a cell-permeable and selective inhibitor of Smad3. It inhibits Smad3 phosphorylation with an IC50 of 3 µM.
DOTA-NHS-ester is a linker for affibody molecules and is applied in small animals PET, SPECT, and CT. DOTA-NHS-ester can be used to label radiotherapeutic agents or imaging probes for the detection of tumors[1].
Desrhamnosylmartynosideis extracted from the root of Scutellaria prostrata. Desrhamnosylmartynoside has absorption bands assignable to hydroxyl,α,β-unsanturate carbonyl groups[1].
α-L-Arabinofuranosidase is a glycosidic hydrolase. α-L-Arabinofuranosidase hydrolyse the nonreducing termini of the a-l-arabinofuranosyl residues as side chains of arabinoxylan, arabinan and arabinogalactan[1].
Nefopam (Fenazoxine) is an orally active, non-opioid and non-steroidal centrally acting analgesic agent. Nefopam blocks voltage-sensitive sodium channels (IC50=27 µM) and modulates glutamatergic transmission in rodents. Nefopam can be used in studies of neuropathic pain, anticonvulsant, as well as the prevention of postoperative shivering and hiccups[1][2][3].
MSC2360844 is a potent, orally active and selective PI3Kδ inhibitor, with an IC50 of 145 nM. MSC2360844 shows highly selective against a panel of 278 additional kinases[1].
AZ191 is a potent small molecule inhibitor that selectively inhibits DYRK1B with IC50 of 17 nM; selective for DYRK1B over both DYRK1A and DYRK2.IC50 value: 17 nM [1]Target: DYRK1B inhibitorin vitro: Using in vitro kinase assays, phospho-specific immunoblot analysis and MS in conjunction with AZ191 we now show that DYRK1B phosphorylates CCND1 at Thr(286), not Thr(288), in vitro and in cells. In HEK (human embryonic kidney)-293 and PANC-1 cells (which exhibit DYRK1B amplification) DYRK1B drives Thr(286) phosphorylation and proteasome-dependent turnover of CCND1 and this is abolished by AZ191 or DYRK1B RNAi, but not by GSK3β inhibitors or GSK3β RNAi.
biotin-Bradykinin is a biological active peptide. (Biotin labeled HY-P0206)
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NH-bis(C2-PEG2-NH-Boc) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Ezurpimtrostat hydrochloride (compound 2-3) is a potent and orally active anti-fibrotic agent. Ezurpimtrostat hydrochloride reduces significantly the liver fibrosis in DEN (diethyl nitrosamine) cirrhotic rat model. Ezurpimtrostat hydrochloride can be used for the research of fibrosis, cancer, autophagy and cathepsins B (CTSB), L (CTSL) and D (CTSD) related diseases [1].
Methyl (tert-butoxycarbonyl)-D-phenylalaninate is a phenylalanine derivative[1].
Bleomycin A5 (Pingyangmycin) is an orally active glycopeptide antibiotics. Bleomycin A5 has a role as an antineoplastic agent, an Apoptosis inducer and a bacterial metabolite[1][2].
MrgprX2 antagonist-2 is an MrgprX2 antagonist extracted from patent WO2021092262A1, example E163. MrgprX2 antagonist-2 can be used for the research of inflammatory disorders of the skin[1].
MKC3946 is a potent and soluble IRE1α inhibitor, used for cancer research.
c-Met-IN-2 is a potent, selective and orally available c-Met inhibitor, with an IC50 of 0.6 nM, with antitumor activity.
ODN 21158 is a potent G-modified TLR3 andTLR9inhibitor. ODN 21158 shows no cytotoxic. ODN 21158 nhibits IFN-α secretion in a dose dependent manner[1].
Quinagolide hydrochloride is a selective dopamine D2 receptor agonist, also is a prolactin inhibitor. Target: dopamine D2 receptor, prolactinQuinagolide is a selective, D2 receptor agonist (or prolactin-release inhibitor) that is used for the treatment of elevated levels of prolactin. Quinagolide is helpful in reducing prolactin levels to reduce milk production for certain medical reasons and to treat some types of infertility, breast problems and menstrual disorders. Quinagolide exerts a strong and specific inhibitory effect on prolactin release by acting directly on the prolactin-secreting cells of the anterior pituitary without reducing the levels of other pituitary hormones.
Tacrine hydrochloride is a potent inhibitor of both AChE and BChE, with IC50s of 31 nM and 25.6 nM, respectively. Tacrine hydrochloride is also a NMDAR inhibitor, with an IC50 of 26 μM. Tacrine hydrochloride can be used for the research of Alzheimer’s disease[1][2].
Indomethacin (Indometacin) sodium is a potent, orally active COX1/2 inhibitor with IC50 values of 18 nM and 26 nM for COX-1 and COX-2, respectively. Indomethacin sodium has anticancer activity and anti-infective activity. Indomethacin sodium can be used for cancer, inflammation and viral infection research.[1][2][3].
ML 10302 hydrochloride is a potent and selective 5-HT4 receptor agonist, with an EC50 of 4 nM。ML 10302 hydrochloride displays more than 680-fold selectivity over 5-HT3 receptor in binding assay[1][2].
Apigenin-7-glucoside exhibits significant anti-proliferative and antioxidant activity, scavengers of ROS.In vitro: exhibits significant anti-proliferative activity against B16F10 melanoma cells after 24 and 48 h of incubation. Apigenin-7-glucoside provoks an increase of subG0/G1, S and G2/M phase cell proportion with a significant decrease of cell proportion in G0/G1 phases. Apigenin-7-glucoside enhances melanogenesis synthesis and tyrosinase activity of B16F10 melanoma cells. [1] Api7G specifically induced the differentiation of CD34+ cells towards the erythroid lineage and inhibited the myeloid differentiation. [2] APIG had strong antioxidant activity against reactive oxygen species (ROS) in vitro in a concentration-dependent manner.
WRNA10 is a potent HIV-1 TAR RNA binder with an IC50 of 10 µM and an CC50 of 40 µM[1].