(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].
Ketotrexate sodium is an orally active antifolate and immunosuppressant. Ketotrexate sodium has good anti-inflammatory activity and is widely used in rheumatoid arthritis (RA). Ketotrexate sodium is used in research into cancer and autoimmune diseases[1][2].
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].
4’-C-Methyl-2-thiouridine is a purine nucleoside analogue. 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].
N-Ethylmaleimide (NEM) is a cysteine protease inhibitor[1]. N-ethylmaleimide specific inhibits phosphate transport in mitochondria[2].
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].
MPT0B014 is a tubulin polymerization inhibitor. MPT0B014 induces cancer cell apoptosis. MPT0B014 can be used for the research of cancer[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].
Mangafodipir, hepatocellular-specific contrast agent, is an efficacious inhibitor of CIPN (chemotherapy-induced peripheral neuropath) and other conditions caused by cellular oxidative stress. Mangafodipir shows no negative interference with the tumoricidal activity of chemotherapy[1][2].
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.
2-Aminoquinoline is a promising compound as bioavailable nNOS inhibitor but suffers from low human nNOS inhibition, low selectivity versus human eNOS, and significant binding to other CNS targets. 2-Aminoquinoline has the potential for the research of antineurodegenerative agents[1].
biotin-Bradykinin is a biological active peptide. (Biotin labeled HY-P0206)
(E)-2-(2-Methylbut-2-enamido)acetic acid is a Glycine (HY-Y0966) derivative[1].
EphB3-IN-1 is the first potent, selective inhibitor of EphB3 that exhibits inhibiting EphB3 autophosphorylation in cells with IC50 of 3 nM; causes foremost inhibition of EphB3 in a panel of 98 kinases, except for RIPK2 and PHKG2; abolishes the EphB3 autophosphorylation at Y608 and Y614 at 100 nM.
Bromo-PEG2-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
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GEM231 is an 18mer antisense oligonucleotide targeting the mRNA of the PKA-I (RIα regulatory subunit of cAMP dependent protein kinase type I ). GEM231 induces cell growth arrest, apoptosis, and differentiation in a variety of cancer cell lines in vitro and in tumors in vivo.
(R)-Mephenytoin ((-)-Mephenytoin), the R-enantiomer of Mephenytoin. Mephenytoin is an Anticonvulsant agent[1][2].
ASC-J9 is an androgen receptor degradation enhancer that effectively suppresses castration resistant prostate cancer cell proliferation and invasion.
Famoxadone (DPX-JE874) is a fungicide acting against a broad spectrum of fungi and is widely used in Integrated Pest Management strategies in different agricultural crops[1].
HIF-1/2α-IN-2 is an inhibitor of HIF-1/2α. HIF-1/2α-IN-2 decrease HIF-1/2α levels and induces iron starvation response by targeting Iron Sulfur Cluster Assembly 2 (ISCA2)[1].
PROTAC BRD9 Degrader-3 is a BRD9 bifunctional degrader for treating cancer.
NH-bis(C2-PEG2-NH-Boc) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
SB-612111 is a novel and potent human opiate receptor-like orphan receptor (ORL-1) antagonist with a high affinity for hORL-1 (Ki=0.33 nM). SB-612111 exhibits selectivity for μ-, κ- and δ-receptors with Ki values of 57.6 nM, 160.5 nM and 2109 nM, respecticely. SB-612111 effectively antagonizes the pronociceptive action of Nociceptin (HY-P0183) in an acute pain model[1].
3,5-Dichloro-2-hydroxybenzenesulfonic acid is used in conjunction with Ampyrone (HY-B1398) (4-AAP) and hydrogen peroxide (H2O2) for chromogenic quantification of peroxidase in coupled enzymatic reactions. 3,5-Dichloro-2-hydroxybenzenesulfonic acid is used to measure hydrogen peroxide production in conjunction with peroxidase[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].