N3-Allyluridine is a uridine analog. Uridine has potential antiepileptic effects, and its analogs can be used to study anticonvulsant and anxiolytic activities, as well as to develop new antihypertensive agents[1].
BSJ-04-122 is a potent, selective, covalent dual MKK4/7 inhibitor with IC50 of 4/181 nM, displays excellent kinome selectivity;BSJ-04-122 covalently targets a conserved cysteine (Cys247 for MKK4, and Cys261 for MKK7) located before the DFG motif.SJ-04-122 exhibits potent cellular target engagement and induces robust target-specific downstream effects.In breast cancer cell lines, BSJ-04-122 potently inhibited JNK phosphorylation, BSJ-04-122 significantly decreased levels of T183/Y185 pJNK at 5 uM, resulting in complete inhibition at 10 uM in MDA-MB-231 cells.The combination of the dual MKK4/7 inhibitor BSJ-04-122 with a selective, covalent JNK inhibitor (JNK-IN-8) demonstrated an enhanced antiproliferative activity against triple-negative breast cancer cells.
MMV390048 is a representative of a new chemical class of Plasmodium PI4K inhibitor (Kdapp=0.3 µM). MMV390048 binds to the ATP binding site of Plasmodium PI4K and does not bind to other P. falciparum and human kinases apart from human PIP4K2C, thus alleviating potential kinase-mediated safety concerns. MMV390048 is an antimalarial agent[1].
Aucubin is an iridoid glycoside with a wide range of biological activities, including anti-inflammatory, anti-microbial, anti-algesic as well as anti-tumor activities.IC50 value:Target:In vitro: Aucubin promotes neuronal differentiation and neurite outgrowth in neural stem cells cultured primarily from the rat embryonic hippocampus [1]. Aucubin significantly reversed the elevated gene and protein expression of MMP-3, MMP-9, MMP-13, iNOS, COX-2 and the production of NO induced by IL-1β challenge in rat chondrocytes [2]. In vivo:
5-BDBD, a potent and selective P2X4 receptor antagonist, inhibits rP2X4R-mediated currents, with an IC50 of 0.75 μM. 5-BDBD completely blocks the basal and acute hyperalgesia induced by nitroglycerin (NTG)[1][2].
7-O-Geranylscopoletin is a coumarin from the root of Atalantia monophylla. Various parts of this plant have been used for folk medicine for several purposes such as the treatment of chronic rheumatism, paralysis, antispasmodic, stimulant and hemiplegia[1].
JMJD6-IN-1 (Compound 1-3) is a JMJD6 inhibitor, with an inhibition rate of 82% at 10 μM. JMJD6-IN-1 inhibits MCF-7 and HCC4006 cell proliferation with IC50s of 19.2 μM and 25.2 μM. JMJD6-IN-1 can be used for research of cancers[1].
(R)-TCB2 is the R-enantiomer of TCB2. TCB2 is a potent anti-human interleukin-2 antibody, facilitates heterodimeric IL-2 receptor signaling and improves anti-tumor immunity[1].
PHA-690509 is an anti-ZikV compound that inhibits ZikV replication. PHA-690509 is also a CDK inhibitor, and inhibits caspase-3 activity[1][2].
Amredobresib is a potent inhibitor of BET. Amredobresib inhibits the binding of bromodomains to acetylated lysines on histone H3 and H4 and thus acts as important regulators of gene transcription. Amredobresib is useful for the research of acute myeloid leukemia (AML) and cancer (extracted from patent WO2019145410A1 and WO2021175824A1)[1].
Fmoc-Thr(tBu)-OH is a threonine derivative[1].
LIMK-IN-1 (Compound 14) is an inhibitor of LIM-Kinase (LIMK), with IC50s of 0.5 nM and 0.9 nM for LIMK1 and LIMK2, respectively. LIMK-IN-1 can be used for ocular hypertension and associated glaucoma research[1].
Vistusertib (AZD2014) is an ATP competitive mTOR inhibitor with an IC50 of 2.81 nM. AZD2014 inhibits both mTORC1 and mTORC2 complexes.
ELX-02 sulfate (NB-124 sulfate) is an investigational, advanced synthetic eukaryotic ribosome selective glycoside (ERSG). ELX-02 sulfate is being developed as a therapy for genetic diseases caused by nonsense mutations[1].
Phytosphingosine is a phospholipid and has anti-cancer activities. Phytosphingosine induces cell apoptosis via caspase 8 activation and Bax translocation in cancer cells[1].
PTP1B-IN-9 is a ubiquitin-proteasome system (UPS)-stressor. PTP1B-IN-9 inhibits ubiquitin-mediated protein degradation upstream of the 20S proteasomal catalytic activites. PTP1B-IN-9 triggers a ubiquitin-proteasome-system (UPS)-stress response without affecting 20S proteasome catalytic activities. Anticancer activity[1].
DPP-4-IN-2 (compound b2) is a potent DPP-4 (dipeptidyl peptidase 4) inhibitor, with an IC50of 79 nM. DPP-4-IN-2 is a structurally analogs of Alogliptin (HY-A0023A). DPP-4-IN-2 can be used for diabetes research[1].
1,3-Dicaffeoylquinic acid is a caffeoylquinic acid derivative that exhibits antioxidant activity and radical scavenging activity.
Boc-Asp(OBzl)-OSu is an aspartic acid derivative[1].
Driselase, a complex mixt. of wall-digesting enzymes, is a specific commercial fungal protoplasting enzyme preparation. Driselase is by far the most potent of the enzymes tested for polysaccharide digestion and greatly increases both tensile and indentation compliances, yet it does not induce wall creep, even after 6 h of digestion[1].
ASGPR ligand-1 is an asialoglycoprotein receptor (ASGPR) ligand compound. ASGPR ligand-1 can be used for kinds of diseases research[1].
Tauroursodeoxycholate is an endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits ERK.
Drp1-IN-1 (comp A-7) is a dynamin-1-like protein (Drp1) inhibitor, with an IC50 of 0.91 μM[1].
SN 2 is a novel and potent activator of TRPML3 ion channel with EC50 of 1.8±0.13 μM.
Fmoc-Tyr(tBu)-OPfp is a tyrosine derivative[1].
VU 0255035 is a highly selective, competitive and brain penetrant muscarinic M1 receptor antagonist with an IC50 of 130 nM. VU 0255035 reduces pilocarpine-induced seizures in mice. VU0255035 is used to examine the role of the M1 receptor in diverse situations[1].
Punicalagin is a polyphenol ingredient isolated from Pomegranate (Punica granatum L.) or the leaves of Terminalia catappa L.. Punicalagin is a anti-hepatitis B virus (HBV) agent and has antioxidant, anti-inflammatory, and anticancer effects[1][2][3].
SARS-CoV-2 nsp13-IN-2 (Compound C2) is a SARS-CoV-2 non-structural protein 13 (nsp13) small-molecule inhibitor with an IC50 of 42 μM against nsp13 ssDNA+ ATPase[1].
FAK-IN-7 (compound 5r) is a FAK inhibitor (IC50=11.72 µM). FAK-IN-7 has good anti-proliferative activity and can be used in cancer research[1].