potent

GLPG2938 (1-(2-Ethoxy-6-(trifluoromethyl)pyridin-4-yl)-3-((5-methyl-6-(1-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl)pyridazin-3-yl)methyl)urea) is a potent and selective antagonist of S1P2.

Bradykinin Potentiator C, a potent inhibitor of angiotensin-converting enzyme (ACE) with an inhibitory concentration (IC 50) of 7.1 μM for rabbit lung ACE, is regarded as a prototype for functional peptides [1].

Bradykinin Potentiator B (also known as Bradykinin Potentiating Peptide B), derived from the venom of Agkistrodon halys blomhoffi, serves as a potent ACE inhibitor. It effectively inhibits the activity of bradykinin inhibitory peptidase [1].

Potentillanoside A is a natural hepatoprotective compound [1].

Bradykinin potentiator-5 is a peptide inflammatory mediator, causes blood vessels to dilate (enlarge), and therefore causes blood pressure to fall.

Compound 2, known as KCC2 potentiators-1, acts as an enhancer of the potassium chloride cotransporter-2 (KCC2). It holds potential for applications in studies related to neurological disorders.

NMDA receptor potentiator-1 (Compound 1368) is a subunit-selective NMDA receptor enhancer with IC50 values of 4 μM for NR2C and 5 μM for NR2D expression.

OV-potentiator-28 is a potentiator of cancer virotherapy. OV-potentiator-28 significantly enhances virus replication-associated luciferase expression, specifically in tumors.

H2 antagonist

MRTX1133 is a KRAS G12D inhibitor (KD=0.2 pM) that is potent, selective, and non-covalent. MRTX1133 exhibits inhibitory activity against KRAS G12D-mutated tumors, but not against KRAS wild-type tumors.

RMC-6236 is an orally effective and novel triple complex RAS (ON) MULTI inhibitor, which is a potent non covalent inhibitor of multiple RAS variants in GTP binding state. RMC-6236 has anti-tumor activity and can be used in research related to RAS driven tumors. With rich experience in compound synthesis, we can provide fast customized synthesis services for this product according to your research needs.

Liproxstatin-1 is a potent and selective inhibitor of ferroptosis (IC50=22 nM). Liproxstatin-1 protects cells from ferroptosis induced by ferroptosis inducers (e.g., Erastin, RSL3).

Ruxolitinib (INCB018424) is a JAK1 2 inhibitor (IC50=3.3 2.8 nM) that is potent and selective. Rixolitinib exhibits antitumor activity and induces autophagy and apoptosis.

KDM4-IN-4 (compound 47) is a potent inhibitor of histone lysine demethylase 4 (KDM4), with a binding constant of approximately 80 μM for the KDM4A-Tudor domain. It inhibits H3K4Me3 binding to the Tudor domain in cellular contexts with an EC50 value of 105 μM, holding potential for anticancer research applications [1].

Iptacopan hydrochloride (LNP023 hydrochloride) is an orally bioavailable, highly potent and highly selective factor B inhibitor with an IC50 of 10 nM. Iptacopan hydrochloride shows direct, reversible, and high-affinity binding to human factor B with a KD of 7.9 nM.

LY-411575, a potent γ-secretase inhibitor, is with IC50 of 0.078 nM in the membrane and 0.082 nM in cell-based. It also suppresses Notch clevage with IC50 of 0.39 nM.

Marimastat (BB2516) (BB-2516) is a potent, broad spectrum matrix metalloprotease (MMP) inhibitor. MMP-9 (IC50=3 nM), MMP-1 (IC50=5 nM), MMP-2 (IC50=6 nM), MMP-14 (IC50=9 nM)and MMP-7 (IC50=13 nM).

O-Propargyl-Puromycin (OP-puro) is a potent protein synthesis inhibitor, a puromycin acetylene analog.

PAF (C16) is a potent MAPK and MEK ERK activator that induces increased vascular permeability. PAF (C16) (PAF (C16)) is a platelet-activating factor, a phospholipid-derived mediator and a ligand for PAF G protein-coupled receptor (PAFR). PAF (C16) has shown anti-apoptotic and anti-inflammatory activity in vitro, inhibiting Caspase-dependent apoptosis by interacting with its receptor (PAF-R) to perform cell signaling.

Elacridar (GG918) is a potent inhibitor of P-glycoprotein and BCRP.

Doramapimod (BIRB 796) is a highly potent inhibitor of p38 MAPK (Kd: 0.1 nM), but weakly inhibits c-RAF, Fyn, Lck, ERK-1, SYK, IKK2, and ZAP-70.

VBIT-12 is a potent inhibitor of VDAC1.

Silmitasertib (CX-4945) is a potent, orally bioavailable inhibitor of casein kinase 2 (CK2; Ki: 0.38 nM).

Bisindolylmaleimide I (GF109203X) is a potent and highly selective protein kinase C (PKC) inhibitor, exhibiting a Ki of 14 nM.