ASP8062 is a potent, selective GABA B receptor positive allosteric modulator (PAM), positive allosteric modulating activity for human and rat GABAB receptors, exerts analgesic effects in rat model of fibromyalgia.

A selective protein phosphatase PHLPP inhibitor with IC50 of 4 uM for PP2C domain of PHLPP2.

(R)-(-)-α-Methylhistamine dihydrochloride is a potent, selective and brain-penetrant agonist of H3 histamine receptor, with a Kd of 50.3 nM. (R)-(-)-α-Methylhistamine dihydrochloride can enhance memory retention, attenuates memory impairment in rats.

Euscaphic acid, a DNA polymerase inhibitor, is a triterpene from the root of the R. alceaefolius Poir. Euscaphic inhibits calf DNA polymerase α (pol α) and rat DNA polymerase β (pol β) with IC50 values of 61 and 108 μM.

RG7834 R-isomer, also known as RO0321, is an enantiomer of RG7834 and a negative control for RG7834. RG7834 R-isomer has R-configuration with CAS#2072057-18-0. RG7834 is a novel oral HBV viral gene expression inhibitor that blocks viral antigen and virion production. RG7834 is highly selective for HBV, and has a unique antiviral profile that is clearly differentiated from nucleos(t)ide analogues.

SR-3576 is a potent JNK3 inhibitor that is highly selective over p38.

TCO-PEG2-NHS ester is a PEG/Alkyl/ether-based PROTAC linker can be used in the synthesis of PROTACs. TCO-PEG2-NHS ester is a click chemistry reagent, it contains a TCO group that can undergo an inverse electron demand Diels-Alder reaction (iEDDA) with molecules containing Tetrazine groups.

PST3.1a is a N-acetylglucosamine glycosyltransferase (MGAT5) inhibitor with the IC50 of 2 μM. PST3.1a inhibits glioblastoma-initiating cell invasiveness and proliferation.

Nisoxetine hydrochloride is a potent and selective inhibitor of noradrenaline transporter (NET), with a Kd of 0.76 nM. Nisoxetine hydrochloride is an antidepressant and local anesthetic, it can block voltage-gated sodium channels.

ML353 (VU0478006) is a highly potent, selective, MPEP-site silent allosteric modulator of mGlu5 receptor with with sub-100 nM affinity.

Novel potent and selective antagonist of human Complement C3a receptor

UoS12258 (UoS-12258) is a selective, positive allosteric modulator of the AMPA receptor with pEC50 of 5.6.

Novel potent and selective NADPH oxidase inhibitor, targeting Nox4 in TGFβ-induced lens epithelial to mesenchymal transition

NUNC10112785 is a serine/threonine kinase inhibitor with a human GSK-3β IC50 of 0.031 μM, human CDK-2 IC50 of 0.016 μM, and human CDK-4 IC50 of 1.99 μM. UNC10112785 can be used for the research of type 2 diabetes.

AZ-8838 (AZ8838) is a potent, and selective PAR2 antagonist with Kd of 125 nM.

Novel potent inhibitor of the GRK2--​dependent bovine tubulin oxidation

PD-089828 is an ATP competitive inhibitor of FGFR-1, PDGFR-β and EGFR (IC50s=0.15, 1.76, and 5.47 µM, respectively) and a noncompetitive inhibitor of c-Src tyrosine kinase (IC50=0.18 µM). PD-089828 also inhibits MAPK with an IC50 of 7.1 µM.

GSK-J1 is a potent and selective inhibitor of the H3K27 histone demethylases JMJD3 and UTX (IC50 = 60 nM for human JMJD3 in vitro).

PF9601N is a selective and potent monoamine oxidase B inhibitor that exhibit anti-Parkinsonian effects in several models of PD.

LDN192960 (LDN 192960) is a highly potent and selective DYRK2 inhibitor with IC50 of 13 nM toward DYRK2 at 50 uM ATP.LDN192960 suppresses Thr25 RPT3 phosphorylation in a dose-dependent manner in HEK293T cells transiently overexpressing DYRK2-FLAG, with maximal effects at 1-10 uM.LDN192960 does not inhibit any of the 130+ kinases including other CMGC kinase family members that are closely related to the DYRKs.LDN192960 binds to the ATP-binding pocket of DYRK2, also potently inhibits DYRK1A, DYRK3 and Pim with IC50 of <3, 122 and 10 nM, respectively.LDN192960 perturbs proteasome activity, induces cell death, and impedes proliferation and invasion on MDA-MB-468 cells.LDN192960 impedes MM progression and delays myeloma-mediated bone degeneration.LDN192960 induces cytotoxicity in bortezomib-resistant MM, both in cells and in vivo. significantly alleviates tumor burden in standard and PDX TNBC models.

CRANAD-2 is a difluoroboron-derivatized curcumins as near-infrared probe for in vivo detection of amyloid-beta deposits. Upon interacting with Abeta aggregates, CRANAD-2 undergoes a range of changes, which include a 70-fold fluorescence intensity increase, a 90 nm blue shift (from 805 to 715 nm), and a large increase in quantum yield. Moreover, this probe also shows a high affinity for Abeta aggregates (K(d) = 38.0 nM), a reasonable log P value (log P = 3), considerable stability in serum, and a weak interaction with albumin. After intravenous injection of this probe, 19-month-old Tg2576 mice exhibited significantly higher relative signal than that of the control mice over the same period of time.

LLL12B is a selective STAT3 inhibitor that suppresses Th17 development, specifically inhibits STAT3 and suppresses Th17 differentiation and expansion.

DPNB-ABT594 is a nitrobenzyl-caged ABT594 and activates nAChRs containing the α4β2 subunits with good selectivity than the α7 subunit. DPNB-ABT594 can be used to map the distribution of nAChRs on neurons of the medial habenula (MHb) and helps to gain a deeper understanding of the nAChR‐mediated Ca2+ signalling in the MHb.

Alogabat (example 8) is a GABAA α5 receptor positive allosteric modulators (PAMs) (extracted from patent WO2018104419A1).

MM0299 analog 13 (MM 0299 derivative 13) is a potent, selective, orally bioavailable, brain-penetrant inhibitor of lanosterol synthase (LSS, competition EC50=28.7 nM) with anti-proliferative activity.

LB42708 is an orally active farnesyltransferase (FTase) inhibitor with IC50 of 0.8, 1.2, and 2.0 nM toward H-ras, N-ras, and K-ras, respectively

CPL500036 (CPL-500036) is a highly potent, selective and orally bioavailable PDE10A inhibitor with IC50 of 35 nM.CPL500036 is highly selective for PDE10A over other PDEs and common off-targets.CPL500036 effectively penetrates the brain where increases cAMP/cGMP levels and phosphorylates effector proteins like AMPA subunits.CPL500036 reduced sensorimotor deficits in 6-OHDA-lesioned rats.Acute and chronic CPL500036 did not reduce effects of L-DOPA in sensorimotor tests.Chronic CPL500036 treatment did not decrease L-DOPA-induced contralateral rotation.

G-Glu-Val, also known as gamma-Glutamyl-L-valine or H-gGlu-Val-OH, is a taste-modulating dipeptide and a main contributor to the "kokumi" taste of edible beans.

DS-6051b is a potent and selective ROS1 and TRK family inhibitor with IC50 of 0.207 nM, 0.622 nM and 0.980 nM against ROS1, NTRK1 and NTRK3. DS-6051b especially inhibits ROS1 G2032R and other crizotinib-resistant ROS1 mutants.

BBO-11818 is an orally active, highly selective (relative to NRAS and HRAS), non-covalent pan-KRAS inhibitor (IC50=28-120 nM). BBO-11818 specifically binds to the Switch-II/Helix 3 pocket, disrupts the KRAS:RAF1 interaction by inducing conformational changes, and blocks the MAPK signaling pathway. BBO-11818 exhibits significant anti-tumor activity, which not only inhibits cell proliferation and induces apoptosis, but also drives tumor regression in xenograft models. BBO-11818 produces synergistic effects when combined with Cetuximab, anti-PD-1 antibody or PI3Kα inhibitor. BBO-11818 is used in the research of KRAS mutation-related malignancies such as pancreatic cancer, non-small cell lung cancer and colorectal cancer.