Novel specific Rac1 inhibitor, interferring with the interaction of Rac1 with Dock180, a relevant Rac1 activator in glioma invasion, and to reduce Rac1-GTP levels

GLN-1062 (Memogain) is an inactive pro-drug of galantamine, the latter being a plant alkaloid approved for the treatment of mild to moderate Alzheimer's disease.

Oncrasin 1 is a proapoptotic substance. Induces abnormal nuclear aggregation of PKCι and suppressing RNA transcription.

WAY-296817 is casein kinase 1 (CK1) inhibitor and can be used for research on the treatment or prevention.

Biotin-aniline is a probe with substantially high reactivity towards RNA and DNA. Biotin-aniline emerges as more efficient probe for capturing subcellular transcriptome in living cells with high spatial specificity.

Tecastemizole (Norastemizole), a major metabolite of Astemizole, is a potent and selective H1 receptor antagonist. Tecastemizole shows anti-inflammatory activities.

Z-944 is a potent, highly selective and oral T-type calcium channel blocker with IC50 of 50-160 nM for human Cav3.1, Cav3.2, and Cav3.3 channels.

(R)-69 is a 5-HT2AR partial agonists with EC50 of 41 nM, and shows 4.6-fold/29-fold selectivity over 5HT2BR/5HT2CR. (R)-69 has substantial brain permeability in mouse pharmacokinetic studies and dose not possess locomotor-stimulating or reinforcing activity.

(R)-70 is a 5-HT2AR partial agonists with EC50 of 110 nM, and shows 6.4-fold/51-fold selectivity over 5HT2BR/5HT2CR. (R)-70 has substantial brain permeability in mouse pharmacokinetic studies and dose not possess locomotor-stimulating or reinforcing activity.

Val-Cit-PAB-MMAF sodium is a drug-linker conjugate for ADC. Val-Cit-PAB-MMAF sodium contains the ADCs linker (peptide Val-Cit-PAB) and a potent tubulin polymerization inhibitor MMAF.

Ivermectin B1a, a derivative of Avermectin B1a, is a main component of Ivermectin. Ivermectin (MK-933) is a broad-spectrum anti-parasite agent. Ivermectin is a candidate therapeutic against SARS-CoV-2/COVID-19.

MAK683-CH2CH2COOH binds to EED (embryonic ectoderm development protein). MAK683-CH2CH2COOH and a VHL ligand for the E3 ubiquitin ligase have been used to design PROTAC EED degrader-1 and PROTAC EED degrader-2.

KB02-COOH is a fragment of synthesis of ubiquitin E3 ligase ligand KB02. KB02 can be used in the synthesis of PROTAC, such as KB02-JQ1 and KB02-SLF.

GD20 is a cell-permeable, nucleotide-inactive-state-selective inhibitor of Gαs, with high selectivity over other G protein subfamilies. GD20 inhibits Gαs steady-state GTPase activity with IC50 of 1.15 μM.

Carbamic acid, N-[2,4-dimethyl-6-(4-morpholinyl)-3-pyridinyl]-, phenylmethyl ester is a new invention for treating, one or more disorders or conditions wherein the dopaminergic system is disrupted, such as one or more disorders or conditions independently selected from the group consisting of: schizophrenia and other psychotic states; mood disorders ADHD; aggression; movement disorders.

Bucolome is a CYP2C9 inhibitor, used as an uricosuric agent or anti-inflammatory agent.

CCG-203769 is a selective G protein signaling (RGS4) inhibitor, which blocks the RGS4-Gαo protein-protein interaction in vitro with an IC50 of 17 nM.

APOL1-IN-1 is a apolipoprotein L1 (APOL1) inhibitor extracted from patent WO2020131807A1 compound 87. APOL1-IN-1 can be used for the research of focal segmental glomerulosclerosis (FSGS) and non-diabetic kidney disease (NDKD)[1].

CDC801 is a potent and orally active phosphodiesterase 4 (PDE4) and tumor necrosis factor-α (TNF-α) inhibitor with IC50 of 1.1 μM and 2.5 μM, respectively.

CARM1-IN-7g is a potent, selective coactivator-associated arginine methyltransferase 1 (CARM1) with IC50 of 8.6 uM, exhibits lower or no activity against a panel of different PRMTs or HKMTs (>80-fold over PRMT1 and SET7).

A novel potent and selective TGF-βRI (ALK5) inhibitor with IC50 of 4.83 nM, dispalys >300-fold selectivity over p38α.

A potent Nrf2 activator that upregulates Nrf2 expression and resulted in translocation of Nrf2 into the nucleus..

ARD2128 is a highly potent, orally bioavailable PROTAC androgen receptor (AR) degrader. ARD-2128 effectively reduces AR protein, suppresses AR-regulated genes in tumor tissues, and inhibits growth of tumor without signs of toxicity. ARD-2128 has the potential for the research of the prostate cancer.

AZD0284 is an inverse agonist of the nuclear receptor RORγ. In development for the treatment of plaque psoriasis vulgaris and respiratory tract disorders.

Philanthotoxin 74 dihydrochloride (PhTx 74) is an AMPAR antagonist; inhibits GluR3 and GluR1 with IC50s of 263 and 296 nM, respectively.

MCB-613 is a novel and potent stimulator of p160 steroid receptor coactivators (SRCs). It is a Pan-SRCs stimulator.

The first in a class, potent and highly selective, direct renin inhibitor with IC50 of 0.6 nM.

Sivopixant (S-600918) is a potent and selective P2X3 receptor antagonist (P2X3 IC50=4.2 nM; P2X2/3 IC50=1100 nM). Sivopixant shows strong analgesic effect.