DTHIB is a direct and selective heat shock factor 1 (HSF1) inhibitor with a Kd of 160 nM for DTHIB binding to the HSF1 DNA binding domain (DBD). DTHIB inhibits HSF1 cancer gene signature (HSF1 CaSig) and selectively stimulates degradation of nuclear HSF1. DTHIB has potently anticancer activities and can be used for prostate cancer research.

OSI-420 (Desmethyl Erlotinib,CP-473420) is an active metabolite of erlotinib which is an orally active EGFR tyrosin kinase inhibitor with IC50 of 2 and 20 nM for human EGFR and EGFR autophosphorylation in tumor cells.

Parsaclisib hydrochloride (INCB050465 hydrochloride) is a potent, selective and orally active inhibitor of PI3Kδ, with an IC50 of 1 nM at 1 mM ATP. Parsaclisib hydrochloride shows approximately 20000-fold selectivity over other PI3K class I isoforms. Parsaclisib hydrochloride can be used for the research of relapsed or refractory B-cell malignancies.

A small molecule inhibitor of clathrin terminal domain and inhibits clathrin-mediated endocytosis.

Seralutinib (GB002) is an inhaled Pdgfr kinase inhibitor. Seralutinib (GB002) is used in the study for pulmonary arterial hypertension.

SJ-172550 is the first MDMX inhibitor with EC50 of 0.84 uM; binds reversibly to MDMX and effectively kills retinoblastoma cells in which the expression of MDMX is amplified.

QLT0267 is an ATP-competitive selective inhibitor of integrin-linked kinase (ILK).

CTP354, also known as C-21191, a novel deuterated subtype-selective GABA(A) modulator. CTP may be potentially useful for treatment of neuropathic pain, spasticity and anxiety disorders. GABAA receptors are found in the nervous system and, when activated, reduce the transmission of certain nerve signals. Several classes of widely used drugs target GABAA receptors, including benzodiazepines, but do not have the receptor subtype selectivity of CTP-354.

Mc-VC-PAB-SN38 consists a cleavable ADC linker (Mc-VC-PAB) and a DNA topoisomerase I inhibitor (SN38). Mc-VC-PAB-SN38 can be used in the synthesis of antibody-drug conjugates (ADCs).

NL3 is a select bacterial cystathionine γ-lyase (bCSE) inhibitor with IC50 of 0.7 μM (3.4 μM against hCSE). NL3 potentiates bactericidal antibiotics against pathogens.

NL2 is a select bacterial cystathionine γ-lyase (bCSE) inhibitor with IC50 of 1.8 μM (25.3 μM against hCSE). NL2 potentiates bactericidal antibiotics against pathogens.

NL1 is a select bacterial cystathionine γ-lyase (bCSE) inhibitor with IC50 of 5.8 μM (29.2 μM against hCSE). NL1 potentiates bactericidal antibiotics against pathogens.

CRBN modulator-1, a Thalidomide analog and a CRBN modulator extracted from WO2020006262A1, compound 10, has an IC50 of 3.5 μM and a Ki of 0.98 μM.

Trandolaprilat is a non-sulfhydryl angiotensin-converting enzyme inhibitor.

Jun8-76-3A is a potent and selective noncovalent SARS-CoV-2 Mpro inhibitor with Ki of 0.07 μM. Jun8-76-3A only selectively inhibits SARS-CoV-2 and SARS-CoV Mpro, but not other viral proteases and host proteases including calpain 1, cathepsins L and K, and trypsin.

Dac51 is a potent FTO inhibitor with IC50 of 0.4 μM, which blocks FTO-mediated immune evasion and synergize with checkpoint blockade for better tumor control.

ATI-2173 is a novel liver-targeted molecule designed to deliver the 5′-monophosphate of clevudine for the treatment of chronic hepatitis B infection.

PD-1/PD-L1-IN 3, a macrocyclic peptide, is a potent and selective inhibitor of the PD-1/PD-L1 and CD80/PD-L1 interactions extracted from patent WO2014151634A1, compound No.1. PD-1/PD-L1-IN 3 interferes with PD-L1 binding to PD-1 and CD80 by binding to PD-L1, with IC50s of 5.60 nM and 7.04 nM, respectively. PD-1/PD-L1-IN 3 can be used for the research of various diseases, including cancer and infectious diseases.

BAR501 impurity is an impurity found in the preparation of BAR501 that acts as an agonist of the G protein-coupled bile acid-activated receptor (GP-BAR1). BAR501 impurity (10 µM) induces a 150% increase in luciferase activity in a GP-BAR1 reporter gene assay.

AST5902 is the active metabolite of Alflutinib.

IXA6 is a novel small molecule compound of inducing IRE1 RNase activity.

BMS-986313 is a tricyclic-carbocyclic RORγt inverse agonist and shows potent GaL4-Luc reporter(GAL4) and human whole blood (hWB) activity (EC50s of 3.6 nM and 50 nM, respectively.

Sisunatovir (RV521), an orally available inhibitor of the RSV fusion (RSV-F) protein, exhibits potent efficacy against a panel of clinical isolates of RSV-A and RSV-B viruses, with IC50s of 1.4 nM and 1.0 nM, respectively.

TAOK inhibitor 43 is a novel potent, selective, ATP-competitive TAO Kinase (TAOK) inhibitor with IC50 of 11 and 15 nM against TAOK1 and TAOK2, respectively; increases the mitotic population, the percentages of mitotic cells displaying amplified centrosomes and multipolar spindles, induces cell death, and inhibits cell growth in centrosome-amplified SKBR3 or BT549 breast cancer cell models.

Acivicin is a glutamine analog that irreversibly inhibits glutamine-dependent amidotransferases involved in nucleotide and amino acid biosynthesis (Kis = 10 and 560 μM for anthranilate synthase and glutamate synthase, respectively).

A 1,2,5-thiadiazolidin-3-one-1,1-dioxide scaffold for design of protein tyrosine phosphatase-1B (PTP1B) inhibitor.

E3 ligase Ligand 4 is a ligand of E3 ligase, used in PROTAC technology.

LC-2 is a potent and first-in-class degrader of endogenous KRAS G12C with DC50 values between 0.25 and 0.76 μM. LC-2 covalently binds KRAS G12C with a MRTX849 warhead and recruits the E3 ligase VHL, inducing rapid and sustained KRAS G12C degradation leading to suppression of MAPK signaling in both homozygous and heterozygous KRAS G12C cell lines.

CS-3150 (Esaxerenone, XL-550) is a highly potent, selective and orally active non-steroidal mineralocorticoid receptor antagonist with IC50 of 9.4 nM; displays >1,000-fold selectivity over other steroid hormone receptors, glucocorticoid receptor, androgen receptor and progesterone receptor; inhibits aldosterone-induced transcriptional activation of human mineralocorticoid receptor with IC50 of 3.7 nM, shows superior potency to that of spironolactone and eplerenone; suppresses aldosterone-induced decrease in urinary Na(+)/K(+) ratio, inhibits blood pressure elevation induced by DOCA/salt-loading in rats.

Selective blocker of the Aquaporin-1 ion channel conductance, slowing cancer cell migration