AZ-194 is a first-in-class, orally active inhibitor of CRMP2-Ubc9 interaction and inhibitor of NaV1.7 (IC50=1.2 μM). AZ194 blocks SUMOylation of CRMP2 to selectively reduce the amount of surface-expressed NaV1.7. Antinociceptive effects[1].

AGB1 is a fast, highly selective, and potent bump-and-hole (B&H)-PROTAC degrader for BromoTag. AGB1 exhibits degradation for Ab:Brd4BD2 L387A and Ab: BromoTag-Brd2 with pDC50s of 7.8 and 7.9. AGB1 exhibits binary affinity to VHL (Kd=125 nM). AGB1 exhibits favorable pharmacokinetic profile in mice with the DC50, 6 h of ∼13 nM.

Felezonexor, also known as CBS9106, SL-801, and BMS566419, is a novel reversible oral CRM1 inhibitor with CRM1 degrading activity. CRM1 plays an important role in the nuclear export of cargo proteins bearing nuclear exporting signal sequences. CBS9106 inhibits CRM1-dependent nuclear export, causing arrest of the cell cycle and inducing apoptosis in a time- and dose-dependent manner for a broad spectrum of cancer cells, including multiple myeloma cells. CBS9106 reduces CRM1 protein levels significantly without affecting CRM1 mRNA expression. Oral administration of CBS9106 significantly suppresses tumor growth and prolongs survival in mice bearing tumor xenograft without a significant loss in body weight.

AHR-10037 is a non-steroidal anti-inflammatory agent with low gastric toxicity. AHR-10037 is a prodrug converted in vivo to a cyclooxygenase inhibitor.

TP-1287, a prodrug of Alvocidib, is an orally active CDK9 inhibitor.

ML 2-23 is a potent PROTAC BCR-ABL degrader. ML 2-23 is selectively degrade BCR-ABL in a proteasome-dependent manner in leukemia cells.

Ethyl methanesulfonate is a DNA ethylating agent, mutagenic to plants and animals and carcinogenic in mammals. It has been used as a model alkylating agent in studies of DNA repair processes. It induces base substitutions of guanine-cytosine (G/C) to adenine-thymine (A/T). EMS also generates point mutations and single nucleotide polymorphisms in genomes.

GBT1118 is a potent and orally active allosteric modifier of hemoglobin oxygen affinity. GBT1118 increases tolerance to severe hypoxia.

MEN 11270, a cyclic decapeptide, is a B2 kinin receptor antagonist. MEN 11270 bound with high-affinity to the B2 kinin receptor constitutively expressed by WI38 human fibroblasts, inhibiting 3H-bradykinin (BK) with pKi of 10.3.

B746 is a clofazimine analog with anti-Mycobacterium avium complex (MAC) activity and is less effective when used with clofazimine or streptomycin.

A potent, specific inhibitor of HCV NS5B polymerase and HCV replication (IC50=1.28 uM, replicon assay).

BAY 73-6691 is a drug developed by Bayer for the treatment of Alzheimer's disease. It was the first compound developed that acts as a phosphodiesterase inhibitor selective for the PDE9A subtype.

Hydrazinocurcumin is a synthetic curcumin derivative that inhibits the proliferation of bovine aortic endothelial cells (BAECs) with IC50 of 520 nM without cytotoxicity, inhibits STAT3 phosphorylation and downregulates an array of STAT3 downstream targets.

Atrovastatin-PEG3-FITC (compound S31) is a KRAS-PDEδ interaction inhibitor. Atrovastatin-PEG3-FITC acts as a ligand in fluorescence anisotropy assay.

TUG-499 is a selective free fatty acid receptor 1 (FFAR1 or GPR40) (Free Fatty Acid Receptor) agonist with a pEC50 of 7.39. TUG-499 exhibits >100-fold selectivity over the related receptors FFA2, FFA3, and the nuclear receptor PPARγ and other diverse receptors, ion channels, and transporters. TUG-499 can be used for the research of type 2 diabetes.

A highly potent agonist of σ1 receptor with Ki of 0.8 nM.

Melagatran is a synthetic, small-peptide direct thrombin inhibitor with anticoagulant activity.

JNJ-40411813 is a novel potent positive allosteric modulator of mGlu2 with EC50 of 147 nM. JNJ-40411813 displays >30-fold selectivity over mGlu1 and mGlu3-8, 10-fold over 5-HT2A. JNJ-40411813 displays an optimal interplay between potency, selectivity, favorable ADMET/PK and cardiovascular safety profile, and central EEG activity; has been investigated in the clinic for schizophrenia and anxious depression disorders.

Belzutifan (PT2977, MK-6482) is a potent and selective small-molecule inhibitor of HIF2α with SPA IC50 of 9 nM, EC50 of 11 nM (HIF-2α luciferase assay). PT2977 demonstrated high potency with EC50 of 17 nM in the VEGFA secretion assay in 786-O cells. PT2977 (0.3, 1, and 3 mg/kg, oral) potently and dose-dependently reduced mRNA levels of human cyclin D1, a target gene regulated by HIF-2α, exhibited excellent antitumor activity in the 786-O mouse xenograft model In phase 1 clinical, PT2977 decreased in the HIF-2α target erythropoietin (EPO) following once daily oral administration of PT2977 at the dose levels of 20, 40, 80, 120, 160, and 240 mg in patients with solid tumors, also showed encouraging outcomes in patients with advanced renal cell carcinoma in an expansion cohort of 55 patients with ccRCC treated at 120 mg q.d.

ML213 is a novel potent, selective KCNQ2 (Kv7.2) and KCNQ4 (Kv7.4) activator with EC50 of 230 and 510 nM, respectively. ML213 displays >80-fold selectivity over other related potassium channels (KCNQ1/3/5). ML213 causes significant hyperpolarization in mesenteric artery smooth muscle cells, shows potent vasorelaxant effects in different blood vessels.

Hi 76-0079 (NNC0076-0079) is a specfic, small molecule inhibitor of hormone-sensitive lipase (HSL) with IC50 of 0.11 uM. Hi 76-0079 does not affect ATGL or other lipases (IC50>50 uM). Hi 76-0079 inhibits lipolysis in vivo.

Enpatoran (M5049) hydrochloride is a potent, orally active, and dual TLR7/8 inhibitor with IC50s of 11.1 nM and 24.1 nM, respectively, in HEK293 cells.

1-Thioglycerol(Mercaptopropanedioltech) is an inhibitor of glycerol kinase activity. It stimulates the synthesis of porphyrin in aerobically growing Escherichia coli.

3,4-Dichlorophenyl isocyanate(1,2-Dichloro-4-isothiocyanatobenzene) is a chemical compound used as a chemical intermediate and in organic synthesis.

Glutaraldehyde(Glutaric dialdehyde, Pentane-1,5-dial) is an effective biochemical reagent used as a protein crosslinker, enzyme immobilization microscopy, histochemistry, and cytochemistry.

BW 755C is a 5-lipoxygenase (5-LO) inhibitor with an IC50 of 5 μM. BW 755C also inhibits cyclooxygenase (COX) with IC50s of 0.65 and 1.2 μg/mL against COX-1 and COX-2, respectively.

Vidofludimus (4sc-101; SC12267) hemicalcium is an orally active inhibitor for dihydroorotate dehydrogenase (DHODH) and also is a novel modulator for farnesoid X receptor (FXR). Vidofludimus hemicalcium, as an immunomodulatory agent, can be used for the research of autoimmune disorders such as inflammatory bowel disease (IBD). Vidofludimus hemicalcium also can be used for the research of fatty liver by targeting FXR.

BMS-433771 dihydrochloride hydrate is a potent orally active inhibitor of respiratory syncytial virus (RSV). BMS-433771 dihydrochloride hydrate is active against both A and B groups of RSV, with an average EC50 of 20 nM. BMS-433771 dihydrochloride hydrate can be used for the research of respiratory tract disease.

Varlitinib (ASLAN001) tosylate is a potent, reversible, small molecule pan-EGFR inhibitor with IC50s of 7, 2, 4 nM for HER1, HER2 and HER4, respectively.

FR 113680 is a tripeptide substance P antagonist that interacts selectively with the NK1 neurokinin receptor.