MSU 38225 (MSU-38225) is a novel small molecule that inhibit the Nrf2 pathway, potentially inhibiting Nrf2 transcriptional activity and cancer cell growth; MSU38225 downregulates Nrf2 transcriptional activity and decreases the expression of Nrf2 downstream targets, including NQO1, GCLC, GCLM, AKR1C2, and UGT1A6. MSU38225 strikingly decreases the protein level of Nrf2, which can be blocked by the proteasome inhibitor MG132. Ubiquitination of Nrf2 is enhanced following treatment with MSU38225. By inhibiting production of antioxidants, MSU38225 increases the level of reactive oxygen species (ROS) when cells are stimulated with tert-butyl hydroperoxide (tBHP). MSU38225 also inhibits the growth of human lung cancer cells in both two-dimensional cell culture and soft agar.

N-Desmethyl Pimavanserin (AC-279) is the active metabolite of Pimavanserin. Pimavanserin is a selective inverse agonist of the 5-HT2A receptor with pIC50 and pKd of 8.73 and 9.3, respectively.

AZD4747 is a highly potent and selective inhibitor of KRASG12C with IC50 of 15 nM. AZD4747 also shows an anticipated low clearance and high oral bioavailability profile in humans.

PDS-0330 is a specific and potent Claudin-1 inhibitor. PDS-0330 interferes with claudin-1/Src association and inhibits colorectal cancer (CRC) progression and metastasis.

CWI1-2 hydrochloride is an inhibitor of IGF2BP2 that binds IGF2BP2 and inhibits its interaction with m6A-modified target transcripts, induces apoptosis and differentiation, and shows promising anti-leukemic effects.

CWI1-2 is an IGF2BP2 inhibitor that binds IGF2BP2 and inhibits its interaction with m6A-modified target transcripts, induces apoptosis and differentiation, and shows promising anti-leukemic effects.

T-518 (T518) is a potent, highly selective, brain penetrant, oral HDAC6 inhibitor with IC50 of 36 nM.T-518 did not obviously inhibit human HDAC1, 4, or 7 at 10 uM, which belongs to Class I or Class IIa HDAC.T-518 showed brain penetration in an oral dose and blocked HDAC6-dependent tubulin deacetylation at Lys40 in mouse hippocampus.T-518 decreased RIPA-insoluble tau accumulation (3-month treatment, 1 and 3 mg/kg), restored impaired axonal transport and novel object recognition in the P301S tau Tg mouse (tauopathy model) by 2-week treatment with dose 1 and 3 mg/kg.

dTRIM24 is a potent TRIM24 bromodomain inhibitor with IC50 of 217.8 nM (TRIM24 ligand displacement).

SG094 is a potent TPC2 inhibitor with antiproliferative effects. SG-094 can be used for the research of cancer.

NH-23-C2 (Caspase-2 inhibitor NH-23-C2) is a potent, selective and cell-permeable endogenous caspase-2 inhibitor, does not block caspase-3 or caspase-8.NH-23-C2 displays off-reactivity with cysteine and threonine proteases (cathepsins B, L, V, S).HCT116 cells were preincubated with NH-23-C2 inhibitor, MDM-2 cleavage was inhibited in a concentration-dependent manner (IC50 =3.11 μM).NH-23-C2 selectively block caspase-2 activity and caspase-2-mediated MDM-2 cleavage.

SC-1 (1-(4-Chloro-3-(trifluoromethyl)phenyl)-3-(4-(4-cyanophenoxy)phenyl)urea, STAT3-IN-7), a Sorafenib analogue and potently inhibits the phosphorylation of STAT3, induces cell apoptosis through SHP-1 dependent STAT3 inactivation.

KT-531 (KT531) is a potent, selective HDAC6 inhibitor with IC50 of 8.5 nM, displays 39-fold selectivity.

Chitosan oligosaccharide (COS) is an oligomer of β-(1→4)-linked D-glucosamine. Chitosan oligosaccharide (COS) activates AMPK and inhibits inflammatory signaling pathways including NF-κB and MAPK pathways.

(-)-Isoproterenol hydrochloride is an agonist of beta-adrenergic receptor. (-)-Isoproterenol hydrochloride is also used in the treatment of bradycardia; bronchodilator.

MS934 (MS-934) is a VHL-recruiting MEK1/2 degrader (PROTAC) with HT29 DC50 of 18/9 nM for MEK1/2 degradation, respectively.MS934 is more potent at inhibiting the growth of HT-29, SK-MEL-28, H3122, and SUDHL1 cells. MS934 also displays good plasma exposure in mice.

ARV-766 is an orally active and potent proteolysis targeting chimera (PROTAC) protein degrader. ARV-766 degrades wild-type androgen receptor (AR) but also relevant AR LBD mutants, including the most prevalent AR L702H, H875Y, and T878A mutations[1].

FX-909（FX 909） is a first-in-class inverse agonist of the peroxisome proliferator-activated receptor gamma (PPARG) lineage transcription factor with EC50 of 1 nM and shows >2000-fold selectivity for PPARG over PPARA/PPARD - acting through a mechanism that promotes a repressive conformation of PPARG.

PTC258 is a specific and orally active splicing modulator of Elongator complex protein 1 gene (ELP1). PTC258 increases the expression of ELP1 in vitro and in vivo. PTC258 is well tolerated in mouse model.

JNT-517 is a small-molecule inhibitor of the phenylalanine transporter SLC6A19 that has the potential to be a first-in-class oral therapy used to treat any person with PKU, regardless of age or genotype. JNT-517 acts at a novel, cryptic allosteric site to block kidney reabsorption of Phe and offers a promising new approach to reduce blood Phe levels. The FDA has granted JNT-517 Rare Pediatric Disease Designation.

CHK-336 (Example 1) is an orally active LDHA inhibitor (IC50<1 nM) that inhibits lactate production in mouse hepatocytes. CHK-336 can be used in the study of hyperoxaluria.

Activity of KIN-3248, a next-generation pan-FGFR inhibitor, against acquired FGFR-gatekeeper and molecular-brake drug resistance mutations

Piperazine Erastin is an analog of Erastin, which can induces ferroptosis in cancer cells, an iron-dependent form of nonapoptotic cell death..

Telotristat ethyl (LX1606) is a novel, orally-delivered inhibitor of tryptophan hydroxylase that reduces serotonin production.

Enasidenib (Idhifa, AG-221) mesylate is an orally available, selective and potent inhibitor of mutant isocitrate dehydrogenase 2 (IDH2).

TTC352 is a synthetic selective estrogen mimic acts as estrogen receptor (ER) partial agonist for the treatment of endocrine-resistant breast cancer.TTC 352 yields an H-bond with Glu353, allows Asp351-to-helix 12 (H12) interaction, sealing ERα's ligand-binding domain, recruiting E2-enriched coactivators, and triggering rapid ERα-induced unfolded protein response (UPR) and apoptosis.TTC-352 is a less potent full estrogen agonist compared to E2, allowing H12 to seal the LBD, which recruits many E2-enriched coactivators, and induces rapid ERα-mediated UPR and apoptosis.

Parbendazole is an anthelmintic drug. Parbendazole is a potent inhibitor of microtubule assembly, destabilizes tubulin and exhibits a broad-spectrum anthelmintic activity.

MS049 is a potent and selective inhibitor of PRMT4 and PRMT6 that is active in cells.

Abrucomstat (3-Nitroxypropanol) acts as an enzyme inhibitor to decrease ruminal methanogenesis.

icFSP1 is a compound class of 3-phenylquinazolinones. icFSP1, unlike iFSP1, is the first described on-target FSP1 inhibitor, does not competitively inhibit FSP1 enzyme activity, but instead triggers subcellular relocalization of FSP1 from the membrane and FSP1 condensation before ferroptosis induction, in synergism with GPX4 inhibition.

Antitumor agent-113 shows cytotoxic effects on A549 cells.