Vigabatrin (γ-Vinyl-GABA) is an orally active, irreversible inhibitor of GABA transaminase, increasing brain GABA levels by blocking its breakdown. It is an antiepileptic drug that enhances inhibitory neurotransmission to control seizures and exhibits potential in treating partial seizures, infantile spasms, and Lennox-Gastaut syndrome.

Zotatifin (eFT226) is a highly effective and sequence-selective inhibitor of the RNA helicase eIF4A. It promotes eIF4A binding to specific mRNA sequences with recognition motifs in the 5′-UTRs, with an IC50 of 2 nM, and disrupts the assembly of the eIF4F initiation complex. By enhancing the interaction between eIF4A and polypurine RNA sequence or structural […]

Giredestrant (GDC-9545; RG6171) is an efficient and potent selective estrogen receptor degrader and a full antagonist with an IC50 of 0.05 nM in T-47D wild-type cells. It also exhibits anti-proliferative activity.

“SD-36 is a potent, selective and efficacious PROTAC degrader of STAT3 protein with Kd of ~50 nM. It also effectively degrades mutated STAT3 proteins in cells and suppresses the transcriptional activity of STAT3 with IC50 of 10 nM. It also exerts anti-tumor activity. SD-36 is a potent, selective and efficacious PROTAC degrader of STAT3 protein […]

Milademetan(RAIN-32, DS-3032) is an oral, selective inhibitor of the MDM2-p53 complex that reactivates p53 to induce cancer cell apoptosis and exhibits an anti-tumor effect.

Methyl-piperidino-pyrazole (MPP) dihydrochloride is a highly selective antagonist for estrogen receptor alpha (ERα), with an affinity 200 times greater than for estrogen receptor beta (ERβ). It inhibits 17β-estradiol binding to ERα by inducing conformational changes that alter the receptor’s binding site and also increases the energy required for genistein’s interaction with ERα.