T2024

A-803467 is a selective NaV1.8 channel blocker.

MS40 is a WDR5 PROTAC that selectively degrades WDR5 and serves as a novel degrader for immune-modulating compounds (IMiDs), including the new substrates CRBN and Ikaros zinc finger (IKZF) transcription factors IKZF1 and IKZF3. MS40 facilitates the degradation of WDR5, resulting in the dissociation of the MLL/KMT2A complex from chromatin, thereby reducing H3K4me2 levels. In vitro, MS40 inhibits the growth of primary leukemia patient cells, and in vivo, it suppresses the expansion of patient-derived xenografts.

SK-124 is an inhibitor of SIK (salt-inducible kinase).

Simufilamum (also known as PTI-125) is an oral small-molecule compound candidate that targets altered conformations of filamin A. It binds and reverts the misfolded filamin A in the brains of Alzheimer's disease patients, thereby slowing the disease's pathological progression. Additionally, PTI-125 reduces tau protein hyperphosphorylation, decreases Aβ42 aggregation and deposition, neurofibrillary tangles, and neuroinflammation. The compound demonstrates concentration-dependent efficacy in vitro, starting at 1 picomolar (pM), in both control groups and post-mortem hippocampal slices from Alzheimer's disease (AD) patients. PTI-125 is the first therapeutic candidate to preferentially bind and reverse pathogenic protein conformations.

Pam2Cys is an L-cysteine thioether where the hydrogen of the thiol group is replaced by a 2,3-di(palmitoyloxy)propyl group. It acts as a Toll-like receptor 2 agonist and a metabolite of Mycoplasma genitalium. Additionally, Pam2Cys is associated with the function of palmitoleic acid.

MRS4608 is a novel and potent antagonist of the P2Y14 receptor.

MRS4654 is an innovative and potent antagonist of the P2Y14 receptor, featuring an IC50 of 15 nM.

Pt(II) Octaethylporphine ketone, a synthetic porphyrin compound, is frequently employed as a phosphorescent oxygen probe for assessing respiration in microbial systems.

MK8457 is a dual inhibitor targeting both SYK and ZAP70.

MK-6325 is a potent inhibitor of the HCV NS3/4A protease.

MS-8709 is a potent and selective G9a/GLP PROTAC Degrader with a DC50(G9a) of 274 nM and a DC50(GLP) of 260 nM. It induces G9a/GLP protein degradation in a concentration-dependent and time-dependent manner via the ubiquitin-proteasome system, without affecting mRNA expression levels. MS-8709 demonstrates superior cell growth inhibition compared to the parent compound UNC0642 in prostate cancer, leukemia, and lung cancer cell models, and exhibits mouse pharmacokinetic characteristics suitable for in vivo efficacy studies.

PD 4'-piperazine is a cereblon ligand that can be utilized for developing PROTAC degraders.