CymitQuimica ha oltre 25 partner, tra i quali spicca il fornitore TargetMol

SRI-31255 is an orally active LRRK2 inhibitor, with IC50 values of 520 nM for human wild-type (WT) and 427 nM for the G2019S mutant. It inhibits kinase activity by binding to the ATP-binding pocket of LRRK2, providing neuroprotective effects. SRI-31255 serves as a lead compound for developing LRRK2-targeted therapies for Parkinson’s disease research.

MS105 is an orally active, selective protein tyrosine kinase 6 (PTK6) PROTAC degrader. It recruits the VHL E3 ligase through a VHL ligand fragment, facilitating ubiquitination and proteasomal degradation of PTK6, thereby inhibiting the proliferation and migration of breast cancer cells and inducing apoptosis (apoptosis). MS105 is a promising compound for breast cancer research.

<p>EGFR/DHFR-IN-2 (9b) is a dual inhibitor of h-DHFR/EGFR TK, exhibiting IC50 values of 0.192 μM for h-DHFR and 0.109 μM for EGFR. It causes cell cycle arrest at the G1/S phase and induces apoptosis. Additionally, EGFR/DHFR-IN-2 (9b) is a potential inhibitor of CYP2C9 and CYP3A4. This compound can be utilized in cancer research.</p>

<p>Pyrithioxin dihydrochloride (Pyrithioxine HCl) has anti-nociceptive and anti-allodynic effects and can be used to study neurological diseases.</p>

CW-2 is a PARP1 PROTAC degrader known for its potent antiproliferative effects against MDA-MB-231 cells (IC50 = 0.72 μM) and cisplatin-resistant cells (A549/CDDP: IC50 = 3.52 μM). It exhibits synergistic antitumor activity and enhanced membrane permeability. CW-2 exerts its antitumor effects by inducing DNA damage, disrupting DNA repair, and triggering mitochondrial-dependent apoptosis (apoptosis).

<p>CHK1-IN-11 (Compound 1) is an orally active inhibitor of checkpoint kinase 1 (CHK1). It is utilized in research focused on cancers with oncogene amplification.</p>

Cryptating agent 222 reduces distannene & creates ligands with metal ions using a potassium mirror.

<p>RP03707 is a PROTAC degrader of KRASG12D.</p>

Dopamine D4 receptor ligand 3 (Compound 16) functions as a dopamine D4 receptor (D4R) antagonist with a pKi of 8.86. In HEK-293T cells, it shows pIC50 values of 5.78, 5.55, and 6.17 for Go, Gi, and βArr2 sensors, respectively. This compound inhibits the activity of human glioma cell lines U87 MG, T98G, and U251 MG, and it induces ROS production and mitochondrial dysfunction in these glioma cells.

<p>Panipenem is a carbapenem antibiotic used in combination with betamipron.</p>

<p>Androstatrione is an androgenic compound.</p>

<p>TEAD-IN-20 is a TEAD inhibitor with IC50 values of 0.021 μM in TEAD4 FRET and 0.044 μM in TEAD4 MCF7-Tead cell lines. It has potential applications in cancer research.</p>

<p>Anti-infective agent 10 (Compound Example 30) is an ns5b polymerase inhibitor that functions as an anti-HCV agent.</p>

<p>STINGagonist-42 (compound 8a) is a potent STING agonist. It activates STING in THP1 and RAW 264.7 cells, with EC50 values of 0.06 μM and 14.15 μM, respectively.</p>

<p>SP11 is a mitochondrial reactive oxygen species (ROS) inhibitor. It activates Fis1 with an IC50 of 9.4 µM by binding to Cys41 and enhances the translocation of Drp1 to mitochondria. SP11 is utilized for research into oxidative stress damage.</p>

<p>Chlormequat chloride (EI 38,555), a plant growth regulator, is widely applied in agriculture because it can promote sturdier growth of the crops.</p>

MRL828 is a compound that combines a Tau pathology-binding ligand with a guanine group modified by ATTEC technology, allowing it to selectively target aggregated tau proteins for clearance via the autophagy-lysosome pathway (ALP). MRL828 reduces intracellular Tau aggregates and facilitates the secretion of Tau.

AR ligand 40 (compound 19c) is an Adenosine A1 Receptor ligand with antagonistic activity. It exhibits antiproliferative effects on SW480, SW48, HCT116, K562, MDA-MB-231, and A549 cells, with EC50 values of 7, 10, 12, 13, 15, and 39 μM, respectively.

BBOX-IN-1 (compound 58) is a potent BBOX inhibitor with an IC50 of 0.02 μM, and it is applicable in research related to triple-negative breast cancer (TNBC).

TPS1-IN-1 (Compound O1) is a potent and broad-spectrum inhibitor of TPS1. It exhibits IC50 values of 14.73 μM for MoTPS1 (Magnaporthe oryzae TPS1) and 59.99 μM for BcTPS1 (Botrytis cinerea TPS1). TPS1-IN-1 exerts its broad-spectrum fungicidal effects by disrupting spore germination, appressorium formation, and turgor pressure accumulation in fungi. With good safety profiles, TPS1-IN-1 has potential as a candidate for novel fungicide development.