NOTA-P2-RM26 is a high-affinity NOTA-conjugated bombesin antagonist for GRPR-targeted tumor imaging

NOTA-E(cRGDfK)2 is a ligand to making 68Ga-DOTA-E[c(RGDfK)]2, which is a PET Imaging agent of SHARPIN-Regulated Integrin Activity. E[c(RGDfk)]2 = glutamic acid-[cyclo(arginyl-glycyl-aspartic acid-D-phenylalanine-lysine).

Caspase-1 Inhibitor IV controls the biological activity of Caspase-1. This small molecule/inhibitor is primarily used for Cancer applications.

DOTA-c(RGDyK) is useful ligand for making 225Ac-DOTA-c(RGDyK), which is a potential radiopharmaceutical for targeted alpha particle therapy.

Alfatide II is ligand for making 18F-Alfatide II PET/CT for Identification of Breast Cancer: A Preliminary Clinical Study. 18F-alfatide II has been proven to have excellent clinical translational potential.

NOTA-NFB is a ligand for making radioactive complex 68Ga-NOTA-NFB, which is am imaging agent and a tracer for CXCR4 evaluation in glioma patients after measuring the dosimetry of 68Ga-NOTA-NFB in healthy volunteers.

Demethyleneberberine, a berberine metabolite, is a mitochondria-targeted antioxidant isolated from Cortex Phellodendri chinensis that exhibits multiple pharmacological activities including anti-microbial, anti-inflammatory, anti-diarrhea and anti-cancer.

Neladalkib, also known as NVL-655, and NUV-655, is a selective, brain-penetrant ALK inhibitor with antitumor activity against the lorlatinib-resistant G1202R/L1196M compound mutation. NUV-655 (NVL-655) inhibited the kinase activity of ALK and ALK G1202R/L1196M with Kiapp < 5 nM in the presence of 1 mM ATP and with selectivity over TRKB. Across a panel of 335 wild-type kinases, NUV-655 (NVL-655) inhibited only 5 other kinases by >50% within 10-fold of its IC50 for ALK. NUV-655 (NVL-655) also selectively inhibited ALK in cells. It inhibited the growth of Ba/F3 cells driven by expression of EML4-ALK variant 1 (v1) with either wild-type kinase domain or drug-resistance mutations G1202R, G1202R/L1196M, or G1202R/G1269A at IC50 values < 10 nM and with selectivity over TRKB. In vivo, NUV-655 (NVL-655) induced regression at well-tolerated doses in a Ba/F3 EML4-ALKv1 G1202R/L1196M xenograft model. Furthermore, NUV-655 (NVL-655) demonstrated brain penetrance in rodent pharmacokinetic studies.

PSMA-I&F is a ligand for making 68Ga/177Lu-PSMA-I&F, which is a PSMA-Targeted Hybrid Tracer. PSMA-I&F is a useful agent for Nuclear and Fluorescence Imaging of Prostate Cancer.

PSMA I＆T is a ligand for making 177Lu-PSMA-I&T for Treatment of Metastatic Castration-Resistant Prostate Cancer.

Mtb ATP synthase-IN-1 is a potent Mycobacterium tuberculosis (Mtb) ATP synthase inhibitor, with MIC of 0.452-0.499 μg/mL against Mtb.

Bromo-PADAP is a dye agent for research use. Bromo-PADAP was reported for the spectrophotometric determination of uranium(VI). Bromo-PADAP is highly sensitive towards uranium, the uranyl complex having a molar absorptivity of 74,000 at 578 nm and pH 7.6. In the presence of a mixed masking solution only a few ions interfere seriously, and the method can be made specific for uranium by a preliminary extraction of uranium into tri-n-octylphosphine oxide, and direct development of the bromo-PADAP colour in the organic phase. Details are given for the determination of uranium in waters, ores, phosphoric acid and phosphate rocks, thorium oxide, and zirconium oxide.

ATH434, also known as PBT434, is a novel, brain-penetrant, inhibitor of α-synuclein aggregation. In transgenic animal models of Parkinson disease (A53T) and MSA (PLP-α-Syn), PBT434 reduced α-synuclein aggregation, preserved neurons and improved motor function. Glial cell inclusions were also reduced in a murine MSA model. PBT434 is thought to act by redistributing reactive iron across membranes, thereby blocking intracellular protein aggregation and oxidative stress. The affinity of PBT434 for iron is greater than that of α-synuclein but lower than that of iron trafficking proteins, e.g., ferritin.

TCMDC-137332 is a compound that exhibits antimalarial activity against Plasmodium falciparum with an IC50 value of 7 nM.

Dimethylamiloride is a Na(+)-H+ exchange inhibitor.

JAK-IN-21 (Example 4) is a selective and potent JAK inhibitor.

Antiviral agent 17 is an anti-infection agent.

H-Val-Pro-Pro-OH is a tripeptide derived from milk proteins, specifically a proline-rich peptide, and is known for its inhibitory activity against Angiotensin I Converting Enzyme (ACE). ACE is a key enzyme in the renin-angiotensin system (RAS), which regulates blood pressure by converting angiotensin I to angiotensin II, a potent vasoconstrictor. Inhibition of ACE leads to reduced angiotensin II levels, resulting in vasodilation and lowered blood pressure.

FHP01 (BA103) is a potent, small molecule inhibitor of DDX3X helicase activity with IC50 of 0.3 uM in in vitro enzyme assays, exhibits very effective antiproliferative and killing activity against different breast cancer cell types (IC50=3.058 and 3.21 μM in MDA MB 468 and MDA MB 231, respectively). FHP01 does not inhibit the ATPase activity of DDX3X and the helicase activity of DDX1 (IC50>100 uM). FHP01 also inhibited WNT signaling, a key tumorigenic pathway already correlated to DDX3X functions in breast cancer model cell lines. FHP01 inhibits ER+/PR+ (IC50 = 12.43 and 10.62 μM in MCF7 and T47D cells, respectively) and HER2+ (IC50 = 13.46 μM in SKBR3) cells, but lower in control MCF10A cells (IC50 = 28.71 μM). FHP01 (45 mg/kg, i.p. injection) suppresses rowth of MDA MB 231 tumor xenografts in nude mice.

HTL0041178 is a potent GPR52 agonist with EC50 of 27.5 nM (human or rat GPR52).

BRD4592 is a small-molecule allosteric inhibitor that targets the tryptophan synthase (TrpAB) of Mycobacterium tuberculosis. TrpAB is a bifunctional enzyme composed of α and β subunits, which catalyzes the final steps of tryptophan biosynthesis. BRD4592 binds at the interface of the α and β subunits, disrupting the enzyme's function.

(R)-GNE-140 (GNE-140) is a novel potent, selective lactate dehydrogenase (LDH) inhibitor with IC50 of 3, 5, and 5 nM for LDHA, LDHB, and LDHC, respectively.

The compound you are referring to is likely a dual inhibitor of p70S6K (S6K1) and Akt, two critical kinases in the PI3K/Akt/mTOR signaling pathway. This pathway is a central regulator of cell growth, proliferation, survival, and metabolism, and its dysregulation is frequently observed in cancers, including solid tumors and non-Hodgkin's lymphoma (NHL). A dual inhibitor targeting both p70S6K and Akt would offer a powerful therapeutic strategy to block this pathway at multiple nodes, potentially overcoming resistance mechanisms and improving treatment outcomes.

CMP-5 (PRMT5-IN-5) is a first-in-class, small-molecule inhibitor that specifically targets protein arginine methyltransferase 5 (PRMT5), an enzyme involved in epigenetic regulation and cellular signaling. PRMT5 catalyzes the symmetric dimethylation of arginine residues on histones and other proteins, playing a critical role in gene expression, cell proliferation, and survival. CMP-5 has shown remarkable specificity in blocking Epstein-Barr virus (EBV)-driven B-lymphocyte transformation and survival, while sparing normal B cells, making it a promising therapeutic candidate for EBV-associated cancers and other PRMT5-dependent diseases.

MT47-100 is a novel compound that exhibits a unique dual functionality as both an allosteric activator and inhibitor of AMP-activated protein kinase (AMPK) complexes, depending on the isoform present. Specifically, MT47-100 acts as a direct activator of AMPK complexes containing the β1 isoform and as a direct inhibitor of AMPK complexes containing the β2 isoform. This isoform-specific modulation of AMPK activity makes MT47-100 a potentially valuable tool for studying the distinct physiological roles of β1- and β2-containing AMPK complexes, as well as a candidate for therapeutic applications targeting AMPK-related pathways.

Hemoglobin modulator TD-1 (TD-1) is a novel allosteric effector of hemoglobin that increases hemoglobin oxygen affinity and reduces SS erythrocyte sickling.

GS-9620 is a potent and selective orally active small molecule agonist of Toll-like receptor 7(TLR-7) in chimpanzees with chronic HBV infection.

α-Galactosylceramide (α-GalCer) is a synthetic glycolipid with antitumorial and immunostimulatory. α-Galactosylceramide is a very potent NKT cell agonist and binds effectively to CD1d. The complex of α-Galactosylceramide plus CD1d binds the NKT cell TCR (T cell antigen receptor).

QS-21, an immunostimulatory saponin, could be used as a potent vaccine adjuvant. QS-21 stimulates Th2 humoral and Th1 cell-mediated immune responses through action on antigen presenting cells (APCs) and T cells. QS-21 can activate the NLRP3 inflammasome with subsequent release of caspase-1 dependent cytokines, IL-1β and IL-18[1][2][3].

Cefonicid Sodium is the sodium salt form of cefonicid, a semisynthetic second-generation broadspectrum cephalosporin with antibacterial activity that inhibits the formation of the bacterial cell wall. Cefonicid binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. PBPs are enzymes involved in the terminal stages of assembling the bacterial cell wall and in reshaping the cell wall during growth and division. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This results in the weakening of the bacterial cell wall and causes cell lysis.