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 (TFA) is a trifluoroacetate (TFA) salt form of the tripeptide H-Val-Pro-Pro-OH, which is derived from milk proteins. This peptide is known for its ability to inhibit Angiotensin I Converting Enzyme (ACE), a key enzyme in the renin-angiotensin system (RAS) that regulates blood pressure. The TFA salt form is commonly used in research and pharmaceutical applications to improve the solubility and stability of the peptide.

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.

ART-812 is a potent inhibitor of DNA polymerase Polθ (also known as Pol theta or POLQ), with an IC50 value of 7.6 nM. This indicates that ART-812 effectively inhibits the enzymatic activity of Polθ at low nanomolar concentrations. Polθ is a key enzyme involved in the microhomology-mediated end joining (MMEJ) pathway, which is an error-prone DNA repair mechanism.

17-AAG (17-N-Allylamino-17-demethoxygeldanamycin), also known by its NSC number 330507 and CP number 127374, is a well-studied inhibitor of Heat Shock Protein 90 (HSP90). HSP90 is a molecular chaperone that plays a critical role in the stabilization and activation of a wide range of client proteins, many of which are involved in oncogenic processes. By inhibiting HSP90, 17-AAG disrupts the function of these client proteins, leading to the degradation of oncogenic proteins and ultimately inhibiting cancer cell growth and survival.

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.

Vamotinib (PF-114) is a potent, selective and orally available inhibitor of native (IC50=0.49 nM) and mutated BCR/ABL (IC50=0.7-4 nM, ABL (T315I) IC50=0.78 nM). PF-114 potently inhibits ABL2, DDR1, DDR2, FMS, FRK, LCK, LYN and PDGFR kinases, but did not inhibit c-SRC, CSK, or c-KIT.

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.

Ilunocitinib (compound 27) is a JAK inhibitor (extracted from patent WO2009114512A1).

(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.

NSC319726 is a mutant p53R175 reactivator; inhibits growth of fibroblasts expressing the p53R175 mutation (IC50 = 8 nM); shows no inhibition for p53 wild-type cells.

CBL0137 (CBL-0137) activates p53 and inhibits NF-kB with EC50s of 0.37 μM and 0.47 μM in the cell-based p53 and NF-kB reporter assays, respectively. It also inhibits histone chaperone FACT (facilitates chromatin transcription complex).

RA608 (RA-608) is a potent, selective, ATP-competitive, orally available CaMKII inhibitor, inhibits human CaMKIIδ, CaMKIIγ, CaMKIIα, and CaMKIIβ with IC50 of 22, 51, 121, and 1135 nM, respectively.RA608 displays a good selectivity profile against a broad panel of 304 human recombinant kinases.RA608 significantly reduces SR Ca leak in human atrial cardiomyocytes, reduces diastolic tension of human atrial trabeculae, does not affect action potential characteristics; attenuates heart failure in the murine HF model induced by TAC.

GS-680 (GS680) is a novel selective and ATP-competitive CaMKII inhibitor with biochemical IC50 of 2.3 and 15.9 nM against CaMKIIδ and CaMKIIα, respectively.GS-680 inhibited phospholamban phosphorylation in NRVM with an EC50 of 98.9 nM.GS-680 inhibits premature atrial contractions.GS-680 significantly reduced CaMKII autophosphorylation.GS-680 inhibits pro-arrhythmic activity in human atrium and improves contractility in failing human ventricle.

TCIP1 is the most potent transcriptional/epigenetic CIP (chemical inducers of proximity) and specifically activates BCL6 target genes. TCIP1 kills diffuse large B cell lymphoma cell lines, including chemotherapy-resistant, TP53-mutant lines and exhibits cell-specific and tissue-specific effects. TCIP1 successfully killed large B cell lymphoma cell lines, including chemotherapy-resistant TP53-mutant lines and exhibited cell-specific and tissue-specific effects. The activation of apoptosis to cell death took place in just 72 hours.BCL6 is critical to the lymphatic system, and mice engineered without the BCL6 gene die of complex inflammatory reactions. BRD4 is heavily involved in genome function and stability across many processes. Concerns regarding utilizing these important gene expressions and how they might affect off-target healthy tissues were addressed in the study.TCIP1 acts in a context-specific manner requiring the expression of BRD4 and BCL6 to both be present in order to bind them and operate at a concentration that would occupy only a tiny fraction of the total BCL6 molecules.TCIP1 induced dramatic transcriptomic changes in the spleen, notably with an upregulation of the FOXO3 gene, which mirrored activity in the targeted cancer cells. Despite the significant transcriptomic changes in the spleen, TCIP1 was well tolerated without adverse effects, with no significant differences in mouse body weight and no noticeable abnormalities such as inflammatory infiltrates or apoptotic cells. BCL6-BRD4 TCIP1 (TCIP1) is a potent BCL6-BRD4 transcriptional/epigenetic chemical inducer of proximity (TCIP) by covalently linking BCL6 binder BI-3812 to BRD4 ligand JQ1, selectively kills DLBCL cells with EC50 of 1.3 nM against KARPAS422 cell. TCIP1 rapidly and robustly killed other DLBCL lines with high levels of BCL6, but JQ1 and BI3812 separately or together shows100–1,000-fold less-effective cell killing. TCIP1 is 200–10,000-fold more potent in killing DLBCL cells than the degradation of BRD4 by dBET1 and/or degradation of BCL6 by BI3802. TCIP1 induces a stable, cooperative protein-protein interaction between bromodomain 1 (BD1) of BRD4 and the BTB domain of BCL6. TCIP1 shows affinity for intracellular ternary complex of BRD4 with Kd of 340 nM in TR-FRET assays. TCIP1 induces G1/S and G2/M block in the cell cycle, TCIP1 (10 nM) represses MYC and its targets while activating pro-apoptotic genes in KARPAS422 cells. TCIP1 kills diffuse large B cell lymphoma cell lines, including chemotherapy-resistant, TP53-mutant lines, at EC50 of 1-10 nM in 72 h and exhibits cell-specific and tissue-specific effects, capturing the combinatorial specificity inherent to transcription.

Nofazinlimab (CS1003) is a humanised IgG4 anti-PD-1 monoclonal antibody. Nofazinlimab can be used for unresectable hepatocellular carcinoma (uHCC) research.