(Rac)-AAA is the racemate of AAA. (Rac)-AAA is an antagonist of 20-HETE receptor. (Rac)-AAA can increase the expression of GPR75 receptor in androgen-insensitive prostate cancer cells. (Rac)-AAA dose-dependently increases p38 phosphorylation. (Rac)-AAA induces a significant decrease in the phosphor-AKT signal in nuclei of cells. (Rac)-AAA mitigates the NF-κB signal in unstimulated cell nuclei. (Rac)-AAA can diminish the membrane associated signal intensity. (Rac)-AAA decreases the FAK phosphorylation induced by 20-HETE.

SCH 34343 is a penem antibiotic. SCH 34343 is highly active against Streptococcus pneumoniae (MIC50 ≤ 0.015 mg/L), viridans streptococci (MIC50 = 0.06 mg/L), streptococci of groups A (MIC50 = 0.03 mg/L), B (MIC50 = 0.06 mg/L), C and G (MIC50 = 0.03 mg/L), and Str. bovis. SCH 34343 can be used for antibacterial research.

DZ-2640 is an oral Carbapenem antibiotic, a prodrug of DU-6681. DU-6681 exhibits antibacterial activity against a broad spectrum of gram-positive and -negative bacteria.

DU-6681 is the active parent compound of DZ-2640. DU-6681 possesses a broad-spectrum and potent in vitro antibacterial activity against the majority of gram-positive and gram-negative bacteria. DU-6681 can be used for antibacterial research.

TPG-20A is a SARS-CoV-2 main protease inhibitor with an IC50 of 27.8 nM. TPG-20A also inhibits MERS-CoV main protease. TPG-20A can be used for the research of infection, such as SARS-CoV-2.

AR-709 is a new type of diaminopyrimidine antibiotic. AR-709 exhibits potent and broad-spectrum antibacterial activity against Streptococcus pneumoniae (MIC = 0.03 mg/L). AR-709 can be used for research on bacterial infections.

KT53 is a highly active, selective, and cell penetrable GSTO1 inhibitor. KT53 can effectively inhibit GSTO1 activity in MDA-MB-435 (IC50 = 35 nM) cells. KT53 significantly enhances the killing effect of cisplatin on MDA-MB-435 cancer cells. KT53 can be used for cancer research.

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i-AZD1775 (TFA) is an immobilizable analogue of AZD1775. i-AZD1775 (TFA) retains the ability to inhibit WEE1 in vitro. i-AZD1775 (TFA) can be studied in anticancer research.

HPK1 ligand-Linker Conjugate 1 is a synthesized target protein ligand-linker conjugate that can be used for synthesis of PROTACs, such as PROTAC HPK1 Degrader-5. PROTAC HPK1 Degrader-5 is a potent and orally active HPK1 PROTAC degrader with anti-tumor activity.

Tropapride is a dopamine D2 receptor antagonist. Tropapride can be used for the research of neurological disease.

EXP-6803 is a specific nonpeptide angiotensin II receptor antagonist with antihypertensive activity. EXP-6803 inhibits the contractile response to angiotensin II with a pA2 value of 7.20. EXP-6803 effectively blocks responses to angiotensin I and II while not affecting responses to bradykinin or acetylcholine in guinea pig ileum. EXP-6803 can be used for hypertension research.

Dalvotoclax (Example 8) is a selective inhibitor of BCL-2. Dalvotoclax has good liver microsomal stability. Dalvotoclax inhibits the activity of anti-apoptotic BCL-2 protein and anti-apoptotic BCL-XL protein. Dalvotoclax can be studied in research for B cell leukemia.

TMP1 is an orally active bispecific inhibitor of M pro (IC50 = 312.5 nM)/TMPRSS2 (IC50 = 1.28 μM, KD = 10.10 μM). TMP1 exhibits broad protection against different SARS-CoV-2 variants in vitro. TMP1 cross-protects against highly pathogenic coronaviruses (SARS-CoV-1, SARS-CoV-2, and MERS-CoV) in vivo and effectively blocks the transmission of SARS-CoV-2. TMP1 can inhibit infection by SARS-CoV-2 escape mutants that are resistant to Nivolumab. TMP1 can be used in coronavirus research.

JMV 3008 is a GHS-R1a antagonist with an IC50 of 5.6 nM. JMV 3008 can be used in the research of diseases such as diabetes and obesity.

BMS 605339 is a linear tetra-peptide α-ketoamide inhibitor of HCV NS3 protease. BMS 605339 can be used in research related to hepatitis C (HCV infection).

BL-8030 is an anti-HCV agent. BL-8030 can be used for the research of infection.

ISAM-CG557 is a selective CB2R agonist, with a Ki of 54.6 nM. ISAM-CG557 reduces intracellular ROS levels and caspase activity. ISAM-CG557 exhibits significant MAPK bias and moderate G-protein bias, with CB2R EC50s of 0.60 nM (cAMP), 60.9 nM (β-arrestin) and 0.03 nM (MAPK). ISAM-CG557 exerts potent anti-inflammatory effects by reducing pro-inflammatory cytokines and increasing anti-inflammatory cytokines in cells. ISAM-CG557 can be used for the study of neuroinflammatory and neurodegenerative disorders.

RS-0481 is an orally active lymphocyte population function restorer. RS-0481 enhances IL-2 production activity. RS-0481 can re-establish the function of certain lymphoid cell populations impaired by the presence of a growing tumor in an animal. RS-0481 markedly augments the tumor-specific cytotoxic T lymphocytes, TDTH, and the nonspecific lymphokine-activated-killer-cell-like cell responses.

GP1 precursor has high affinity to GPIIb/IIIa receptors of activated platelets. GP1 precursor can be radiolabeled with [18F] and used as a PET Tracer for visualizing active platelet aggregation at the molecular level. GP1 precursor can be used for the detection of Thrombi.

(-)-JJ-450 is a non-competitive antagonist targeting the androgen receptor (AR). (-)-JJ-450 is more potent than (+)-JJ-450 in inhibiting androgen-induced AR activity, and the mechanism of AR inhibition by (+)-JJ-450 is different from that of Enzalutamide (MDV3100), which may target the ligand binding domain (LBD) of AR. (-)-JJ-450 inhibits the transcriptional activity of wild-type AR and mutant ARF876L by inhibiting AR nuclear translocation and promoting nuclear degradation of unbound AR. (-)-JJ-450 can be used in the study of castration-resistant prostate cancer (CRPC) resistant to Enzalutamide.

SPK-843 is an antifungal agent. SPK-843 shows inhibitory activity against A. fumigatus MF-13, A. flavus TIMM 0057, and A. niger TIMM 2814 with MICs of 0.5 μg/mL, 0.25 μg/mL, and 0.0625 μg/mL, respectively. SPK-843 exhibits dose-dependent efficacy in murine models of pulmonary aspergillosis. SPK-843 can be used for the research of related fungal infections.

YH-0623 is an orally active mitochondrial RNA polymerase (POLRMT) inhibitor (IC50 = 50.48 nM, Nanoluciferase Bioluminescence Resonance Energy Transfer (NanoBRET) assay). YH-0623 exhibits antiproliferative effects on 22Rv1 cells by reducing the expression of mitochondrial-related genes. YH-0623 inhibits 22Rv1 cell growth, colony formation, and the expression of OXPHOS-related proteins. YH-0623 significantly inhibits tumor growth in a prostate cancer xenograft mouse model. YH-0623 is indicated for prostate cancer research.

(1S,2S,3R)-PLX-4545 is the (1S,2S,3R) enantiomer of PLX-4545. PLX-4545 is an orally active and selective cereblon-based molecular glue degrader of IKZF2 (zinc finger transcription factor Helios). PLX-4545 can reprogram immunosuppressive regulatory T cells into pro-inflammatory effector T cells, thereby enhancing anti-tumor immune responses.

MC-207110 is a broad-spectrum efflux pump inhibitor. MC-207110 is active against all three known Mex efflux pumps from P. aeruginosa and their close Escherichia coli efflux pump homolog (AcrAB-TolC). MC-207110 can decrease the intrinsic resistance of P. aeruginosa to fluoroquinolones. MC-207110 can be used for the research of infection .

WAY-126299A is an orally active dual-acting 5-1ipoxygenase inhibitor (IC50: 12.2 μM) and leukotriene D4 antagonist (pKB: 6.4). WAY-126299A inhibits antigen-induced leukotriene-dependent bronchoconstriction. WAY-126299A can be used for research of asthma.

MK-2748 is a hepatitis C virus (HCV) NS3/4a protease inhibitor. MK-2748 exhibits broad-spectrum and potent antiviral activity, with nanomolar-level activity against all genotypes (gt1a-gt6) (IC₅₀ < 0.115 nM), showing only slightly weaker activity against gt3a (1.212 nM), and maintaining high inhibitory activity against drug-resistant mutant strains such as gt1b R155K (IC₅₀ = 0.032 nM) and D168Y (IC₅₀ = 0.057 nM). MK-2748 can be used in the research of HCV infection.

BMS-354326 is a tryptase inhibitor with an IC50 of 1.8 nM. BMS-354326 exhibits excellent selectivity against trypsin and most other related serine proteases. BMS-354326 can be used in the research of asthma and inflammatory diseases.

U80215, a dansylated peptide, is a competitive human renin inhibitor with the IC50 of 2.3 μM. U80215 shows excitation and emission maxima at 340 and 530 nm.

Onychocin B is a cyclic tetrapeptide isolated from Onychocola sclerotica. Onychocin B is a calcium channel blocker with an IC50 of 7.1 μM for Cav1.2.