| DC74726 |
Nintedanib esylate |
Nintedanib, also known as BIBF1120, is a potent inhibitor of multiple receptor tyrosine kinases (RTKs) and non-receptor tyrosine kinases (nRTKs). Nintedanib inhibits the following RTKs: platelet-derived growth factor receptor (PDGFR) α and β, fibroblast growth factor receptor (FGFR) 1-3, vascular endothelial growth factor receptor (VEGFR) 1-3, and Fms-like tyrosine kinase-3 (FLT3). Nintedanib binds competitively to the adenosine triphosphate (ATP) binding pocket of these receptors and blocks the intracellular signaling which is crucial for the proliferation, migration, and transformation of fibroblasts representing essential mechanisms of the IPF pathology. Nintedanib esylate was approved in 2014 for the treatment of idiopathic pulmonary fibrosis (IPF). |
|
| DC74727 |
Nirogacestat free base |
Nirogacestat, also known as PF-03084014, is a potent and selective gamma secretase (GS) inhibitor with potential antitumor activity. PF-03084014 binds to GS, blocking proteolytic activation of Notch receptors. Nirogacestat enhances the Antitumor Effect of Docetaxel in Prostate Cancer. Nirogacestat enhances docetaxel-mediated tumor response and provides a rationale to explore GSIs as adjunct therapy in conjunction with docetaxel for men with CRPC (castration-resistant prostate cancer). |
|
| DC74728 |
Cardiogenol C HCl |
Cardiogenol C is a diaminopyrimidine compound that induces the differentiation of MHC- (myosin heavy chain) positive cardiomyocytes from embryonic stem cells with an EC50 value of 0.1 µM. Cardiogenol C upregulates cardiac markers and induces cardiac functional properties in lineage-committed progenitor cells. Cardiogenol C can induce Mouse Hair Bulge Progenitor Cells to Transdifferentiate into Cardiomyocyte-like Cells. |
|
| DC74729 |
Rezatapopt |
Rezatapopt, also known as PC14586, is p53 Y220C reactivator that binds selectively to p53 Y220C mutant protein and restores the p53 wildtype conformation and transcriptional activity, resulting in potent preclinical antitumor activity. PC14586 was structurally designed to bind tightly to a crevice within the mutant protein (KD~2.5 nM). PC14586 was shown to stabilize the Y220C mutant in the wild type conformation, resulting in reactivation of p53 transcriptional activity and subsequent expression of its target proteins (e.g. p21, MDM2, Bax, PUMA). The reactivation of p53 function is highly selective to Y220C mutant cells and results in arrest of the cell cycle in vitro (IC50 ~0.230-1.8 μM). In nude mice bearing Y220C mutant NUGC3 gastric cancer xenograft tumors, oral administration of PC14586 results in a dose responsive anti-tumor effect. In human xenografts, PC14586 was shown to convert Y220C mutant to the wildtype conformation, resulting in activation of p53 transcription. |
|
| DC74730 |
Pimicotinib |
Pimicotinib, also known as ABSK021, is a tyrosine kinase inhibitor and antineoplastic. It is a small molecule CSF-1R inhibitor that is orally available. Pimicotinib has antitumor activity and a solid white to off-white appearance. Its formula is C22H24N6O3 and its CAS number is 2253123-16-7. |
|
| DC74731 |
Xanthine oxidoreductase-IN-5 |
Xanthine oxidoreductase-IN-5 is an orally active xanthine oxidoreductase (XOR) inhibitor |
|
| DC74732 |
BLK degrader1 |
BLK degrader 1 (compound 9) is a selective degrader of B-lymphoid tyrosine kinase (BLK). |
|
| DC74733 |
Orziloben |
Orziloben is a medium chain fatty acid (MCFA) analogue. |
|
| DC74734 |
Telotristat ethyl |
Telotristat ethyl, also known as LX 1032 or LX 1606, is an oral serotonin synthesis inhibitor or peripheral tryptophan hydroxylase (TPH) inhibitor . Telotristat etiprate has activity in controlling diarrhea associated with carcinoid syndrome. LX1606 acts by inhibiting the enzyme tryptophan hydoxylase (TPH) and reduces serotonin production both inside and outside the GI tract without affecting brain serotonin levels. TPH is the rate-limiting enzyme involved in serotonin biosynthesis and is present in metastatic carcinoid tumor cells. |
|
| DC74735 |
BCAT-IN-4 |
BCAT-IN-4 (Compound 1) is a BCAT inhibitor. |
|
| DC74736 |
HA5 |
HA5 inhibits Streptococcus mutans biofilm. |
|
| DC74737 |
Antitumor agent-109 |
Antitumor agent-109 (compound 6) is an inhibitor of hyaluronic acid (HY-B0633A) targeting to CD44. |
|
| DC74738 |
HDAC-IN-58 |
HDAC-IN-58 is a HDAC inhibitor. |
|
| DC74739 |
rac-Vestitone |
Vestitone reductase catalyzes a stereospecific NADPH-dependent reduction of (3R)-vestitone in the bio sysnthesis of antimicrobial isoflavonoid phytoalexin medicarpin. |
|
| DC74740 |
URAT1 inhibitor 7 |
URAT1 inhibitor 7 (compound 10f) is a potent URAT1 inhibitor. |
|
| DC74741 |
FC-116 |
FC-116 is a Tubulin inhibitor that effectively inhibits tumor growth in mice. |
|
| DC74742 |
STAT3-IN-15 |
STAT3-IN-15 is a potent and orally active STAT3 inhibitor. |
|
| DC74743 |
sEH inhibitor-14 |
sEH inhibitor-14 (compound 33) is a benzoxazolone-5-urea analogue. |
|
| DC74744 |
BBT |
BBT is an enhancer of impaired glucose-stimulated insulin secretion (GSIS). |
|
| DC74745 |
(-)-GSK598809 free base |
(-)-GSK598809, also known as (1S,5R)-GSK598809, is a selective D(3)R antagonist recently progressed in Phase I trials. GSK-598809 may decrease the rewarding effects of contextual cues associated with drug intake preclinically, which may reduce drug craving in humans. |
|
| DC74746 |
DC-Y13-27 |
DC-Y13-27, a derivative of DC-Y13, is a YTHDF2 inhibitor (KD: 37.9 μM). |
|
| DC74747 |
Xanthine oxidoreductase-IN-4 |
Xanthine oxidoreductase-IN-4 is an orally active xanthine oxidoreductase (XOR) inhibitor. |
|
| DC74748 |
O4I4 |
O4I4 (compound 23) is a OCT4-inducing compound with metabolical stability. |
|
| DC74749 |
Mtb-IN-2 |
Mtb-IN-2 (compound 10c) is an antimicrobial agent against Mycobacterium tuberculosis (Mtb). |
|
| DC74750 |
Kanamycin A sulfate |
Kanamycin, also known as kanamycin A, is an aminoglycoside bacteriocidal antibiotic, available in by mouth, intravenous, and intramuscular forms, and used to treat a wide variety of infections. Kanamycin is isolated from the bacterium Streptomyces kanamyceticus and its most commonly used form is kanamycin sulfate. Kanamycin interacts with the 30S subunit of prokaryotic ribosomes. It gives birth to substantial amounts of mistranslation and indirectly inhibits translocation during protein synthesis. |
|
| DC74751 |
SAR407899 free base |
SAR407899 is a potent and selective Rho kinase inhibitor with promising antihypertensive activity. SAR407899 potently inhibits endothelin-1-induced constriction of renal resistance arteries. SAR407899 is equipotent against human and rat-derived Rho-kinase 2 with inhibition constant values of 36 nM and 41 nM, respectively. SAR407899 is approximately 8-fold more active than fasudil. SAR407899 potently (mean IC(50) values: 122 to 280 nM) and species-independently relaxed precontracted isolated arteries of different species and different vascular beds. The antihypertensive effect of SAR407899 was superior to that of fasudil and Y-27632. |
|
| DC74752 |
SARS-CoV-2-IN-39 |
SARS-CoV-2-IN-39 (compound 21) is a SARS-CoV-2 inhibitor with an EC50 of 1 μM. |
|
| DC74753 |
L-Tyrosinol HCl |
L-Tyrosine is an aromatic, polar, non-essential amino acid that contains a highly reactive α-amino, α-carboxyl, and phenolic hydroxyl group. L-tyrosine modulates biofilm formation of Bacillus cereus ATCC 14579. L-Tyrosine Limits Mycobacterial Survival in Tuberculous Granuloma. |
|
| DC74754 |
SB-277011 HCl |
SB-277011, also known as SB-277011-A, is an orally active, potent and selective dopamine D(3) receptor antagonist with high oral bioavailability and CNS penetration in the rat. SB-277011 potentiated phMRI response to acute amphetamine challenge in the rat brain. SB-277011 attenuated ethanol consumption in ethanol preferring (P) and non-preferring (NP) rats. |
|
| DC74755 |
Prulifloxacin |
Prulifloxacin, also known as NM-441, is an inhibitor of bacterial DNA gyrase used to treat urinary tract infections. Prulifloxacin is an oral fluoroquinolone with a broad in vitro activity spectrum against Gram positive and negative bacteria and among fluoroquinolones has the lowest power of inducing resistance. In vitro and in vivo studies have shown its clinical efficacy and pathogen eradication. |
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