| DC75840 |
Exenatide free base |
Exenatide is a medication used to treat diabetes mellitus type 2. Exenatide binds to the intact human Glucagon-like peptide-1 receptor (GLP-1R) in a similar way to the human peptide glucagon-like peptide-1 (GLP-1); exenatide bears a 50% amino acid homology to GLP-1 and it has a longer half-life in vivo. It is used together with diet, exercise, and potentially other antidiabetic medication. It is a less preferred treatment option after metformin and sulfonylureas. |
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| DC75841 |
Adaprolol maleate |
Adaprolol maleate is a beta-blocker and opthalmic which may be used in the treatment of Glaucoma or other ailments of the eye. Adaprolol has marked electrophysiologic effects. Its major action was on sinus node; it prolonged the basic sinus cycle length and had significant effect on intrinsic automaticity as reflected by the prolonged corrected sinus node recovery time and sinuatrial conduction time. There was, also, direct effect on atrial function and AV nodal function. Adaprolol prolonged the effective refractory period of the His-Purkinje system and the ventricle. The potency of adaprolol's electrophysiologic effects are higher compared to other widely used beta-blockers. Adaprolol appears to be a potent beta-blocker with particularly strong antiarrhythmic effect and it would be very useful in the treatment of both supraventricular and ventricular tachyarrhythmias and ectopic beats. |
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| DC75842 |
Latrepirdine HCl |
Latrepirdine, also known as dimebolin (sold as Dimebon), is an antihistamine drug which has been used clinically in Russia since 1983. Research is continuing in both Russia and western nations into potential applications as a neuroprotective drug to combat Alzheimer's disease and, possibly, as a nootropic as well. However, a Phase III clinical trial for Alzheimer's disease treatment failed to show any benefit. (Source: http://en.wikipedia.org/wiki/Latrepirdine) |
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| DC75843 |
Olodaterol free base |
Olodaterol, also known as BI 1744, is a long acting beta-adrenoceptor agonist used as an inhalation for treating patients with chronic obstructive pulmonary disease (COPD), manufactured by Boehringer-Ingelheim. Olodaterol was approved by FDA in 2014 for the treatment of chronic obstructive pulmonary disease. |
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| DC75844 |
MDK-7553 |
MDK-7553, also known as CD38 inhibitor 78c and Compound-78c, is a potent CD38 inhibitor. MDK-7553 has CAS#1700637-55-3, which was reported in J Med Chem. 2015 Apr 23;58(8):3548-71. For the convenience of scientific communication, we name it as MDK-7553. The last four digits of CAS# were used for its name. |
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| DC75845 |
FIPI free base |
FIPI is a potent and selective phospholipase D inhibitor. FIPI attenuate mercury-induced lipid signaling leading to protection against cytotoxicity in aortic endothelial cells. FIPI rapidly blocks in vivo PA production with subnanomolar potency. FIPI may be a potential therapeutic for autoimmunity and cancer metastasis. |
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| DC75846 |
Gboxin chloride |
Gboxin chloride is an oxidative phosphorylation inhibitor that targets glioblastoma but not embryonic fibroblasts or neonatal astrocytes. Gboxin rapidly and irreversibly compromises oxygen consumption in glioblastoma cells. Gboxin relies on its positive charge to associate with mitochondrial oxidative phosphorylation complexes in a manner that is dependent on the proton gradient of the inner mitochondrial membrane, and it inhibits the activity of F0F1 ATP synthase. |
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| DC75847 |
NLX-204 HCl |
NLX-204 is a potent and selective ERK1/2 phosphorylation-preferring serotonin 5 HT1A receptor agonist with pKi = 10.19. NLX-204 displayed high selectivity in the SafetyScreen44 panel (including hERG channel), high solubility, metabolic stability, and Caco-2 penetration and did not block CYP3A4, CYP2D6 isoenzymes, or P-glycoprotein. Preliminary in vivo studies confirmed its promising pharmacokinetic profile. NLX-204 also robustly stimulated ERK1/2 phosphorylation in rat cortex and showed highly potent (MED = 0.16 mg/kg) and efficacious antidepressant-like activity, totally eliminating immobility in the rat Porsolt test. |
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| DC75848 |
AT-7519 free base |
AT-7519 free base is a drug that acts as a multi-cyclin-dependent kinase inhibitor for Cdk1/cyclin B, Cdk2/Cyclin A, Cdk3/Cyclin E, Cdk4/Cyclin D1, Cdk5/p35, and Cdk6/Cyclin D3. AT7519 is an ATP competitive Cdk inhibitor but is inactive against all non-Cdk kinases with the exception of GSK3β. AT7519 shows potent antiproliferative activity in a variety of human tumor cell lines such as SW620. AT7519 induces activation of GSK-3β by down-regulating GSK-3β phosphorylation, which also contributes to AT7519 induced apoptosis independent of the inhibition of transcription. |
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| DC75849 |
Chloro-SU5416 |
Chloro-SU5416, also known as Chloro-Semaxanib, is a potent and selective FLT3 inhibitor and RET inhibitor. Chloro-Semaxanib is a derivative of Semaxanib with a chloro atom at 5-position. Chloro-SU5416 has inhibitory activity for FLT3 and selectively induces growth arrest, apoptosis, and cell cycle arrest in Ba/F3 and AML cell lines expressing a constitutively activated FLT3. |
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| DC75850 |
SKF-38393 HBr |
SKF-38393, also known as (+/-)-SKF-38393, is a synthetic compound of the benzazepine chemical class which acts as a selective D1/D5 receptor partial agonist. It has stimulant and anorectic effects. SKF 38393 improves temporal order memory performance in maternally deprived rats. SKF 38393 reverses cocaine-conditioned place preference in mice. SKF 38393 induces GAP-43 expression and long-term potentiation in hippocampus in vivo. |
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| DC75851 |
Fatostatin HBr |
Fatostatin, also known as 125B11 or Fatostatin A, is an inhibitor of SREBP activation, preventing SCAP-mediated escort of either SREBP-1 or SREBP-2 to the Golgi (IC50 = 5.6 µM). |
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| DC75852 |
AZD-8418 |
AZD-8418 is an mGlu2 receptor positive allosteric modulators that attenuates nicotine-taking and nicotine-seeking behavior. Acute treatment with AZD8418 (0.37, 1.12, 3.73, 7.46, and 14.92 mg/kg) and AZD8529 (1.75, 5.83, 17.5, and 58.3 mg/kg) deceased nicotine self-administration and had no effect on food-maintained responding. Chronic treatment with AZD8418 attenuated nicotine self-administration, but tolerance to this effect developed quickly. The inhibition of nicotine self-administration by chronic AZD8529 administration persisted throughout the 14 days of treatment. Chronic treatment with either PAMs inhibited food self-administration. AZD8418 (acute) and AZD8529 (acute and subchronic) blocked cue-induced reinstatement of nicotine- and food-seeking behavior. |
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| DC75853 |
Ursodiol |
Ursodiol, also known as Ursodeoxycholic acid, is a synthetically-derived form of ursodiol, a bile acid produced by the liver and secreted and stored in the gallbladder. Also produced by the Chinese black bear liver, ursodiol has been used in the treatment of liver disease for centuries. This agent dissolves or prevents cholesterol gallstones by blocking hepatic cholesterol production and decreasing bile cholesterol. Ursodiol also reduces the absorption of cholesterol from the intestinal tract. |
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| DC75854 |
AZD-1236 |
AZD1236 is a potent and reversible inhibitor of human MMP-9 and MMP-12 (IC50 = 4.5 and 6.1nM, respectively), with >10-fold selectivity to MMP-2 and MMP-13 and >350-fold selectivity to other members of the enzyme family. AZD1236 activity is approximately 20 to 50-fold lower at the rat, mouse, and guinea pig orthologues. In acute models of lung injury, AZD1236 inhibited the haemorrhage and inflammation induced by instillation of human MMP-12 into rat lungs by ~80% at 0.81mg/kg, and also abolished macrophage infiltration into BAL fluid induced by tobacco smoke inhalation in the mouse. |
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| DC75855 |
Pexidartinib HCl |
Pexidartinib, also known as PLX-3397, is a CSF1R inhibitor with IC50 of 20 nM in development by Plexxikon for the treatment of tenosynovial giant cell tumors. It is in a phase 3 clinical trial for Pigmented Villonodular Synovitis (PVNS) or Giant Cell Tumor of the Tendon Sheath (GCT-TS). Pexidartinib hydrochloride exposure induces developmental toxicity and immunotoxicity in zebrafish embryos via activation of Wnt signaling. |
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| DC75856 |
Levofloxacin hydrochloride |
Levofloxacin hydrochloride ((-)-Ofloxacin hydrochloride), a synthetic fluoroquinolone antibiotic, is an inhibitor of DNA gyrase and Topoisomerase IV. It exhibits bactericidal effects by preventing bacterial DNA replication. |
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| DC75857 |
PROTAC tubulin-Degrader-1(compound W13) |
PROTAC tubulin-Degrader-1(compound W13) is an inhibitor of PROTAC tubulin exhibiting antitumor activity against human lung cancer. |
|
| DC75858 |
TH-Z816 |
TH-Z816 is an inhibitor of ,KRAS(G12D) with an IC50 of 14 μM in an SOS-catalyzed nucleotide exchange assay with GDP as the incoming nucleotide. |
|
| DC75859 |
SLF1081851 hydrochloride |
SLF1081851 hydrochloride is a potential inhibitor of Spns2 that blocks S1P release with an IC50 of 1.93 μM. It can be developed as a probe for studying Spns2 biology and immune modulation. |
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| DC75860 |
PHI-101 |
PHI-101 is an orally active, potent third-generation inhibitor of FLT3 that overcomes resistance to multiple drug-resistant mutations. It has potential for research in relapsed or refractory acute myeloid leukemia (AML). |
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| DC75861 |
Bromoenol lactone |
Bromoenol lactone((6E)-Bromoenol lactone) is a selective, irreversible, potent inhibitor of calcium-independent phospholipase A2 (iPLA2β) with an IC50 value of ≈7 μM. It prevents antigen-stimulated exocytosis in mast cells without hindering Ca2+ influx. |
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| DC75862 |
Elenestinib phosphate |
Elenestinib phosphate(BLU-263 phosphate) is a potent and orally active inhibitor of tyrosine kinase that exhibits potent inhibition of c-KIT (D816V) mutation. BLU-263 phosphate has the potential for its use in the research of systemic mastocytosis (SM). |
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| DC75863 |
Envonalkib |
Envonalkib(TQ-B3139; CT-71; Formula 1) is a potent and orally active inhibitor of ALK, that exhibits IC50 values of 1.96 nM, 35.1 nM, and 61.3 nM for wild-type and mutated L1196M and G1269S-ALK. Envonalkib is also used in the research of non-small cell lung cancer. |
|
| DC75864 |
Cu(II)-Elesclomol |
Cu(II)-Elesclomol, a Cu2+ complex of Elesclomol, is a weak inhibitor of DNA topoisomerase I. It is also highly capable of inducing cuproptosis and apoptosis. It induces DNA double-strand breaks in K562 cells and causes a G1 cell cycle block. Cu(II)-Elesclomol displays anticancer activity. |
|
| DC75865 |
TI17 |
TI17 is an inhibitor of thyroid hormone receptor-interacting protein Trip13. TI17 efficiently suppresses the proliferation of multiple myeloma (MM) cells and triggers cell cycle arrest and apoptosis. Trip13, an AAA-ATPase involved in double-strand break (DSB) repair, is targeted by TI17, leading to impaired function and heightened DNA damage. |
|
| DC75866 |
(R)-HTS-3 (GLXC-25878) |
(R)-HTS-3 (GLXC-25878) is a potent, selective, and cell-active inhibitor of lysophosphatidylcholine acyltransferase 3 (LPCAT3) with an IC50 of 0.09 µM, an enzyme critical for synthesizing C20:4-containing phospholipids. It reduces arachidonic acid-d8 incorporation into phospholipids and mitigates RSL3-induced ferroptosis in HT-1080 and 786-O cancer cells. |
|
| DC75867 |
Ifebemtinib |
Ifebemtinib(IN10018, BI853520) is a highly selective, potent inhibitor of focal adhesion kinase (FAK), with an IC50 of 1 nM for inhibiting FAK autophosphorylation. It also inhibits FER Kinase and FES Kinase with IC50s of 900 nM and 1040 nM, respectively, inhibiting spheroid formation and orthotopic tumor growth in malignant pleural mesothelioma. IN10018 exhibits anti-tumor activity in vitro and in vivo. |
|
| DC75868 |
AZ14133346 |
AZ14133346 (compound 36) is a potent and selective inhibitor of EGFR Exon20 insertions, with the IC50 of 85 nM. AZ14133346 plays an important role in cancer research. |
|
| DC75869 |
MI-217 |
MI-217 is a potent SIRT3 inhibitor. MI-217 induces MDA-MB-231 apoptosis. MI-217 can be used in the study of breast cancer. |
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