| 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. |
|
| 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. |
|
| 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). |
|
| 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. |
|
| 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). |
|
| 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. |
|
| DC75870 |
(S)-Gebr32a |
(S)-Gebr32a is a potent PDE4 inhibitor with IC50 values of 19.5, 2.1 µM for PDE4 cat; PDE4D3, respectively. |
|
| DC75871 |
ST80 |
ST80 is an inhibitor for interaction of OTUD4 and CD73. ST80 decreases CD73 protein level, increases CD73 protein turnover, reduces immune evasion of tumor cells, and thus exhibits antitumor efficacy against immunosuppressive triple-negative breast cancer (TNBC). |
|
| DC75872 |
HL435 |
HL435 is a heterobifunctional molecule that degrades BRD4 by linking to JQ1, with DC50 of 11.9 nM and 21.9 nM, in MDA-MB-231 and MCF-7 cells, respectively. HL435 inhibits the proliferation of MDA-MB-231, MCF-7, 22Rv1 and A549, arrests the cell cycle and induces apoptosis. HL435 exhibits antitumor activity in mouse model. |
|
| DC75873 |
Rugonersen sodium |
Rugonersen sodium is a locked-nucleic acid (LNA)- modified antisense oligonucleotides (ASOs), and results in reduction of ubiquitin-protein ligase E3A (UBE3A) silencing. Angelman syndrome (AS) sodium is a severe neurodevelopmental disorder caused by the loss of neuronal E3 ligase UBE3A, Rugonersen has been used for AS reasearch. |
|
| DC75874 |
Tritetracosanoin |
Tritetracosanoin (Trilignocerin) is a triacylglycerol of the tetracosanoic acid. |
|
| DC75875 |
BMS-185411 |
BMS-185411 is a selective retinoic acid receptor alpha (RARα) antagonist, with an IC50 value of 140 nM. |
|
| DC75876 |
Amoitone B |
Amoitone B, a derivative of cystosporone B, is an agonist of NR4A1. Amoitone B has anticancer activity. |
|
| DC75877 |
7(S)-Maresin 1 |
7(S)-Maresin 1 is an inactive 7(S) exomer of Maresin 1, containing a 7(R) hydroxyl group. It can be used as a negative control. Maresin 1 is a specific regulator of endogenous DHA production in the human body, which can stimulate the production and secretion of intracellular Ca2+. |
|
| DC75878 |
(Rac)-L-659989 |
(Rac)-L-659989 is the racemate of L-659989. L-659989 s an orally active, extremely potent, selective and competitive platelet activating factor (PAF) receptor antagonist. |
|
| DC75879 |
MRS8028 |
MRS8028 is an agonist for A3 adenosine receptor (A3AR), which binds hA3AR with Ki of 2.44 nM. MRS8028 is potential for ameliorating ischemia and inflammatory diseases. |
|
| DC75880 |
Lanepitant |
Lanepitant (LY303870) is a selective neurokinin-1 (NK-1) receptor antagonist. Lanepitant blocks neurogenic inflammation and pain transmission by preventing the binding of substance P to NK-1 receptors on both neuronal and non-neuronal tissues. Lanepitant can be used to study osteoarthritis. |
|
| DC75881 |
O-Arachidonoyl glycidol |
O-Arachidonoyl glycidol (compound 1) is a 2-arachidonoylglycerol (2-AG) analog. O-Arachidonoyl glycidol inhibits cytosolic 2-oleoylglycerol (2-OG) hydrolysis with an IC50 value of 4.5 µM. O-Arachidonoyl glycidol blocks 2-OG hydrolysis in membrane fractions and anandamide hydrolysis with IC50s of 19, 12 µM, respectively. |
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