| DC75515 |
S107 free base |
S107 is a Type 1 ryanodine receptor (RyR1) stabilizer; binds RyR1 and enhances the binding affinity of calstabin-1. Inhibits Ca leak from the sarcoplasmic reticulum (SR). |
|
| DC75516 |
GJ-103 free acid |
GJ-103 is an active analog of the read-through compound GJ072. Chemical-induced read through of premature stop codons might be exploited as a potential treatment strategy for genetic disorders caused by nonsense mutations. |
|
| DC75517 |
ML241 HCl |
ML241 is a potent and selective inhibitors of p97 ATPase. ML241 inhibit p97 ATPase with IC(50) values of 100 nM. ML241 inhibits degradation of a p97-dependent but not a p97-independent proteasome substrate in a dual-reporter cell line. ML241 may be a novel agent for the chemotherapy of cancer, and provide a rationale for developing pathway-specific p97 inhibitors. |
|
| DC75518 |
BMS-986205 |
Linrodostat, also known as BMS-986205, ONO-7701 and F001287, a potent and selective, orally active IDO1 inhibitor with potential immunomodulating and antineoplastic activities. BMS-986205 specifically targets and binds to IDO1, a cytosolic enzyme responsible for the oxidation of the amino acid tryptophan into the immunosuppressive metabolite kynurenine. By inhibiting IDO1 and decreasing kynurenine in tumor cells, BMS-986205 restores and promotes the proliferation and activation of various immune cells, including dendritic cells (DCs), natural killer (NK) cells, and T lymphocytes, and causes a reduction in tumor-associated regulatory T cells (Tregs). |
|
| DC75519 |
GJ-103 sodium |
GJ103 sodium salt is an active analog of the read-through compound GJ072. Chemical-induced read through of premature stop codons might be exploited as a potential treatment strategy for genetic disorders caused by nonsense mutations. |
|
| DC75520 |
BAY41-4109 racemic |
BAY41-4109 racemic is a mixture of R-isomer of BAY41-4109 and S-isomer of BAY41-4109. BAY-41-4109 is a heteroaryldihydropyrimidine (HAP) antiviral compound effective on Hepatitis B virus (HBV) capsid assembly and on preformed HBV capsids. |
|
| DC75521 |
PF-CBP1 HCl |
PF-CBP1, also known as PF-06670910, is potent and highly-selective inhibitor of the bromodomain of CREB binding protein (CBP BRD) that down regulates targets of CBP in macrophages primary neurons. |
|
| DC75522 |
BEC HCl |
BEC, also known as S-(2-boronoethyl)-L-cysteine, is an a slow-binding and competitive Arginase II inhibitor with Ki of 0.31 μM (ph 7.5). BEC significantly enhances NO-dependent relaxation of human penile corpus canvernosum smooth muscle in vitro at concentrations between 0.1-1.0 mM. S-(2-boronoethyl)-L-cysteine binds to arginase as a transition state analogue and enhances smooth muscle relaxation in human penile corpus cavernosum. |
|
| DC75523 |
Odevixibat |
Odevixibat, also known as AZD 8294, is a potent, once-daily, non-systemic ileal bile acid transport inhibitor (IBATi). Odevixibat is being developed to treat rare pediatric cholestatic liver diseases, including progressive familial intrahepatic cholestasis (PFIC), biliary atresia and Alagille syndrome. Odevixibat acts locally in the small intestine. Odevixibat was approved in 2021 to treat pruritus. |
|
| DC75524 |
SP-187 HCl |
SP-187, also known as N-9-DNJ and UV-4B, is an alpha-Glucosidase inhibitor potentially for the treatment of dengue fever and influenza infection. Proline-producing strains of Serratia marcescens were more osmotolerant than wild-type strains. Growth inhibition by proline analogs was significantly enhanced by increasing the osmotic stress of the medium. |
|
| DC75525 |
PD168,077 new |
PD168,077 is a dopamine D4 receptor agonist which has a facilitatory effect on memory consolidation. |
|
| DC75526 |
Sudoterb free base |
Sudoterb, also known as LL3858, is an anti-tubercular drug candidate. |
|
| DC75527 |
Rucaparib free base |
Rucaparib is a tricyclic indole poly(ADP-Ribose) polymerase (PARP1) inhibitor with potential chemosensitizing, radiosensitizing, and antineoplastic activities. Rucaparib selectively binds to PARP1 and inhibits PARP1-mediated DNA repair, thereby enhancing the accumulation of DNA strand breaks and promoting genomic instability and apoptosis. |
|
| DC75528 |
Phosphoethanolamine |
Phosphoethanolamine is an ethanolamine derivative that is used to construct two different categories of phospholipids. One category termed a glycerophospholipid and the other a sphingomyelin, or more specifically within the sphingomyelin class, a sphingophospholipid. Phosphorylethanolamine is a polyprotic acid with two pKa values at 5.61 and 10.39. On April 14, 2016, a law was passed in Brazil allowing the use of synthetic phosphoethanolamine for cancer treatment, despite opposition from the Brazilian Medical Association, the Brazilian Society of Clinical Oncology, and the regulatory agency ANVISA. However, shortly after, the country's Supreme Court suspended the law. |
|
| DC75529 |
JNJ16259685 |
JNJ16259685 is a potent, non-competitive mGlu1 antagonist (Ki = 0.34 nM). JNJ16259685 inhibits glutamate-induced Ca2+ response at the human mGlu1 receptor with an IC50 value of 0.55 nM. JNJ16259685 is selective over mGlu5 (> 400-fold) and displays no activity at mGlu2, mGlu3, mGlu4, mGlu6, AMPA or NMDA receptors (IC50 > 10 μM). |
|
| DC75530 |
Givinostat HCl |
Givinostat or gavinostat, aslo known as ITF2357, is a potent and orally active histone deacetylase inhibitor with potential anti-inflammatory, anti-angiogenic, and antineoplastic activities. It is a hydroxamate used in the form of its hydrochloride. Inhibition of HDAC activity by ITF2357 ameliorates joint inflammation and prevents cartilage and bone destruction in experimental arthritis.ITF2357 reduces cytokines and protects islet β cells in vivo and in vitro. ITF2357 decreases surface CXCR4 and CCR5 expression on CD4(+) T-cells and monocytes and is superior to valproic acid for latent HIV-1 expression in vitro. |
|
| DC75531 |
BAY-K-8644 |
BAY-K-8644, also known as BAYK 8644 andBAY-K-8644, is a L-type Ca2+ channel activator (EC50 = 17.3 nM). BAYK 8644 has positive inotropic, vasoconstrictive and behavioral effects in vivo. |
|
| DC75532 |
PMPA free acid |
PMPA is a NAALADase inhibitor. PMPA increases threshold for electroconvulsions and enhances the antiseizure action of valproate against maximal electroshock-induced seizures in mice. Inhibition of NAALADase by 2-PMPA attenuates cocaine-induced relapse in rats: a NAAG-mGluR2/3-mediated mechanism. PMPA attenuates magnetic resonance BOLD signals in brain of anesthetized mice: evidence of a link between neuron NAAG release and hyperemia. |
|
| DC75533 |
AZD8542 |
AZD8542 is an antagonist of Smoothened (SMO), with potential as an oncology therapeutic. It is a novel Hedgehog (Hh) pathway antagonist on tumor progression with an emphasis on the role of the stroma compartment. |
|
| DC75534 |
AZD6703 free base |
AZD6703 is a potent, selective and reversible orally bioavailable inhibitor of p38 mitogen-activated protein kinase 14 (MAPK14). |
|
| DC75535 |
Importazole HCl |
Importazole is a small molecule inhibitor of the transport receptor importin-β. Importazole specifically inhibits the function of importin-β, likely by altering its interaction with RanGTP. Importazole is a valuable tool to evaluate the function of the importin-β/RanGTP pathway at specific stages during the cell cycle. |
|
| DC75536 |
Pibrentasvir |
Pibrentasvir, also known as ABT-530, is a protease inhibitor potentially for the treatment of HCV infection. |
|
| DC75537 |
AZD-1386 |
AZD1386 is an orally available antagonist of the transient receptor potential channel TRPV1. Note: Structure of this product was from NIH/NCATS web page: https://drugs.ncats.io/drug/210323T9CP and drugbank web page: https://go.drugbank.com/drugs/DB15333. |
|
| DC75538 |
LY2365109 HCl |
LY2365109 is a Potent and selective glycine transporter 1 (GlyT1) inhibitor (IC50 values are 15.8 and > 30 000 nM at GlyT1 and GlyT2 respectively). LY2365109 increased cerebrospinal fluid levels of glycine and potentiated NMDA-induced increases in dialysate levels of neurotransmitters in the prefrontal cortex (PFC) and the striatum. GlyT1 overexpression in the epileptic brain constitutes a new target for therapeutic intervention, and that GlyT1 inhibitors constitute a new class of antiictogenic drugs. |
|
| DC75539 |
AZD6538 |
AZD6538 is a novel mGluR5 negative allosteric modulators selected for clinical development. |
|
| DC75540 |
Exatecan mesylate |
Exatecan, also known as DX 8951, is semisynthetic, water-soluble camptothecin derivative with antineoplastic activity. Exatecan mesylate inhibits topoisomerase I activity by stabilizing the cleavable complex between topoisomerase I and DNA and inhibiting religation of DNA breaks, thereby inhibiting DNA replication and triggering apoptotic cell death. This agent does not require enzymatic activation and exhibits greater potency than camptothecin and other camptothecin analogues |
|
| DC75541 |
Ulixertinib HCl |
Ulixertinib, also known as BVD-523 and VRT752271, is an inhibitors of ERK protein kinase. Downmodulation of ERK protein kinase activity inhibits VEGF secretion by human myeloma cells and myeloma-induced angiogenesis. Upon oral administration, BVD-523 inhibits both ERK 1 and 2, thereby preventing the activation of ERK-mediated signal transduction pathways. This results in the inhibition of ERK-dependent tumor cell proliferation and survival. The mitogen-activated protein kinase (MAPK)/ERK pathway is often upregulated in a variety of tumor cell types and plays a key role in tumor cell proliferation, differentiation and survival. |
|
| DC75542 |
LP-471756 |
LP-471756 is antagonist of GPR139. |
|
| DC75543 |
Mozavaptan free base |
Mozavaptan, also known as OPC 31260, is a vasopressin receptor antagonist marketed by Otsuka. In Japan, it was approved in October 2006 for hyponatremia (low blood sodium levels) caused by syndrome of inappropriate antidiuretic hormone (SIADH) due to ADH producing tumors. |
|
| DC75544 |
OTS514 HCl |
OTS514 is a potent TOPK (T-LAK cell-originated protein kinase) inhibitor. OTS514 exhibits growth suppressive effect on small cell lung cancer. TS514 effectively suppressed growth of SCLC cell lines (IC50 ; 0.4 ~ 42.6 nM) and led to their apoptotic cell death. Treatment with OTS514 suppressed forkhead box protein M1 (FOXM1) activity, which was involved in stemness of CSC. Furthermore, OTS514 treatment reduced CD90-positive SCLC cells and showed higher cytotoxic effect against lung sphere-derived CSC-like SCLC cells. |
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