| DC75605 |
Isuzinaxib |
APX-115, also known as EWHA-18278, is a potent, orally active pan NADPH oxidase (Nox) inhibitor. APX-115 protects development of diabetic nephropathy in podocyte specific NOX5 transgenic mice. APX-115 might be a promising therapeutic agent for the treatment of DN because of its pan-NOX inhibitory activity, including its NOX5 inhibitory activity, and also owing to its anti-inflammatory effect. |
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| DC75606 |
Fluoxetine |
Fluoxetine is an antidepressant of the selective serotonin reuptake inhibitor (SSRI) class. It is used for the treatment of major depressive disorder, obsessive–compulsive disorder, bulimia nervosa, panic disorder, and premenstrual dysphoric disorder. |
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| DC75607 |
BMS-P5 free base |
BMS-P5 is a Novel Peptidylarginine Deiminase 4 (PAD4) Inhibitor with pIC50 values in the range of 5-7.5. BMS-P5 Blocks Formation of Neutrophil Extracellular Traps and Delays Progression of Multiple Myeloma. Administration of BMS-P5 to multiple myeloma-bearing mice delays appearance of symptoms and disease progression Targeting PAD4 may be beneficial for treatment of multiple myeloma. |
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| DC75608 |
Verubecestat TFA |
Verubecestat, also known as MK-8931 or SCH 900931, is a potent and selective beta-secretase inhibitor, and BACE1 protein inhibitor or Beta-site APP-cleaving enzyme 1 inhibitor. Verubecestat is a promising novel therapeutic drug candidate in Alzheimer's disease. Verubecestat reduced Aβ cerebral spinal fluids (CSF) levels up to 92% and was well tolerated by patients. |
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| DC75609 |
Amiselimod HCl |
Amiselimod, also known as MT1303, is a potent and selective immunosuppressant and sphingosine 1 phosphate receptor modulator. Amiselimod may be potentially useful for treatment of multiple sclerosis; inflammatory diseases; autoimmune diseases; psoriasis and inflammatory bowel diseases. Amiselimod is currently being developed by Mitsubishi Tanabe Pharma Corporation. |
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| DC75610 |
Emavusertib |
Emavusertib, also known as CA-4948 is a potent IRAK4/FLT3 inhibitor with anti-tumor activity. CA-4948 demonstrated good cellular activity in ABC DLBCL and AML cell lines. CA-4948 demonstrated moderate to high selectivity in a panel of 329 kinases as well as exhibited desirable ADME and PK profiles including good oral bioavailability in mice, rat, and dog and showed >90% tumor growth inhibition in relevant tumor models with excellent correlation with in vivo PD modulation. |
|
| DC75611 |
Fadraciclib free base |
Fadraciclib, also known as CYC065, is an orally bioavailable inhibitor of cyclin dependent kinases 2, 5 and 9 (CDK2/5/9) with potential antineoplastic and chemoprotective activities. CYC065 selectively binds to and inhibits the activity of CDK2, 5 and 9, which leads to inhibition of CDK2, 5 and 9-dependent cellular pathways, downregulation of genes involved in the pro-survival pathway, prevention of the activation of DNA double-strand break repair pathways, and induction of both cell cycle arrest and apoptosis. This inhibits the proliferation of CDK2/5/9-overexpressing tumor cells. In addition, CYC065 protects hematopoietic stem and progenitor cells (HSPCs), prevents myelosuppression, and preserves the function of the bone marrow. |
|
| DC75612 |
CGS20625 |
CGS-20625 is an anxiolytic drug used in scientific research. It has similar effects to benzodiazepine drugs, but is structurally distinct and so is classed as a nonbenzodiazepine anxiolytic. It produces anxiolytic and anticonvulsant effects, but with no sedative effects even at high doses, and no significant muscle relaxant effects. It is orally active in humans, but with relatively low bioavailability. CGS-20625 is a positive allosteric modulator at several GABAA receptors types. Due to its alicyclic moiety potency at γ1 subunit, containing receptor types is more pronounced for CGS-20625 compared to benzodiazepines. γ1 subunits are expressed at higher levels in the central amygdala. |
|
| DC75613 |
EST64454 HCl |
EST64454 is a Highly Soluble σ1 Receptor Antagonist Clinical Candidate for Pain Management. EST64454 shows an outstanding aqueous solubility, which together with its high permeability in Caco-2 cells will allow its classification as a BCS class I compound. It also shows high metabolic stability in all species, linked to an adequate pharmacokinetic profile in rodents, and antinociceptive properties in the capsaicin and partial sciatic nerve ligation models in mice. |
|
| DC75614 |
GTS-21 HCl |
GTS-21, also known as DMBX-A, is a derivative of the natural product anabaseine that acts as a partial agonist at neural nicotinic acetylcholine receptors. It binds to both the α4β2 and α7 subtypes, but activates only the α7 to any significant extent. Both GTS-21 itself and its demethylated active metabolite 4-OH-GTS-21 display nootropic and neuroprotective effects, and GTS-21 is being investigated for the treatment of Alzheimer's disease, nicotine dependence, and, most significantly, for schizophrenia. |
|
| DC75615 |
Verosudil |
Verosudil, also known as AR-12286, is a potent and selective Rho kinase inhibitor. AR-12286 was well tolerated and provided statistically significant reduction in IOP (intraocular pressure) in patients with XFS (exfoliation syndrome) and OHT (ocular hypertension) or XFG (exfoliative glaucoma). This drug may represent an additional therapeutic paradigm for the treatment of XFG. |
|
| DC75616 |
(S,R,S)-AHPC free base |
(S,R,S)-AHPC , also known as also known as MDK7526; VHL Ligand 1; Protein degrader 1, is a potent and selective protein degrader. MDK7526 has CAS#1448297-52-6, its HCl salt has CAS#1448189-80-7. MDK7526 is potential useful for the targeted degradation of the androgen receptor. MDK7526 binds androgen receptor such that androgen receptor is placed in proximity to the ubiquitin ligase to effect degrdn. (and inhibition) of androgen receptor. |
|
| DC75617 |
Asciminib free base |
Asciminib, also known as ABL001, is a potent allosteric inhibitor of BCR-ABL. ABL001 prevents emergence of resistant disease when administered in combination with nilotinib in an in vivo murine model of chronic myeloid leukemia. Cell proliferation studies demonstrate that ABL001 selectively inhibited the growth of CML and Ph+ ALL cells with potencies ranging from 1-10nM range. ABL001 was tested for activity against clinically observed mutations and found to be active in the low nM range. In the KCL-22 mouse xenograft model, ABL001 displayed potent anti-tumor activity with complete tumor regression observed and a clear dose-dependent correlation with pSTAT5 inhibition. |
|
| DC75618 |
Amodiaquine free base |
Amodiaquine (trade names Camoquin, Flavoquine), a 4-aminoquinoline compound related to chloroquine, is used as an antimalarial and anti-inflammatory agent. Amodiaquine has been shown to be more effective than chloroquine in treating chloroquine-resistant Plasmodium falciparum malaria infections and may give more protection than chloroquine when used as weekly prophylaxis. Amodiaquine, like chloroquine, is generally well tolerated. Amodiaquine is a histamine N-methyltransferase inhibitor. It is on the World Health Organization's List of Essential Medicines, the most important medications needed in a basic health system. |
|
| DC75619 |
Bacteriochlorophyll a |
Bacteriochlorophyll a is a Bacteriochlorophyll from Rhodopseudomonas sphaeroides. The compounds of this class strongly absorb light at lambda=770-850 nm. This unique property opens new therapeutic opportunities due to deeper tissue penetration of light, thereby increasing the photodamage for tumor eradication. |
|
| DC75620 |
Benzovindiflupyr |
Benzovindiflupyr is a fungicide. It inhibits mitochondrial complex II, also known as succinate dehydrogenase (SDH; IC50 = 5.2 nM), and mycelial growth of S. sclerotiorum (EC50 = 0.011 µg/ml). Benzovindiflupyr (60 µg/ml) completely protects eggplant leaves from S. sclerotiorum infection. Formulations containing benzovindiflupyr have been used to control various fungal diseases in agriculture. |
|
| DC75621 |
Bisantrene HCl |
Bisantrene, aslo known as CL-216942 and NSC 337766, is topoisomerase II poisons and DNA intercalators. It may be used as model compounds to study P-glycoprotein-mediated multiple drug resistance (MDR1). Bisantrene may be used as a Rac1 inhibitor. Bisantrene intercalates with and disrupts the configuration of DNA, resulting in DNA single-strand breaks, DNA-protein crosslinking, and inhibition of DNA replication. This agent is similar to doxorubicin in activity, but unlike doxorubicin, does not exhibit cardiotoxicity. |
|
| DC75622 |
Enpatoran free base |
Enpatoran, also known as M5049, is a novel potent and selective TLR7/8 inhibitor for treatment of autoimmunity. M5049 showed potent and selective activity in a range of cellular assays for inhibition of TLR7/8 and block synthetic ligands and natural endogenous RNA ligands such as microRNA and Alu RNA. M5049 was found to be potent in vivo as TLR7/8 inhibition efficaciously treated disease in several murine lupus models. M5049 had greater potency in disease models than expected based on its in vitro potency and pharmacokinetic/pharmacodynamic properties. M5049 may be efficacious in treating autoimmunity and has the potential to provide benefit to a variety of patients with varying disease pathogenesis. |
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| DC75623 |
BCI inhibitor |
BCI is an allosteric inhibitor of dual specificity phosphatase (DUSP). BCI specifically inhibits DUSP6 and DUSP1 with EC50s of 13.3 and 8.0 μM in cells, respectively. |
|
| DC75624 |
Selinexor free base |
Selinexor, also known as KPT-330, is an orally bioavailable, potent and selective XPO1/CRM1 Inhibitor. Selinexor is effective in acquired resistance to ibrutinib and synergizes with ibrutinib in chronic lymphocytic leukemia. Selinexor potentiates the antitumor activity of gemcitabine in human pancreatic cancer through inhibition of tumor growth, depletion of the antiapoptotic proteins, and induction of apoptosis. Selinexor has strong activity against primary AML cells while sparing normal stem and progenitor cells. |
|
| DC75625 |
Cetirizine Hydrochloride |
Cetirizine hydrochloride is a potent second-generation histamine H1 antagonist that is effective in the treatment of allergic rhinitis, chronic urticaria, and pollen-induced asthma. Cetirizine hydrochloride is a carboxylated metabolite of hydroxyzine that acts as a selective Histamine H1 receptor inverse agonist. Compared to its parent compound, it shows similar antihistaminic activity, but with greater H1 selectivity and less sedative effects. |
|
| DC75626 |
Amlodipine |
Amlodipine (as besylate, mesylate or maleate) is a medication used to lower blood pressure and prevent chest pain. It belongs to a group of medications known as dihydropyridine-type calcium channel blockers. By widening of blood vessels it lowers blood pressure. In angina, amlodipine increases blood flow to the heart muscle to relieve pain due to angina. |
|
| DC75627 |
LDN-192960 free base |
LDN-192960 is an inhibitor of Haspin and Dual-specificity Tyrosine-regulated Kinase 2 (DYRK2) |
|
| DC75628 |
DFN75624 |
DFN75624 is a dengue viral replication inhibitor. DFN75624 was first reported in patent WO 2018215315 (Janssen Pharmaceuticals). This product has no formal name at the moment. For the convenience of communication, a temporary code name was therefore proposed according to MedKoo Chemical Nomenclature (see web page: https://www.medkoo.com/page/naming). |
|
| DC75629 |
ANT3310 sodium |
ANT3310 is a Novel Broad-Spectrum Serine β‑Lactamase Inhibitor of the Diazabicyclooctane Class, Which Strongly Potentiates Meropenem Activity against Carbapenem-Resistant Enterobacterales and Acinetobacter baumannii. |
|
| DC75630 |
Ivosidenib |
Ivosidenib, also known as AG-120 and RG-120, is an orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1), with potential antineoplastic activity. Ivosidenib specifically inhibits a mutated form of IDH1 in the cytoplasm, which inhibits the formation of the oncometabolite, 2-hydroxyglutarate (2HG). This may lead to both an induction of cellular differentiation and an inhibition of cellular proliferation in IDH1-expressing tumor cells. |
|
| DC75631 |
Dinoprostone |
Dinoprostone, also known as PGE2, Prostaglandin E₂, is a product of arachidonic acid metabolism that binds to EP1, EP2, EP3, & EP4 receptors with high affinity (Kd = 1-10 nM). Involved in vasodilator actions of kinins |
|
| DC75632 |
Cefiderocol free base |
Cefiderocol (free base), also known as S-649266, is a potent siderophore cephalosporin antibiotic with a catechol moiety on the 3-position side chain. S-649266 shows potent in vitro activity against the non-fermenting Gram-negative bacteria Acinetobacter baumannii, Pseudomonas aeruginosa and Stenotrophomonas maltophilia, including MDR strains such as carbapenem-resistant A. baumannii and metallo-β-lactamase-producing P. aeruginosa. S-649266 showed potent in vitro activities against A. baumannii producing carbapenemases such as OXA-type β-lactamases, and P. aeruginosa producing metallo-β-lactamases such as IMP type and VIM type. FDA approved this drug in 11/14/2019 To treat patients with complicated urinary tract infections who have limited or no alternative treatment options |
|
| DC75633 |
AZD1446 tosylate |
AZD1446, also known as TC-6683, is a novel highly selective α4β2 nicotinic acetylcholine receptor agonist for the treatment of cognitive disorders. AZD1446 showed favorable pharmaceutical properties and in vivo efficacy in animal models has been identified as a potential treatment for cognitive deficits associated with psychiatric or neurological conditions and had been evaluated in phase 2 clinical trials as a treatment for Alzheimer's disease. |
|
| DC75634 |
SR-717 lithium |
SR-717 is an agonist of stimulator of interferon genes STING for treating cancer. SR-717 demonstrates broad interspecies and interallelic specificity. SR-717 functions as a direct cyclic guanosine monophosphate-adenosine monophosphate (cGAMP) mimetic that induces the same "closed" conformation of STING. SR-717 displayed antitumor activity; promoted the activation of CD8+ T, natural killer, and dendritic cells in relevant tissues; and facilitated antigen cross-priming. SR-717 also induced the expression of clinically relevant targets, including programmed cell death 1 ligand 1 (PD-L1), in a STING-dependent manner. |
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