| DC74850 |
DeBio-1143 (AT-406) |
DeBio-1143, also known as AT-406, ARRY-334543and SM-406, is an orally bioavailable inhibitor of IAP (Inhibitor of Apoptosis Protein) family of proteins with potential apoptotic inducing and antineoplastic activity. AT-406 selectively inhibits the biological activity of IAP proteins, including X chromosome-linked IAP (XIAP), the cellular IAPs 1 (c-IAP1) and 2 (c-IAP2) and melanoma inhibitor of apoptosis protein (ML-IAP). This may restore and promote the induction of apoptosis through apoptotic signaling pathways. AT-406 may work synergistically with cytotoxic drugs to overcome tumor cell resistance to apoptosis. |
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| DC74851 |
CO101244 HCl |
CO-101244, also known as RO-63-1908 and PD-174494, is a novel, potent and selective antagonist of NR2B-containing NMDA receptors (IC50 values are 0.043, > 100 and > 100 μM for NR1A/2B, NR1A/2A and NR1A/2C subunit combinations respectively). CO-101244 displays neuroprotective effects in vivo and in vitro. |
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| DC74852 |
Dov-Val-Dil-OH TFA |
Dov-Val-Dil-OH is a useful chemical intermediate for synthesis of auristatin-related compounds, such as Monomethyl auristatin E (MMAE), Auristatins are antimitotic agents which inhibits cell division by blocking the polymerisation of tubulin. |
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| DC74853 |
CZC-54252 HCl |
CZC-54252 is a potent inhibitor of leucine-rich repeat kinase 2 (LRRK2) with IC50 values 1.28 nM and 1.85 nM for wild-type and G2019S mutant forms of LRRK2 respectively. CZC-54252 attenuates neuronal injury induced by LRRK2-G2019S mutant activity in primary human neurons (EC50 = 1 nM). Activating mutations in leucine-rich repeat kinase 2 (LRRK2) are present in a subset of Parkinson's disease (PD) patients and may represent an attractive therapeutic target. |
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| DC74854 |
HLCL-61 HCl |
HLCL-61 is a potent and selective PRMT5 inhibitor for treatment of acute myeloid leukemia. HLCL-61 resulted in significantly increased expression of miR-29b and consequent suppression of Sp1 and FLT3 in AML (acute myeloid leukemia) cells. As a result, significant antileukemic activity was achieved. The increased PRMT5 activity enhanced AML growth in vitro and in vivo while PRMT5 downregulation reduced it. In AML cells, PRMT5 interacted with Sp1 in a transcription repressor complex and silenced miR-29b preferentially via dimethylation of histone 4 arginine residue H4R3. |
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| DC74855 |
GSK269962 |
GSK269962 is a selective ROCK inhibitor with IC50 values of 1.6 and 6 nM for ROCK-I and ROCK-II, respectively. GSK269962 can become an alternative worth considering in OAB treatment. |
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| DC74856 |
AZD6482 (S-isomer) |
AZD6482 (S-isomer), CAS#1173900-37-2, is an isomer of AZD6482 (MedKoo Cat#406268) with S-configuration. AZD6482 is a potent, selective and ATP competitive PI3Kβ inhibitor (IC(50) 0.01 μm). AZD6482 inhibited insulin-induced human adipocyte glucose uptake in vitro (IC(50) of 4.4 μm). This is the first human target validation for PI3Kβ inhibition as anti-platelet therapy showing a mild and generalized antiplatelet effect attenuating but not completely inhibiting multiple signaling pathways with an impressive separation towards primary hemostasis. AZD6482 at 'supratherapeutic' plasma concentrations may attenuate insulin signaling, most likely through PI3Kα inhibition. |
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| DC74857 |
XI-011 HCl |
XI-011 (NSC146109), a small-molecule inhibitor of MDMX, showed robust anti-proliferation activity against several cervical cancer cell lines. XI-011 promoted apoptosis of cervical cancer cells via stabilizing p53 and activating its transcription activity. Moreover, XI-011 inhibited the growth of xenograft tumor in HeLa tumor-bearing mice, as well as enhanced the cytotoxic activity of cisplatin both in vitro and in vivo. |
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| DC74858 |
SRI-37330 free base |
SRI-37330 is an orally bioavailable, non-toxic small molecule TXNIP inhibitor. SRI-37330 effectively rescued mice from streptozotocin- and obesity-induced (db/db) diabetes. SRI-37330 inhibited expression and signaling of thioredoxin-interacting protein, SRI-37330 treatment inhibited glucagon secretion and function, reduced hepatic glucose production, and reversed hepatic steatosis. Rescue assays confirmed that the impact of FTO on the TXNIP/NLRP3 pathway was significantly reversed by the TXNIP inhibitor SRI-37330. |
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| DC74859 |
BMS-345541 HCl |
BMS 345541 is a selective allosteric inhibitor of IKK (IC50 values are 0.3 and 4.0 μM for IKKβ and IKKα respectively). It attenuates LPS-induced cytokine production in vitro and blocks NFκB dependent transcription in mice. BMS 345541 also suppresses joint destruction in a mouse model of arthritis. |
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| DC74860 |
PXS-5505 free base |
PXS-5505 is a Pan-Lysyl Oxidase Inhibitor that has been found to ameliorate multiple-organ fibrosis by inhibiting collagen crosslinks in rodent models in systemic sclerosis. PXS-5505 inhibited lysyl oxidase activity in the skin and LOXL2 activity in the lung. PXS-5505 exhibited anti-fibrotic effects in the SSc skin mouse model, reducing dermal thickness and α-smooth muscle actin. Similarly, in the bleomycin-induced mouse lung model, PXS-5505 reduced pulmonary fibrosis toward normal levels, mediated by its ability to normalise collagen/elastin crosslink formation. PXS-5505 also reduced fibrotic extent in models of the ischaemia-reperfusion heart, the unilateral ureteral obstruction kidney, and the CCl4-induced fibrotic liver. |
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| DC74861 |
MeIQx |
MeIQx, also known as 8-Methyl-IQX, is a synthetic, pale orange to brown crystalline solid that is soluble in dimethylsulfoxide and methanol. It is produced in small quantities for research purposes. 2-Amino-3,8-dimethylimidazo[4,5-f]quinoxaline is formed naturally during the cooking of muscle-derived foods (meat and fish). Levels of this chemical produced in this manner are dependent on cooking temperature, cooking time and method of cooking (direct or indirect). It is one of the most abundant heterocyclic amines in a typical Western diet. 2-Amino-3,8-dimethylimidazo[4,5-f]quinoxaline has also been detected in processed food flavorings, beer, wine, and cigarette smoke. It is reasonably anticipated to be a human carcinogen. |
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| DC74862 |
HUN78821 |
HUN78821, also known as 7-benzyl-4-(2-methylbenzyl)-1,2,6,7,8,9-hexahydroimidazo[1,2-a]pyrido[3,4-e]pyrimidin-5(4H)-one dihydrochloride is a chemical reagent for research use. It has CAS#1638178-82-1. According to MedKoo Chemical Nomenclaturee (see web page: https://www.medkoo.com/page/naming)., this chemical can be named as HUN78821. |
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| DC74863 |
Ninerafaxstat HCl |
Ninerafaxstat, also known as CV 8972, IMB-1018972 and IMB-101, is a novel mitotropic agent. Ninerafaxstat increases myocardial metabolic efficiency by shifting substrate utilization towards glucose through reducing fatty acid oxidation (inhibiting 3-ketoacyl CoA thiolase). Ninerafaxstat can be used for the research of cardiovascular diseases. |
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| DC74864 |
VUN32779 |
VUN32779, also known as 7-benzyl-4-(2-methylbenzyl)-1,2,6,7,8,9-hexahydroimidazo[1,2-a]pyrido[3,4-e]pyrimidin-5(4H)-one is a chemical reagent for research use. It has CAS#1616632-77-9. According to MedKoo Chemical Nomenclaturee ((see web page: https://www.medkoo.com/page/naming)., this chemical can be named as VUN32779. |
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| DC74865 |
AGI25696-Analog |
AGI25696-Analog is a demethyl analog of AGI-25696, which is a methionine adenosyltransferase 2A (MATA2 ) inhibitor. AGI-25696 is potentially useful for treatment of cancer. AGI-25696 blocks growth of MTAP-deleted tumors in vivo. Note: The correct structure of AGI-25696 is CAS#2201065-84-9. Many vendors mistakenly listed CAS#2201066-35-3 as its AGI25696. J. Med. Chem. 2021, 64, 8, 4430–4449 published AGI25696 structure (it is CAS#2201065-84-9). |
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| DC74866 |
DPPS |
DPPS is a form of phosphatidylserine (PS), an anionic phospholipid. |
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| DC74867 |
Asulacrine free base |
Asulacrine, also known as CI-921; NSC-343499; SN-21407, is a topoisomerase ll inhibitor with antineoplastic properties. Asulacrine inhibits the enzyme topoisomerase ll, thereby blocking DNA replication and RNA and protein synthesis. |
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| DC74868 |
Alectinib HCl |
Alectinib, also known as AF802, or CH5424802 or RO5424802, is a potent, selective, and orally available ALK inhibitor with a unique chemical scaffold, showing preferential antitumor activity against cancers with gene alterations of ALK, such as nonsmall cell lung cancer (NSCLC) cells expressing EML4-ALK fusion and anaplastic large-cell lymphoma (ALCL) cells expressing NPM-ALK fusion in vitro and in vivo. Alectinib inhibited ALK L1196M, which corresponds to the gatekeeper mutation conferring common resistance to kinase inhibitors, and blocked EML4-ALK L1196M-driven cell growth. Alectinib (as HCl salt) was approved in Dec. 2015. |
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| DC74869 |
Pyrilutamide |
Pyrilutamide, also known as KX826, is an androgen receptor (AR) antagonist and a potential first-in-class topical drug for the treatment of androgenetic alopecia (AGA) and acne vulgaris. |
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| DC74870 |
NAN190 free base |
NAN-190 is a mixed antagonist and partial agonist of the serotonin (5-HT) receptor subtype 5-HT1A. NAN-190 potentiates the circadian response to light and speeds re-entrainment to advanced light cycles. NAN-190 potentiates the impairment of retention produced by swim stress. NAN-190 is a possible antagonist for methamphetamine. |
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| DC74871 |
Mebeverine Acid |
Mebeverine acid is a metabolite of the antispasmodic agent mebeverine. |
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| DC74872 |
SKF89976A HCl |
SKF89976A is a potent GABA uptake inhibitor, which is selective for GAT-1 (IC50 values are 0.13, 550, 944 and 7210 μM for hGAT-1, rGAT-2, hGAT-3 and hBGT-1 respectively). SKF89976A inhibits transport current competitively (Ki = 7 μM) and transmitter-gated current non-competitively (Ki = 0.03 nM). It is able to pass the blood-brain barrier after systemic administration and is active in vivo. |
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| DC74873 |
W-9 HCl |
W-9 is a Calmodulin antagonist |
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| DC74874 |
ABT-925 free base |
ABT-925, also known as A-37203, BSF-201640; DAT-201; Lu-201640; and A-437203, is a selective dopamine D3 receptor (DRD3) antagonist with an approximately 100-fold higher in vitro affinity for dopamine D₃ versus D₂ receptors. ABT-925 was tested in schizophrenia. ABT-925 is a selective dopamine D₃ receptor antagonist with an approximately 100-fold higher in vitro affinity for dopamine D₃ versus D₂ receptors. |
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| DC74875 |
Ensitrelvir |
Ensitrelvir, also known as S-217622, is an antiviral drug developed by Shionogi in partnership with Hokkaido University, which acts as an orally active 3C-like protease inhibitor for the treatment of COVID-19 infection. It is taken by mouth, and has been successfully tested against the recently emerged Omicron variant. It is the first orally active non-covalent, non-peptidic, SARS-CoV-2 3CL protease inhibitor (IC50=13 nM). It became the first Japanese domestic pill to treat COVID-19, third to be regulatorally approved in Japan; in February 2022. |
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| DC74876 |
Deuremidevir HBr |
Deuremidevir, also known as VV116, JT001, and mindeudesivir, is a chemically-modified version of the antiviral remdesivir with oral bioavailability and potent activity against SARS-CoV-2. Deuremidevir is a deuterated, tri-isobutyrate ester prodrug of the RDV parent nucleoside, and is rapidly metabolized into the parent nucleoside (116-N1) in the body. 116-N1 is intracellularly converted to the nucleoside triphosphate active form, which would interfere with the function of RNA-dependent RNA polymerase of SARS-CoV-2, thus exerting antiviral effects. Deuremidevir showed potent activity against a panel of SARS-CoV-2 variants (alpha, beta, delta, and omicron) and excellent therapeutic efficacy in the mice model. Note: the non-labeled analog is called GS621763 (Cat#465727). |
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| DC74877 |
Propargylcholine bromide |
Propargylcholine bromide is an alkynyl derivative of choline that has a propargyl group in place of one methyl group. It can be used to assay phospholipid synthesis and localization in cells and tissues using Raman scattering microscopy or click chemistry labeling with fluorescent or affinity-tagged azides. |
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| DC74878 |
TMPH inhibitor |
TMPH is an inhibitor of CNS nicotinic receptor. Evaluation of nicotinic acetylcholine receptor (nAChR) subunits expressed in Xenopus laevis oocytes indicated that TMPH can produce a potent and long-lasting inhibition of neuronal nAChR formed by the pairwise combination of the most abundant neuronal α (i.e., α3 and α4) and β subunits (β2 and β4), with relatively little effect, because of rapid reversibility of inhibition, on muscle-type (α1β1γδ) or α7 receptors. |
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| DC74879 |
GW3965 HCl |
GW-3965 is a liver X receptor agonist. GW3965 represses the production of pro-inflammatory cytokines by murine mast cells. GW3965 improves recovery from mild repetitive traumatic brain injury in mice partly through apolipoprotein E. GW3965 reduces tissue factor production and inflammatory responses in human islets in vitro. GW3965 dose-dependently regulates lps-mediated liver injury and modulates posttranscriptional TNF-alpha production and p38 mitogen-activated protein kinase activation in liver macrophages. |
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