at 001

RRx-001 is a potent inhibitor ofglucose 6-phosphate dehydrogenase(G6PD) and with potent antimalarial activity

ICG-001 antagonizes Wnt/β-catenin/TCF-mediated transcription and specifically binds to element-binding protein (CBP) with IC50 of 3 μM, but is not the related transcriptional coactivator p300.

EPI-001 is an androgen receptor N-terminal domain antagonist with IC50 of ～6 μM and a selective PPAR-gamma modulator.

LIT-001 improves social interaction in a mouse model of autism.It is the first nonpeptide oxytocin receptor agonist with EC50 of 55 nM and Ki of 226 nM.

AKI-001 is a potent Aurora kinase inhibitor, which exhibits low nanomolar potency against both Aurora A and Aurora B enzymes, excellent cellular potency (IC50 < 100 nM), and good oral bioavailability. Phenotypic cellular assays show that both Aurora A and Aurora B are inhibited at inhibitor concentrations sufficient to block proliferation. Importantly, the cellular activity translates to potent inhibition of tumor growth in vivo. An oral dose of 5 mg/kg QD is well tolerated and results in near stasis (92% TGI) in an HCT116 mouse xenograft model.

NHLP-001 is an ionizable liposome that can be used to make nanoparticles, often in the form of nanoparticles to deliver mRNA drugs.

LJ-001 shows broad-spectrum activity against virtually all enveloped RNA and DNA viruses. LJ001 inhibits the infection of transmissible gastroenteritis virus (TGEV) and porcine delta coronavirus (PDCoV).

ANEB-001 is an orally active CB1 inhibitor suitable for studies on acute cannabinoid intoxication.

PCLX-001 is a small-molecule compound that acts as an orally active inhibitor of N-myristoyltransferase (NMT), specifically targeting NMT1 and NMT2 with IC50 values of 5 nM and 8 nM, respectively. This compound demonstrates anti-tumor effects and effectively inhibits the early signaling of B-cell receptor (BCR). Consequently, PCLX-001 is a valuable tool for researching B-cell malignancies [1] [2].

SN-001 was reported as a STING inhbiitor, which inhibited the activation of the STING signal pathway and to prevent or treat a STING- mediated disease.

ATX-001, an ionizable cationic lipid, is utilized in the creation of lipid nanoparticles (LNPs) for mRNA delivery [1].

YC-001, an inverse agonist and antagonist of rod opsin, reversibly binds and stabilizes the rod opsin structure. This compound demonstrates protective effects against bright light-induced retinal degeneration in mice, suggesting its research potential for retinal degeneration treatments.

TBAP-001 is a RAF kinase inhibitor, with an IC50 of 62 nM in BRAF V600E kinase assay and an IC50 of 18 nM in Cell-Based Phosho-ERK Assay.

Aldose reductase-IN-1 (AT-001) is a aldose reductase inhibitor (IC50: 28.9 pM).

Dimethylaminomicheliolide HCl has potential anti-inflammatory and anti-tumor activity and inhibits the proliferation of glioblastoma cells by targeting pyruvate kinase 2 (PKM2) and reconnecting aerobic cell populations.

FT001 is a potent, selective and orally available inhibitor of BET Bromodomain with antitumor activity. FT001 inhibited the expression of MYC with the IC50 value of 0.46 μM). FT001 has potent antiproliferative effects against MV-4-11 and demonstrates significant MYC mRNA suppression both in vitro and in vivo.

ICG001 antagonizes Wnt β-catenin TCF-mediated transcription and specifically binds to element-binding protein (CREB)-binding protein (CBP) with IC50 of 3 μM, but is not the related transcriptional coactivator p300.

DJ001 is a highly specific, selective, and non-competitive protein tyrosine phosphatase σ (PTPσ) inhibitor with an IC50 of 1.43 μM, and it promotes the regeneration of hematopoietic stem cells.

NB001 (HTS 09836) is an adenyl cyclase 1 inhibitor that affects both neural and non-neural pain.

AH 001 is an agonist of synthetic melatoninergic.

RP-001 hydrochloride is a selective agonist of picomolar short-acting S1P1 (EDG1)(EC50 of 9 pM), has little activity on S1P2-S1P4 and only moderate affinity for S1P5.

KL 001 is a Cryptochrome protein (CRY) stabilizer. KL001 prevented ubiquitin-dependent degradation of CRY, resulting in lengthening of the circadian period. KL001-mediated CRY stabilization inhibited glucagon-induced gluconeogenesis in primary hepatocytes. KL001 thus provides a tool to study the regulation of CRY-dependent physiology and aid development of clock-based therapeutics of diabetes.

AVX-001, a cytosolic phospholipase A2 (cPLA2) inhibitor, is used potentially for the treatment of psoriasis.

MD001 is a dual agonist of peroxisome proliferator-activated receptor α (PPARα) and PPARγ.1 It binds to PPARα and PPARγ (Kds = 9.55 and 0.14 μM, respectively) but does not bind to PPARβ/δ at concentrations up to 500 μM. It increases transcriptional activity of PPARα and PPARγ in a cell-based luciferase reporter assay when used at a concentration of 10 μM. MD001 (10 μM) increases expression of PPARα, PPARγ, and retinoid X receptor (RXR), as well as PPARα and PPARγ target genes, in HepG2 cells. It increases glucose consumption as well as expression of GLUT2 and GLUT4 in HepG2 and 3T3-L1 cells, respectively, in a concentration-dependent manner. MD001 (20 mg/kg) decreases levels of glucose, insulin, free fatty acids, triglycerides, LDL, alanine aminotransferase (ALT), and aspartate aminotransferase (AST) in blood and reduces the size and number of hepatic lipid droplets in diabetic db/db mice.References1. Kim, S.-H., Hong, S.H., Park, Y.-J., et al. MD001, a novel peroxisome proliferator-activated receptor α/γ agonist, improves glucose and lipid metabolism. Sci. Rep. 9(1), 1656 (2019). MD001 is a dual agonist of peroxisome proliferator-activated receptor α (PPARα) and PPARγ.1 It binds to PPARα and PPARγ (Kds = 9.55 and 0.14 μM, respectively) but does not bind to PPARβ/δ at concentrations up to 500 μM. It increases transcriptional activity of PPARα and PPARγ in a cell-based luciferase reporter assay when used at a concentration of 10 μM. MD001 (10 μM) increases expression of PPARα, PPARγ, and retinoid X receptor (RXR), as well as PPARα and PPARγ target genes, in HepG2 cells. It increases glucose consumption as well as expression of GLUT2 and GLUT4 in HepG2 and 3T3-L1 cells, respectively, in a concentration-dependent manner. MD001 (20 mg/kg) decreases levels of glucose, insulin, free fatty acids, triglycerides, LDL, alanine aminotransferase (ALT), and aspartate aminotransferase (AST) in blood and reduces the size and number of hepatic lipid droplets in diabetic db/db mice. References1. Kim, S.-H., Hong, S.H., Park, Y.-J., et al. MD001, a novel peroxisome proliferator-activated receptor α/γ agonist, improves glucose and lipid metabolism. Sci. Rep. 9(1), 1656 (2019).

AKP-001 is a novel inhibitor of p38 MAPK.

JT001 (NLRP3-IN-19) sodium is a potent, specific, and orally active NLRP3 inhibitor that impedes NLRP3 inflammasome assembly, curbing cytokine release and averting pyroptosis. It is utilized in research focused on nonalcoholic steatohepatitis and liver fibrosis [1].

LIT-001 free base improves social interaction in a mouse model of autism. LIT-001 free base is the first nonpeptide oxytocin receptor (OT-R) agonist (EC50=55 nM; Ki=226 nM).

NPD-001 is an effective inhibitor of TbrPDEB1. NPD-001 is 10-fold more potent on hPDE4 (hPDE4B1 IC50 = 0.6 nM) than on TbrPDEB1 (IC50 = 4 nM).

IMMH001, also known as SYL930, is an orally active compound that exhibits potent selectivity as an agonist for the S1P1 receptor, which is the sphingosine-1-phosphate receptor 1. This compound effectively reduces the levels of various chemokines and proinflammatory cytokines, such as IL-1β, IL-5, IL-18, IP10, CCL3, and CCL5. IMMH001 finds utility in research focused on rheumatoid arthritis (RA) [1] [2].

Relatlimab(BMS-986016) is a monoclonal antibody targeting human anti-LAG-3, generated by immunization of transgenic mice with human immunoglobulin carrying recombinant LAG-3 protein.Relatlimab has a blocking effect, blocking the interaction of LAG-3 MHC II (IC50: 0.67 nM) and LAG-3 FGL1 (IC50: 0.019 nM). Relatlimab is often used with Nivoluma to treat advanced melanoma.

CIAC001, a pyruvate kinase PKM2 inhibitor, exhibits anti-neuroinflammatory properties. It effectively suppresses LPS-induced production of proinflammatory nitric oxide (NO) and provides protection to immunologically active BV-2 cells with an IC50 value of 2.5 μM. Additionally, CIAC001 demonstrates anti-neuroinflammation effects in mouse models and attenuates chronic morphine-induced addiction [1].

RP-001 is a selective agonist of picomolar short-acting S1P1 (EDG1)(EC50 of 9 pM), has little activity on S1P2-S1P4 and only moderate affinity for S1P5.

BMX-001 is a third-generation, cationic, lipophilic, manganese (Mn), and porphyrin-based mimetic of the human mitochondrial manganese superoxide dismutase (MnSOD). It also has antioxidant and potential chemoprotective activities.

TNM001 is a fully human monoclonal antibody to RSV for the study of lower respiratory tract diseases due to RSV infection.

ICI 215,001 hydrochloride acts as an antagonist at β1 and β2 adrenergic receptors when it has low intrinsic agonist activity.

MBRI-001 is a deuterium-substituted plinabulin derivative and a potent anti-cancer agent with better pharmacokinetic characteristics tand lower toxicity.

EAI001 is a potent and selective mutant epidermal growth factor receptor (EGFR) variant inhibitor that inhibits EGFRL858R/T790M with an IC50 value of 24 nM.EAI001 can be used in cancer research.

RO320-2947/001 is a bioactive chemical.

Compound N001-0004 is a useful organic compound for research related to life sciences and the catalog number is T131388.

ODN BW001, an oligodeoxynucleotide (ODN), regulates the proliferation and activation of osteoblasts [1] [2].

BCH001 is a specific small-molecule inhibitor of PAPD5.

ALK-001 is a vitamin A analog, which may be used to treat Stargardt disease.

Retro-2 cycl is a dihydroquinazolinone (DHQZ) retrograde trafficking inhibitor. Retro-2 cycl (RN 1-001) inhibits JCPyV and HPV16 pseudovirus(IC50s of 54 μM and 160 μM, respectively),with antiviral agent.

Wnt signaling is required for direct multiple biological processes and also plays key roles in the pathogenesis of various diseases. Cyclic AMP response element-binding protein (CREB) is a transcription factor that is a member of the leucine zipper family of DNA binding proteins. This protein binds as a homodimer to the cAMP-responsive element, an octameric palindrome. The protein is phosphorylated by several protein kinases, and induces transcription of genes in response to hormonal stimulation of the cAMP pathway. Via generating a transcriptionally active complex with β-catenin, CREB acts as a mediator of Wnt signaling.ICG-001 is an inhibitor of β-catenin/CREB mediated transcription. The direct cellular target of ICG-001 is CREB. the inhibitory IC50of ICG-001 against β-catenin/CREB mediated transcription was 3 μM. ICG-001 treatment at the concentration of 25 μM for 24h significantly increased caspase activity in both colon cancer cell lines SW480 and HCT116 cell lines but not in normal colonic epithelial cells CCD-841Co. In a cell growth inhibition assay, the IC50s of ICG-001 against SW480 and HCT116 cells were 4.43 μM and 5.95 μM, respectively.In a SW620 nude mouse xenograft model, an water-soluble analog of ICG-001 given at the dose of 150 mg/kg i.v. once in every 2 days dramatically suppressed tumor growth. In a bleomycin-induced pulmonary fibrosis mice model, ICG-001 given at the dose of 5 mg/kg per day reversed pulmonary fibrosis. In a rat myocardial infarction model, ICG-001 was administrated subcutaneously at the dose of 50 mg/kg/day for 10 days which significantly improved cardiac contractile function after myocardial infarction in the rats.