at 001

AKP-001 is a novel inhibitor of p38 MAPK.

RRx-001 是一种低氧选择性的表观遗传因子，被用作放射或化疗敏感剂，能诱发凋亡，克服骨髓瘤的耐药性。它是G6PD 的有效抑制剂，具有抗疟、抗癌活性。它是免疫检查点的抑制剂，可下调CD47和SIRP-α。

ICG001 是β-catenin/TCF 介导的一种转录抑制剂，选择性地阻断 β-catenin/CBP 相互作用而不干扰 β-catenin/p300 相互作用。它可特异性结合 CREB 蛋白，IC50为3 μM。

EPI-001 是一种选择性雄激素受体 (AR) 的抑制剂，靶向 AR 的反式激活单元 5，可抑制 AR 氨基末端结构域的反式激活，IC50值约为 6 μM。它也是一种选择性的PPARγ调节剂，对去势抵抗性前列腺癌具有活性。

SN-001 是一种 STING 抑制剂，可抑制 STING 信号通路的激活并预防或治疗 STING 介导的疾病。

LIT-001 是非肽类催产素受体激动剂，EC50为55 nM，Ki 为226 nM。它可改善孤独症小鼠模型的社交互动。

TBAP-001是RAF 激酶的泛抑制剂，IC50为 62 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 是一种可电离脂质体，可用于制作纳米颗粒，常以纳米颗粒的形式传送 mRNA 药物。

LJ-001 显示出对几乎所有包膜 RNA 和 DNA 病毒的广谱活性。 LJ001 抑制传染性胃肠炎病毒 (TGEV) 和猪 delta 冠状病毒 (PDCoV) 的感染。

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.

AH 001 is an agonist of synthetic melatoninergic.

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

CNB-001 是一种高效的 5-lipoxygenase (5-LOX) 抑制剂，能够降低 5-LOX 的表达并提升蛋白酶体活性。此外，CNB-001 在阿尔茨海默病转基因小鼠中可增加 eIF2α 的磷酸化以及 HSP90 和 ATF4 的水平，抑制可溶性 Aβ 和泛素化聚集蛋白的积累。它能够维持突触相关蛋白的表达并提升记忆能力，是用于阿尔茨海默病研究的重要化合物。

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).

ANEB-001 是一种口服具有活力的 CB1 抑制剂，能够用于急性大麻素中毒的研究。

PCLX-001是一种小分子化合物，它作为N-myristoyltransferase (NMT)的口服活性抑制剂，专门针对NMT1和NMT2，其IC50值分别为5 nM和8 nM。该化合物展示了抗肿瘤效果，并有效抑制B细胞受体(BCR)的早期信号传导。因此，PCLX-001是研究B细胞恶性肿瘤的宝贵工具[1] [2]。

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).

PNB-001是一种口服活性的CCK2选择性配体和拮抗剂，具有抗炎和镇痛活性。

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.

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.

RO320-2947/001 is a bioactive chemical.

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

YC-001 是一种针对杆状视蛋白的反向激动剂和拮抗剂。它能与视杆视蛋白可逆地结合，从而稳定其结构，保护小鼠免受强光诱导的视网膜变性，显示出研究视网膜变性疾病潜力。

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

ATX-001，一种可电离的阳离子脂质，适用于形成脂质纳米颗粒（LNP），用于mRNA递送。

Aldose reductase-IN-1 (AT-001)是醛糖还原酶的高效抑制剂, IC50=为28.9 pM。

Dimethylaminomicheliolide HCl 具有潜在的抗炎和抗肿瘤活性，通过靶向丙酮酸激酶 2 （PKM2） 和重新连接有氧细胞群来抑制胶质母细胞瘤细胞的增殖。

FT001是一种有效的、选择性的和具有口服活性的 BET Bromodomain 抑制剂，具有抗肿瘤活性。FT001抑制 MYC 的表达，IC50为0.46 μM。FT001对 MV-4-11具有有效的抗增殖作用，并在体外和体内显著抑制 MYC mRNA 水平。

ICG001 拮抗 Wnt β-catenin TCF 介导的转录，并特异性结合元件结合蛋白(CREB) 结合蛋白 (CBP)，IC50 为 3 μM，但不是相关的转录共激活因子 p300。

DJ001 是一种高度特异性，选择性和非竞争性的蛋白酪氨酸磷酸酶-σ (PTPσ) 抑制剂，IC50 为 1.43 μM。DJ001 对其他磷酸酶无抑制活性，对蛋白质磷酸酶 5 仅有中等抑制活性。DJ001 促进造血干细胞再生。

APX001 is a prodrug of APX-001A. APX001 is the first-in-class inhibitor of the fungal protein Gwt1.

NB001 (HTS 09836) 是腺苷酸环化酶 1 的抑制剂，对神经和非神经疼痛有作用。

mG2N001 是代谢型谷氨酸受体 mGluR2 的负变构调节剂 (NAM) (IC50: 93 nM)，并作为拮抗剂与 mGluR2 结合 (Ki: 63 nM)。mG2N001 具有微粒稳定性和血浆稳定性，其放射性同位素 [11C]mG2N001 可用于 PET 成像。[11C]mG2N001 的脑异质性和脑渗透性好，能够选择性地积累在富含 mGluR2 的区域，产生高对比度的大脑图像。

KL001 是一流的隐花色素蛋白 (CRY)稳定剂，可与 CRY1 和 CRY2 特异性相互作用。其中CRY 是一种对蓝光敏感的黄素蛋白，参与调节动植物的昼夜节律。KL001能够防止泛素依赖性 CRY 降解，从而延长了昼夜节律周期，具有控制空腹激素诱导的糖异生的潜力。

JT001（NLRP3-IN-19）sodium是一种高效、特异的口服NLRP3抑制剂，能够阻断NLRP3炎症小体的聚集，从而抑止细胞因子释放并防止细胞焦亡。此化合物主要应用于非酒精性脂肪肝炎和肝纤维化的研究领域。

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).

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].

CIAC001是一种丙酮酸激酶PKM2的抑制剂，它展现出了抗神经炎症活性。这种化合物能够抑制LPS诱导的一氧化氮(NO)产生(IC50=2.5 μM)，并保护BV-2免疫活性细胞。在小鼠模型中，CIAC001减轻了慢性吗啡引起的成瘾和神经炎症症状。

Relatlimab(BMS-986016) 是一种靶向人抗 LAG-3 的单克隆抗体，由携带重组 LAG-3 蛋白的人免疫球蛋白的转基因小鼠免疫生成。Relatlimb 有阻断作用，可阻断 LAG-3 MHC II 的相互作用（IC50 ： 0.67 nM），阻断了 LAG-3 FGL1 的相互作用（ IC50：0.019 nM）。Relatlimab 常与 Nivoluma 一起用来治疗晚期黑色素瘤。

ACT001 是一种口服有效的 PAI-1抑制剂，主要是通过抑制 PI3K 和 AKT 的磷酸化。ACT001 通过直接与 STAT3结合来抑制 STAT3 的磷酸化和 PD-L1 表达。ACT001 是一种 DMAMCL (Micheliolide 的前药) 的富马酸盐形式，可以透过血脑屏障。ACT001 通过抑制 PAI-1/PI3K/AKT 通路与顺铂产生协同作用。ACT001 具有有效的抗胶质母细胞瘤 (GBM) 活性和免疫调节作用。

ICI 215,001 hydrochloride 在其内在激动剂活性较低的情况下可充当 β1 和 β2 肾上腺素受体的拮抗剂。

EAI001 是一种具有有效性和选择性的突变体表皮生长因子受体 (EGFR) 变构抑制剂，对 EGFRL858R/T790M 有抑制作用， IC50 值为 24 nM。EAI001 可用于研究癌症。

ODN BW001 是一种寡核苷酸。ODN BW001 在成骨细胞增殖和激活中起调节作用。

BCH001 是喹啉衍生物，是一种选择性PAPD5抑制剂。它可以恢复先天性角化病诱导的多能干细胞中的端粒酶活性和端粒长度。它对聚 (A)-特异性核糖核酸酶或几种其他多核苷酸聚合酶均无抑制作用。它可用于调控衰老。

Compound N001-0004 是一种有用的有机化合物，可用于生命科学领域的相关研究，其产品编号为 T131388。

Retro-2 cycl 是一种抗病毒剂，是一种逆行运输抑制剂，抑制 JCPyV（IC50s：54 μM）和 HPV16 假病毒（IC50s：160 μM）。

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.