p 58

ACP-5862 is a major active and pyrrolidine ring-opened metabolite of Acalabrutinib (IC50: 5.0 nM for BTK). Acalabrutinib is an irreversible and highly selective BTK inhibitor (IC50: 3 nM; EC50: 8 nM).

PP58 是 PDGFR、FGFR 和 Src 家族的抑制剂。

ASP-5854 is an adenosine A(2A) receptor antagonist with the potential to improve motor deficits in Parkinson's disease.

ASP5878 is an oral bioavailable fibroblast growth factor receptor (FGFR) inhibitor with potential anti-tumor activity.

ASP5878 是一种 FGFR 1 (IC50:0.47 nM)、FGFR 2 (IC50:0.6 nM)、FGFR 3 (IC50:0.74 nM)、和 FGFR 4 (IC50:3.5 nM)的抑制剂，具有口服活性，具有潜在的抗肿瘤作用。

TP-5801 是口服具有活力的非受体酪氨酸激酶 (TNK1) 抑制剂，IC50 值为 1.40 nM，具有抗肿瘤作用。

TP-5801 TFA为口服活性非受体酪氨酸激酶（TNK1）抑制剂（IC50=1.40 nM），展现抗肿瘤活性。

Delmitide acetate (RDP58) 是一种 d-异构体十肽，具有抗炎活性和口服活性。该化合物能够抑制 TNF-α、IFN-γ 以及白细胞介素 (IL)-12 的生成，同时提高血红素加氧酶 1 的活性，可用于针对溃疡性结肠炎的研究。

Antileishmanial agent-2 是一种基于 3-Br-isoxazoline 的疟原虫抑制剂恶性疟原虫（D10 和 W2 菌株）和利什曼原虫属。 (L. infantum 和 L.tropica) 前鞭毛体，IC50 为 0.035、0.058、3.5 和 7.5 μM。

GV-58 是选择性 N 型和 P Q 型 Ca2+ 通道激动剂，EC50值分别为7.21和8.81uM。它对 CDK 激酶活性的抑制作用减少了 20 倍。

WR-S-462 是一种STAT3抑制剂，在体外能有效地阻碍STAT3的磷酸化及其生物学功能。该化合物对MDA-MB-231细胞的IC50为0.03 μM，并表现出对STAT3蛋白的强结合亲和力，其Kd为58 nM。WR-S-462 能抑制p-STAT3的核转位，特异性抑制MDA-MB-231细胞中p-STAT3Tyr705的表达，以及由STAT3调控的下游靶基因如Cyclin D1、Bcl-2和Bcl-xl的表达。此外，WR-S-462 有效抑制三阴性乳腺癌 (TNBC) 的生长和转移。

Beauvericin A is a cyclodepsipeptide and derivative of beauvericin originally isolated fromB. bassianathat has diverse biological activities.1,2,3It is active againstM. tuberculosis(MIC = 25 μg/ml) andP. falciparum(IC50= 12 μg/ml).2Beauvericin A is toxic to brine shrimp (LD100= 32 μg/ml).3 1.Gupta, S., Montillor, C., and Hwang, Y.-S.Isolation of Novel Beauvericin Analogues from the Fungus Beauveria bassianaJ. Nat. Prod.58(5)733-738(1995) 2.Nilanonta, C., Isaka, M., Kittakoop, P., et al.Antimycobacterial and antiplasmodial cyclodepsipeptides from the insect pathogenic fungus Paecilomyces tenuipes BCC 1614Planta Med.66(8)756-758(2000) 3.Shi, S., Li, Y., Ming, Y., et al.Biological activity and chemical composition of the endophytic fungus Fusarium sp. TP-G1 obtained from the root of Dendrobium officinale Kimura et MigoRec. Nat. Prod.12(6)549-556(2018)

Ciprofibrate impurity A is an impurity of Ciprofibrate. Ciprofibrate is a PPARα agonist[1]. [1]. Passilly, P., et al., Phosphorylation of peroxisome proliferator-activated receptor alpha in rat Fao cells and stimulation by ciprofibrate. Biochem Pharmacol, 1999. 58(6): p. 1001-8.

Purfalcamine is an orally active, selective Plasmodium falciparum calcium-dependent protein kinase 1 (PfCDPK1) inhibitor with an IC50 of 17 nM and an EC50 of 230 nM. Purfalcamine has antimalarial activity and causes malaria parasites developmental arrest at the schizont stage[1][2]. Purfalcamine has low activity against Toxoplasma gondii calcium-dependent protein kinase 3 (TgCDPK3)[1]. Purfalcamine (225, 450 nM) has no effect on the parasitemia in the first 32 hours. After about 40 hours, parasite level remains stable and then begins dropping[1]. Purfalcamine inhibits proliferation with EC50s of 171-259 nM for P. falciparum strains (3D7, Dd2, FCB, HB3 and W2), which indicates effectiveness against drug-resistant parasites[1]. Given that the EC50 value for P. falciparum (3D7) is 230 nM, Purfalcamine shows a therapeutic window ranging from 23-fold to 36-fold (EC50s for CHO=12.33 μM, HEp2=7.235 μM, HeLa=7.029 μM and Huh7=5.476 μM)[1]. Purfalcamine (10 mg kg; oral gavage; BID; for 6 days) demonstrates a delay in the onset of parasitemia in treated mice[1]. Purfalcamine (20 mg kg; orally gavage) exhibits a Cmax of 2.6 μM with a half-life of 3.1 hours[1]. Animal Model: Male BALB c mice, 7 weeks of age with the malaria parasite[1] [1]. Nobutaka Kato, et al. Gene expression signatures and small-molecule compounds link a protein kinase to Plasmodium falciparum motility. Nat Chem Biol. 2008 Jun;4(6):347-56. [2]. Rajshekhar Y Gaji, et al. Expression of the essential Kinase PfCDPK1 from Plasmodium falciparum in Toxoplasma gondii facilitates the discovery of novel antimalarial drugs. Antimicrob Agents Chemother. 2014 May;58(5):2598-607.

Substance P-Gly-Lys-Arg，也称为 β-Preprotachykinin (58-71)，是 Substance P (Substance P ) 的类似物。