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15

抑制剂 & 化合物

1

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T61699	Osunprotafib AC 484,Osunprotafib,AC484,ABBV-CLS-484	Phosphatase	Metabolism
	ABBV-CLS-484 (Osunprotafib) 是一种具有亚纳摩尔活性的有效的PTPN2抑制剂，具有抗肿瘤活性，可增强T细胞抗肿瘤免疫力。ABBV-CLS-484可用于治疗肿瘤、食管癌和消化系统疾病。
T17257L	WR99210 hydrochloride(47326-86-3 free base) WR99210 hydrochloride(47326-86-3 free base),6,6-Dimethyl-1-[3-(2,4,5-trichlorophenoxy)propoxy]-1,6-dihydro-1,3,5-triazine-2,4-diamine	Others	Others
	WR99210 hydrochloride 是恶性疟原虫二氢叶酸还原酶 (pfDHFR) 的有效抑制剂，pfDHFR 是主要的疟疾药物靶点。它对野生型、双突变体和四突变体二氢叶酸还原酶具有亚纳摩尔效力。
T13193	TPN171	PDE	Metabolism
	TPN171是一种有效的 PDE5抑制剂，对 PDE5具有亚纳摩尔效价，对 PDE5比对 PDE6具有良好的选择性，具有治疗肺动脉高压(PAH)的潜力。在动物模型中，TPN171被证明具有比西地那非更持久的作用，为临床使用每日一次口服提供了基础。
T24989	85548e 85548 e,85548-e,U 85548e,U85548e,U-85548e
	85548e is used as an inhibitor that exhibiting subnanomolar affinity towards HIV type-1 aspartic proteinase (HIV-1 PR).
T10236	ACHN-975 TFA	Others	Others
	ACHN-975 TFA is a selective LpxC inhibitor with a subnanomolar inhibitory. It is against a wide range of gram-negative bacterias with low MIC values (≤1 μg/mL).
T71875	OM-137
	OM137 is an inhibitor of Aurora kinases. which is growth inhibitory to cultured cells when applied at high concentration and potentiates the growth inhibitory effects of subnanomolar concentrations of paclitaxel.
T24839	Stampidine HI-113,HI 113,HI113
	Stampidine can prevent the sexual transmission of HIV-1. It exhibited remarkable subnanomolar to low nanomolar in vitro antiretroviral potency against nucleoside reverse transcriptase inhibitor-resistant primary clinical HIV isolates, non-nucleoside RT-re
T26642	Aplaviroc hydrochloride AK602,AK 602,GW873140A,GW-873140,GW873140,AK-602,Aplaviroc HCl
	Aplaviroc is a human cellular CC chemokine receptor 5 (CCR5) entry inhibitor. Aplaviroc binds specifically to CCR5 and demonstrates potent anti-human immunodeficiency virus activity in vitro in the subnanomolar range. In vitro studies show that aplaviroc
T28510	REDX05358 REDX 05358,REDX-05358
	REDX05358 is a highly selective and potent pan RAF inhibitor with a potential therapeutic for BRAF and RAS mutant tumors. REDX05358 has improved therapeutic potential and predicted safety profile. REDX05358 demonstrates subnanomolar binding affinity for B
T10236L	ACHN-975	Others	Others
	ACHN-975 is a highly potent and selective LpxC inhibitor, demonstrating subnanomolar inhibitory activity. It effectively targets a broad spectrum of gram-negative bacteria, with low minimum inhibitory concentration (MIC) values (≤1 μg/mL)[1].
T70693	MRT-92 HCl salt
	MRT-92 is a potent and selective Smoothened (Smo) receptor inhibitor. MRT-92 displays subnanomolar antagonist activity against Smo in various Hh cell-based assays. MRT-92 inhibits rodent cerebellar granule cell proliferation induced by Hh pathway activation through pharmacologic (half maximal inhibitory concentration [IC50] = 0.4 nM) or genetic manipulation. Smo is the target of anticancer drugs that bind to a long and narrow cavity in the 7-transmembrane (7TM) domain.
T61827	RJ-34
	RJ-34, an aristolactam analogue, demonstrates strong antitumor effects across a wide range of cancer cell lines, with subnanomolar GI 50 values (GI 50 <0.1 nM) observed for A431, MES-SA, MES-SA/DX5, HCT-15, and HCT-15/CLO2 cells [1].
T36689	KuWal151
	Potent and selective CLK inhibitor (IC50 values are 28, 88 and 510 nM for CLK4, 1 and 2, respectively). Exhibits no significant activity at CLK3, DYRK, CDK or GSK3 at a concentration of 10 μM. Inhibits growth of a range of cancer cell lines in vitro at subnanomolar concentrations. Walter et al (2018) Molecular structures of cdc2-like kinases in complex with a new inhibitor chemotype. PLoS One 13 e0196761 PMID:29723265
T76732	CC-90002
	CC-90002 是一种人源化抗 CD47 单克隆抗体 (mAb)。CC-90002 与 CD47 具有高亲和力，具有亚纳摩尔 Kd 值。CC-90002 可用于血液系统恶性肿瘤和实体瘤的研究。
T71618	Oxocarbazate
	Oxocarbazate, also known as CID23631927, is an inhibitor of human cathepsin L. In the cathepsin L inhibition assay, The oxocarbazate caused a time-dependent 17-fold drop in IC50 from 6.9 nM (no preincubation) to 0.4 nM (4-h preincubation). Slowly reversible inhibition was demonstrated in a dilution assay. CID23631927 demonstrate activity in blocking both SARS-CoV (IC50 = 273 nM) and Ebola virus (IC50 = 193 nM) entry into human embryonic. CID 23631927 was a subnanomolar, slow-binding, reversible...

化合物

Cat.No: T61699

Synonym: AC 484,Osunprotafib,AC484,ABBV-CLS-484

Target: Phosphatase

WR99210 hydrochloride(47326-86-3 free base)

Cat.No: T17257L

Synonym: WR99210 hydrochloride(47326-86-3 free base),6,6-Dimethyl-1-[3-(2,4,5-trichlorophenoxy)propoxy]-1,6-dihydro-1,3,5-triazine-2,4-diamine

Target: Others

Cat.No: T13193

Target: PDE

Cat.No: T24989

Synonym: 85548 e,85548-e,U 85548e,U85548e,U-85548e

Cat.No: T10236

Target: Others

Cat.No: T71875

Cat.No: T24839

Synonym: HI-113,HI 113,HI113

Aplaviroc hydrochloride

Cat.No: T26642

Synonym: AK602,AK 602,GW873140A,GW-873140,GW873140,AK-602,Aplaviroc HCl

Cat.No: T28510

Synonym: REDX 05358,REDX-05358

Cat.No: T10236L

Target: Others

MRT-92 HCl salt

Cat.No: T70693

Cat.No: T61827

Cat.No: T36689

Cat.No: T76732

Cat.No: T71618

Cat. No.	Product Name	Target	Signaling Pathways
T21351	Maytansine NSC-153858,NSC153858,Maitansina,NSC 153858,Maitansine,美坦新	Microtubule Associated; Antibiotic	Cytoskeletal Signaling; Microbiology/Virology
	Maytansine (NSC-153858) 是从变叶美登木中分离的一种高效微管靶向天然产物，可诱导有丝分裂阻滞并在亚纳摩尔浓度杀死肿瘤细胞。

天然产物

Cat.No: T21351

Synonym: NSC-153858,NSC153858,Maitansina,NSC 153858,Maitansine,美坦新

Target: Microtubule Associated, Antibiotic

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