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61

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T3626	Acalabrutinib ACP-196,阿可替尼	BTK	Angiogenesis; Tyrosine Kinase/Adaptors
	Acalabrutinib (ACP-196) 是一种不可逆的、高效的、具有口服活性、选择性的第二代BTK 抑制剂。它与 BTK 的 ATP 结合口袋中的 Cys481 共价结合。它在慢性淋巴细胞性白血病 (CLL) 小鼠模型中显示出强大的靶向作用和功效。
T15444	GSK962	Others	Others
	GSK962 是 GSK963 的非活性对映异构体，可用于确认靶点作用。
T77191	Clivatuzumab	Others	Others
	Clivatuzumab为人源化抗粘液素单抗，可靶向大部分胰腺癌细胞表面高表达的MUC1表位，对多种肿瘤细胞均有较好的治疗效果。
T9853	STING activator Compound 53	STING	Immunology/Inflammation
	基于 oxindole 核心结构的 STING activator Compound 53 在永生化细胞和原代细胞中表现出强大的 STING（人 EC50 185 nM）的靶向功能激活以及与 STING 激活一致的细胞因子诱导指纹。
T8984	FLTX1	Estrogen Receptor/ERR; Estrogen/progestogen Receptor	Endocrinology/Hormones
	FLTX1 is a fluorescent derivative of Tamoxifen, designed to efficiently target and label intracellular Tamoxifen-binding sites (estrogen receptors) both under permeabilized and non-permeabilized conditions. Additionally, FLTX1 demonstrates strong antiestrogenic activity in breast cancer cells, resembling the potent antiestrogenic properties of Tamoxifen. Notably, FLTX1 does not exhibit any estrogenic agonistic effect on the uterus.
T9127	MYLS22	Others	Others
	MYLS22 是视神经萎缩 1 的选择性抑制剂。它通过影响 NFkB 活性和血管生成基因表达抑制血管生成，靶向作用于内皮细胞 OPA1 ，减少肿瘤的生长。
T67930L	CWI1-2 HCL	Apoptosis	Apoptosis
	CWI1-2 HCL 是一种有效的 IGF2BP2 抑制剂，结合 IGF2BP2 并抑制其与 m6A 修饰的靶转录物的相互作用，可诱导细胞凋亡和分化，具有治疗白血病的作用。
T0520	Lenvatinib 仑伐替尼,E7080	VEGFR; FGFR; c-RET; PDGFR; c-Kit	Angiogenesis; Apoptosis; Tyrosine Kinase/Adaptors
	Lenvatinib (E7080) 是一种多靶点受体酪氨酸激酶抑制剂，抑制 VEGFR1-3、FGFR1-4、KIT、PDGFR 和 RET 等，具有口服活性。Lenvatinib 对 VEGFR2 和 VEGFR3 的抑制活性最强 (IC50=4/5.2 nM)。Lenvatinib 具有强效抗肿瘤活性。
T17870	cIAP1 ligand 1 E3 ligase Ligand 12	Others	Others
	cIAP1 ligand 1 (E3 ligase Ligand 12) 是基于 LCL161 衍生物的细胞凋亡蛋白配体，可募集 IAP 泛素连接酶以降解靶蛋白，可用于和雄激素受体配体偶联开发蛋白降解剂，可用于研究前列腺癌。
T12831L	SAR405	PI3K; Autophagy	Autophagy; PI3K/Akt/mTOR signaling
	SAR-405 是一种选择性 PIK3C3/Vps34 抑制剂，IC50为1.2 nM，Kd 为1.5 nM，可防止自噬并与肿瘤细胞中的 MTOR 抑制协同作用。它抑制饥饿或 mTOR 抑制诱导的自噬，具有抗癌活性。
T36083	DS-7423	PI3K; mTOR	PI3K/Akt/mTOR signaling
	DS-7423 是PI3K 和mTOR 的有效抑制剂，抑制PI3Kα 和 mTOR 的IC50分别为15.6 nM 和 34.9 nM。DS-7423表现出抗癌活性。
T20658	Etofenprox
	Etofenprox, a synthetic pyrethroid, has insecticidal efficacy against mosquito larvae & on non-target organisms.
T69777	DKFZ-251
	DKFZ-251 is a potent inhibitor of kallikrein-related peptidase 6 with on-target cellular activity. DKFZ-251 demonstrated good selectivity for KLK6 compared to other KLKs, and on-target activity in a cellular assay.
T71197	JW-7-25-1
	JW-7-25-1 is a potent multi-target inhibitor, acting on MELK, PIK3CA, mTOR, GSK3A and CDK7.
T19989	Imazamethabenz Imazamethabenz-methyl,Assert,HSDB 6675,Dagger
	Imazamethabenz is a herbicide. Imazamethabenz-methyl is used on cereals and sunflowers, especially against wild oat. Activity and selectivity are due to differential de-esterification to the active parent acid in target and crop species.
T76881	Teclistamab
	Teclistamab 是一种人源化的 BCMA 和 CD3双特异性抗体，可识别靶细胞上的 BCMA 和 T 细胞上的 CD3，诱导 T 细胞介导的细胞毒性，导致 T 细胞的活化和随后的靶细胞裂解。Teclistamab 可用于多发性骨髓瘤等相关疾病研究。
T22860	Imeglimin	Others	Others
	Imeglimin is the first in a new tetrahydrotriazine-containing class of oral antidiabetic agents. It has been shown to act on the liver, muscle, and pancreatic β-cells to uniquely target the key defects of type 2 diabetes.
T14105	Acid-PEG4-C2-Boc	Others	Others
	Acid-PEG4-C2-Boc is a linker compound based on polyethylene glycol (PEG) and alkyl/ether. It is utilized in the synthesis of PROteolysis TArgeting Chimeras (PROTACs) for the purpose of inhibiting the mechanistic Target of Rapamycin (mTOR)[1].
T16578	PRN694	Others	Others
	PRN694 shows extended target residence time on ITK and RLK, enabling durable attenuation of effector cells in vitro and in vivo. PRN694 is an irreversible, highly selective, and effective covalent interleukin-2-inducible T-cell kinase (ITK) and resting ly
T26817	Bim-BLK-A Bim Blocker A,Compound A,Bim BLK A,BimBLKA
	Bim-BLK-A efficiently blocks Bim-induced apoptosis after Bax is activated on the mitochondria. The cellular target of Bim-BLK-A was identified to be the succinate dehydrogenase subunit B (SDHB) protein of complex II of the mitochondrial electron transfer
T77012	Flotetuzumab
	Flotetuzumab (MGD006; S80880) 是一种双特异性 CD123/CD3双亲和再靶向 (DART) 抗体。Flotetuzumab 通过同时结合靶细胞的 CD123和效应 T 细胞的CD3，而重新激活 T 细胞，导致 T 细胞介导的靶细胞的细胞毒性。Flotetuzumab 对小鼠中急性髓系白血病 (AML) 患者来源异种移植物 (PDX) 模型具有抑制效力。
T78412	Biotin-NH-PSMA-617
	Biotin-NH-PSMA-617为标记有生物素的PSMA-617小分子，专门针对前列腺特异性膜抗原（PSMA），后者为肿瘤细胞所特有表达。
T38674	yGsy2p-IN-H23 yGsy2p-IN-H23
	yGsy2p-IN-H23 is a potent, first-in-class inhibitor specifically designed to target yeast glycogen synthase 2 (yGsy2p). It demonstrates an IC50 value of 875 μM for human glycogen synthase 1 (hGYS1). This compound binds precisely within the uridine diphosphate glucose (UDPG) binding pocket of yGsy2p. Its utilization in research primarily focuses on studying glycogen storage diseases (GSDs).
T70886	PT-S58
	PT-S58 is a PPAR β/δ full antagonist, and a derivative of GSK0660. PT-S58 has a three-fold higher affinity for the receptor than GSK0660 and is a potent inhibitor of agonist-induced target gene expression. PT-S58 are effective on PPRE-independent functions of PPARβ/δ. Unlike GSK0660, PT-S58 blocks the recruitment co-repressor molecules such as SMRT.
T39346	PQR626 PQR626
	PQR626 is a rapamycin derivative that acts as a highly potent, selective, orally active, and brain-penetrant mTOR inhibitor. It exhibits remarkable inhibitory effects on the mammalian target of the rapamycin (mTOR) pathway, with an IC50 value of 5 nM and a Ki value of 3.6 nM. This compound, PQR626, holds promise for advancing research in the field of neurological disorders.
T69056	Albizziin
	Albizziin is amino acid analog which acts as a competitive inhibitor of asparagine synthetase with respect to glutamine. Albizziin has been used to isolate mutants of Chinese hamster ovary cells with alterations in levels of the target enzyme. Several classes of mutations can be distinguished on the basis of cross-resistance to beta-aspartyl hydroxamate, another amino acid analog. Studies on asparagine synthetase indicate that resistance to albizziin may be due to altered regulation of asparagin...
T76751	Lenzilumab
	Lenzilumab (KB 003) 是一种靶向CSF2/GM-CSF 的人源化单克隆抗体，可用于 COVID-19、慢性粒单核细胞白血病 (CMML) 和幼年粒单核细胞白血病 (JMML) 研究。
T79524	JPC0323	5-HT Receptor	GPCR/G Protein; Neuroscience
	JPC0323为双5-HT2C/5-HT2A受体正变构调节剂，具备良好的靶向性、血浆暴露水平及脑部穿透能力，适用于神经系统疾病研究领域。
T38542	H-D-Phe-Pip-Arg-pNA acetate H-D-Phe-Pip-Arg-pNA acetate,S-2238 acetate
	H-D-Phe-Pip-Arg-pNA (S-2238) acetate is a chromogenic substrate designed based on the N-terminal fragment of the A alpha chain of fibrinogen, which is the physiological target of thrombin. As a specific indicator of thrombin activity, H-D-Phe-Pip-Arg-pNA acetate is utilized to quantify. This assay, utilizing H-D-Phe-Pip-Arg-pNA acetate, ensures high sensitivity, accuracy, and ease of execution.
T38303	Apramycin (Nebramycin II)
	Apramycin(Nebramycin II) is an aminoglycoside antibiotic used in veterinary medicine. IC50 value:Target: Apramycin stands out among aminoglycosides for its mechanism of action which is based on blocking translocation and its ability to bind also to the eukaryotic decoding site despite differences in key residues required for apramycin recognition by the bacterial target. The drug binds in the deep groove of the RNA which forms a continuously stacked helix comprising non-canonical C.A and G.A bas...
T81739	Multi-target kinase inhibitor 2	EGFR	Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	Multi-target kinase inhibitor 2 (compound 5K) 作为一种multi-targeted kinase抑制剂，对EGFR、Her2、VEGFR2和CDK2酶表现出强效活性，IC50值在40至204 nM之间。此化合物对包括HepG2、HeLa、MDA-MB-231 和 MCF-7在内的多种细胞系均显示出显著的细胞毒性，其IC50值分别为41、57、51 和 59 μM。此外，Multi-target kinase inhibitor 2 还能诱导HepG2细胞发生周期阻滞和凋亡 (apoptosis)。
T74911	ODN 24987
	ODN 24987，一种鸟嘌呤修饰的抑制性寡核苷酸（ODN），作用于TLR9，能够抑制IL-6和IFN-α的释放，适用于免疫紊乱研究。ODN 24987 序列为5’-C-C-T-G-G-C-c7G-G-G-G-3’。
T68324	KCN1
	KCN1, a novel synthetic sulfonamide, is a HIF pathway inhibitor with potential anticancer activity in vitro and in vivo anti-pancreatic cancer activities and preclinical pharmacology. KCN1 specifically inhibited HIF reporter gene activity in several glioma cell lines at the nanomolar level. KCN1 also downregulated transcription of endogenous HIF-1 target genes, such as VEGF, Glut-1, and carbonic anhydrase 9, in a hypoxia-responsive element (HRE)-dependent manner. KCN1 potently inhibited the grow...
T14144	AGN-195183	Others	Others
	AGN 195183 is a potent and selective agonist of RARα(Kd=3 nM) with improved binding selectivity relative to AGN 193836; no activity on RARβ/γ. IC50 value: 3 nM (Kd); 200 nM (EC80, RAR Trans.) Target: RARα agonist Compound 4(AGN-195183) inhibited the growt
T72244	CBB1007 trihydrochloride
	CBB1007三盐酸盐是 LSD1选择性抑制剂，IC50值为5.27uM。
T76880	Tepoditamab
	Tepoditamab (MCLA-117) 是一种双特异性的单克隆抗体，可以与骨髓细胞的 CLEC12A 和细胞毒性 T 细胞的 CD3结合。其中，CLEC12A 是一种骨髓分化抗原。Tepoditamab (MCLA-117) 可以杀死 AML 白血病母细胞和 AML 白血病干细胞，诱导 T 细胞介导的急性髓细胞增殖裂解，可用于急性骨髓性白血病（AML）研究。
T75324	Azidocillin
	Azidocillin 是一种半合成青霉素，是一种具有口服活性的 β-内酰胺类抗生素 (antibiotic)。Azidocillin 具有叠氮化功能，并在细菌内 (bacteria) 保持靶向活性。Azidocillin 可用于研究牙科手术引起的骨炎，或中耳炎、肠球菌败血症和其他细菌感染性疾病。
T63605	AG6033
	AG6033 是潜在的新型 CRBN 调节剂。AG6033 能够调控CRBN 与多种抗肿瘤靶蛋白的相互作用，对多种肿瘤细胞表现出抑制作用。AG6033 能够降解 GSPT1 和 IKZF1，并诱导 CRBN 依赖的细胞毒性作用。
T61811	GPVI antagonist 3
	GPVI antagonist 3 (Compound 2) is a potential antagonist that shows promising antiplatelet activity by selectively inhibiting the interaction between the Glycoprotein VI (GPVI) receptor and its ligands. It demonstrates potent inhibitory effects, with IC50 values of 1.01 μM for collagen, 1.92 μM for CRP, 7.24 μM for convulxin, and 51.74 μM for thrombin. GPVI is a major collagen receptor on platelets, making it an ideal target for safe and effective antithrombotic treatment. Therefore, GPVI antago...
T64171	LXR antagonist 2
	LXR antagonist 2 (compound 10rr) 是一种有效的 LXR (肝 X 受体) 反向激动剂，能够作用于 LXRβ (IC50: 0.36 μM) 和 LXRα (IC50: 2.25 μM)。 LXR antagonist 2 是一种脂肪生成抑制剂，能够下调 LXR 靶基因 SREBP-1c、ACC、FAS 和 SCD-1。LXR antagonist 2 对 Triton WR-1339 诱导的高脂血症小鼠表现出降脂活性。
T14215	AMG 837 sodium salt	Others	Others
	AMG 837 sodium salt is a potent GPR40 agonist(EC50=13 nM) with a superior pharmacokinetic profile and robust glucose-dependent stimulation of insulin secretion in rodents. IC50 value: 13 nM (EC50) [1] Target: GPR40 agonist AMG 837 displayed the expected t
T14382	AZD7687	Others	Others
	AZD7687 is a potent and selective DGAT1 inhibitor with an IC50 value of 80 nM (hDGAT1). IC50 value: 80 nM [1] Target: DGAT1 in vitro: Plasma AZD7687 exposure was measured repeatedly. AZD7687 markedly reduced postprandial TAG excursion with a steep concent
T63991	BRD4/CK2-IN-1
	BRD4/CK2-IN-1 是高效的、口服具有活力的 BRD4/CK2 (含溴结构域蛋白 4/酪蛋白激酶 2) 双靶点抑制剂，能够作用于 BRD4 (IC50: 180 nM) 和 CK2 (IC50: 230 nM)。在三阴性乳腺癌 (TNBC) 中，BRD4/CK2-IN-1 能够诱导细胞凋亡和自噬相关的细胞死亡。BRD4/CK2-IN-1 表现出显著的抗癌效果，且没有明显毒性。
T14614	Biperiden Hydrochloride KL 373 (Hydrochloride),盐酸比哌立登	Others	Others
	Biperiden Hydrochloride (KL 373 Hydrochloride) is an antiparkinsonian agent, which is the selective central M1 cholinoreceptors blocker and it is used for the adjunctive treatment of all forms of Parkinson's disease (postencephalitic, idiopathic, and arte
T69671	SR1903 TFA
	SR-1903 is a modulator of retinoic acid receptor-related orphan receptor γ (RORγ) and liver X receptor (LXR). It is an inverse agonist of RORγ and an agonist of LXR. It also binds to peroxisome proliferator-activated receptor γ (PPAR) but does not activate it. SR-1903 inhibits LPS-induced expression of triggering receptor expressed on myeloid cells 1 (TREM-1). It also inhibits LPS-induced expression of the LXR target genes IL-6 and IL-33 and increases expression of ABCG1, FASN, and SCD-1. SR-190...
T76008	Protein Kinase C (19-31) (TFA)
	Protein Kinase C (19-31) TFA 是蛋白激酶 C (PKC)的抑制剂,是由 PKCa (残基 19-31) 伪底物调控域衍生而来，25 位丝氨酸取代野生型丙氨酸作为蛋白激酶 C 底物肽，用于检测蛋白激酶 C 的活性。Protein kinase C (PKC) TFA 通过磷酸化丝氨酸和苏氨酸氨基酸残基上的羟基来调控其它蛋白的功能。
T71534	CIA-1 hcl(452087-38-6 Free base)	Gamma-secretase	Neuroscience; Proteases/Proteasome; Stem Cells
	CIA-1对核受体COUP-TFII 具有抑制作用，在前列腺癌细胞系中IC50范围从1.2μM 到7.6μM 之间。CIA-1在体外抑制多种前列腺癌细胞系的生长并抑制COUP-TFII 活性以调节其靶基因。CIA-1在体内对前列腺癌异种移植小鼠模型中的肿瘤生长具有抑制作用。
T77038	Interferon alfa
	Interferon alfa 是 I 型干扰素，可激活新基因，对靶细胞产生有效抗病毒和抗增殖活性。Interferon alfa 的信号传导需要 Stat1和 Stat2 的受体依赖性激活，形成异源二聚化 STAT。STAT 复合物与 DNA 结合蛋白 IRF-9 (p48) 结合并形成 ISGF-3 (IFN 刺激基因因子 3)。随后由 ISGF-3 进一步激活驱动基因，实现抗病毒功能。
T9644	Triciferol
	Triciferol 作为具有结合了 VDR 激动剂和 HDAC 拮抗剂活性的多重配体发挥作用。Triciferol 直接与 VDR 结合 (IC50=87 nM)，在一些 1,25D 靶基因上作为具有 1,25D 样效力的激动剂发挥作用。Triciferol 诱导显著的微管蛋白高乙酰化，并增强组蛋白乙酰化。Triciferol 在体外癌细胞模型中也表现出有效的抗增殖和细胞毒性活性。
T80919	Tumour-associated MUC1 epitope
	Tumour-associated MUC1 epitope是一种具有标志性的生物活性肽。作为高度糖基化的I型跨膜糖蛋白MUC1的一部分，该肽通过特定的胞外结构域展现，该结构域包含20个氨基酸组成的可变数量串联重复序列(VNTR)。在多种人类腺癌及血液恶性肿瘤（如多发性骨髓瘤和B细胞淋巴瘤）中细胞表面表达过量，因此，MUC1是许多免疫治疗策略的关键靶点。

化合物

Cat.No: T3626

Synonym: ACP-196,阿可替尼

Target: BTK

Cat.No: T15444

Target: Others

Cat.No: T77191

Target: Others

STING activator Compound 53

Cat.No: T9853

Target: STING

Cat.No: T8984

Target: Estrogen Receptor/ERR, Estrogen/progestogen Receptor

Cat.No: T9127

Target: Others

Cat.No: T67930L

Target: Apoptosis

Cat.No: T0520

Synonym: 仑伐替尼,E7080

Target: VEGFR, FGFR, c-RET, PDGFR, c-Kit

Cat.No: T17870

Synonym: E3 ligase Ligand 12

Target: Others

Cat.No: T12831L

Target: PI3K, Autophagy

Cat.No: T36083

Target: PI3K, mTOR

Cat.No: T20658

Cat.No: T69777

Cat.No: T71197

Cat.No: T19989

Synonym: Imazamethabenz-methyl,Assert,HSDB 6675,Dagger

Cat.No: T76881

Cat.No: T22860

Target: Others

Acid-PEG4-C2-Boc

Cat.No: T14105

Target: Others

Cat.No: T16578

Target: Others

Cat.No: T26817

Synonym: Bim Blocker A,Compound A,Bim BLK A,BimBLKA

Cat.No: T77012

Biotin-NH-PSMA-617

Cat.No: T78412

Cat.No: T38674

Synonym: yGsy2p-IN-H23

Cat.No: T70886

Cat.No: T39346

Synonym: PQR626

Cat.No: T69056

Cat.No: T76751

Cat.No: T79524

Target: 5-HT Receptor

H-D-Phe-Pip-Arg-pNA acetate

Cat.No: T38542

Synonym: H-D-Phe-Pip-Arg-pNA acetate,S-2238 acetate

Apramycin (Nebramycin II)

Cat.No: T38303

Multi-target kinase inhibitor 2

Cat.No: T81739

Target: EGFR

Cat.No: T74911

Cat.No: T68324

Cat.No: T14144

Target: Others

CBB1007 trihydrochloride

Cat.No: T72244

Cat.No: T76880

Cat.No: T75324

Cat.No: T63605

GPVI antagonist 3

Cat.No: T61811

LXR antagonist 2

Cat.No: T64171

AMG 837 sodium salt

Cat.No: T14215

Target: Others

Cat.No: T14382

Target: Others

Cat.No: T63991

Biperiden Hydrochloride

Cat.No: T14614

Synonym: KL 373 (Hydrochloride),盐酸比哌立登

Target: Others

Cat.No: T69671

Protein Kinase C (19-31) (TFA)

Cat.No: T76008

CIA-1 hcl(452087-38-6 Free base)

Cat.No: T71534

Target: Gamma-secretase

Interferon alfa

Cat.No: T77038

Cat.No: T9644

Tumour-associated MUC1 epitope

Cat.No: T80919

Cat. No.	Product Name	Target	Signaling Pathways
TN5369	Dehydroleucodine Dehydroleucodin
	Dehydroleucodine has antidiarrheal, anti-inflammatory, anti-microbial, embryotoxicity, gastric cytoprotective, anti-cancer activities. Dehydroleucodine has an important inhibitory effect in cellular pathways regulating adipocyte differentiation by modulat
T73402	Flavipin
	Flavipin 是一种芳香烃受体(Ahr)激动剂，可诱导小鼠 CD4+T 细胞和 CD11b+巨噬细胞表达 Ahr 下游基因。Flavipin 抑制 Arid5a 在 Il23a3'UTR 上的稳定功能，这是一种新发现的靶 mRNA。Flavipin 具有清除 DPPH 自由基的能力，IC50值为7.2 μM，对α-葡萄糖苷酶具有较强的抑制作用，IC50值为 33.8 μM。

天然产物

Dehydroleucodine

Cat.No: TN5369

Synonym: Dehydroleucodin

Cat.No: T73402

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