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62

抑制剂 & 化合物

6

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T5210	BAI1	Apoptosis; BCL	Apoptosis
	BAI1 是一种选择性凋亡因子BAX 变构抑制剂。它结合 BAX 并变构抑制其激活，具有潜力研究 BAX 依赖性细胞死亡介导的疾病。
T10826	CK-666	HIV Protease; Microtubule Associated	Cytoskeletal Signaling; Microbiology/Virology; Proteases/Proteasome
	CK-666 是一种肌动蛋白相关蛋白 Arp2/3 复合物的细胞渗透性抑制剂。它与 Arp2/3 复合物结合，稳定复合物的非活性状态，阻止 Arp2 和 Arp3 亚基进入活化的丝状短节距构象。
T19889	L-5-BromoTryptophan L-5-溴色氨酸,5-BrW,5 BrW	Others	Others
	L-5-BromoTryptophan (5-BrW) 是色氨酸(Trp) 效应物的类似物，可抑制血红蛋白 S 的凝胶化。
T20344	Acetylcholine bromide	Others	Others
	Acetylcholine bromide 是乙酰胆碱的溴化物盐。它是一种神经递质，存在于神经肌肉接头、自主神经节、副交感神经效应器接头、交感神经效应器接头的一个子集以及中枢神经系统的许多部位。
TP2506	Ser-Asn-Thr-Arg
	Ser-Asn-Thr-Arg 是一种四肽化合物，是通过转录激活因子样效应子截断形成的化合物。
T9184L	Compound 3344 hydrochloride 4-(2,3-dihydro-1,4-benzodioxin-5-yl)-~{N}-[3-[(dimethylamino)methyl]phenyl]-2-methoxy-aniline hydrochloride(2368246-78-8 free base),Compound 3344 hydrochloride (2368246-78-8 free base)	Ras	GPCR/G Protein; MAPK
	Compound 3344 hydrochloride 是 KRAS 效应相互作用的抑制剂，亲和力为 126nm。
T24706	RBC10 RBC 10,RBC-10	GTPase	GPCR/G Protein
	RBC10 抑制 Ral 与其效应物 RALBP1 的结合，以及抑制 Ral 介导的鼠胚胎成纤维细胞的细胞扩散和人类癌细胞系的非贴壁依赖性生长。
T11718	JI051 JI-051	Gamma-secretase	Neuroscience; Proteases/Proteasome; Stem Cells
	JI051 具有抗肿瘤作用，能够与癌症相关蛋白伴侣 prohibitin 2 (PHB2) 相互作用，通过抑制 Notch 下游效应基因 Hes1 转录来促使细胞周期停滞，抑制HEK293 细胞和胰腺癌细胞增殖。
T6738	Z-FA-FMK	SARS-CoV; Cysteine Protease	Microbiology/Virology; Proteases/Proteasome
	Z-FA-FMK 是一种广谱的卤代甲基酮抑制剂，可抑制冠状病毒蛋白酶3CL，Ki 为 25.7 μM。它可以不可逆地抑制半胱氨酸蛋白酶，也可以抑制效应半胱天冬酶。
T6634	RBC8	GTPase; Ras	GPCR/G Protein; MAPK
	RBC8是一种特异性 GTP 酶 RalA/RalB 抑制剂，通过抑制 Ral 与其效应物 RALBP1 的结合，对 GTP 酶 RhoA 和 Ras 没有抑制作用。
TP1076L	AUNP-12 acetate AUNP-12 acetate (1353563-85-5 Free base)	PD-1/PD-L1	Apoptosis; Cell Cycle/Checkpoint; Immunology/Inflammation
	AUNP-12 acetate 是一种 PD-1的多肽抑制剂，在抑制淋巴细胞增殖和效应功能上对 PD-1和 PD-2等效，具有免疫激活和良好的抗肿瘤活性。
T77471	Tinurilimab BAY 1834942
	Tinurilimab (Bay 1834942) 是一种单克隆抗体，靶向并抑制 CEACAM6，CEACAM6 属于免疫检查点调节剂。 Tinurilimab 可用于效应 T 细胞对抗肿瘤的研究。
T77170	Siplizumab MEDI-507	Others	Others
	Siplizumab (MEDI-507) 是一种人源化靶向 CD2 的 IgG1 单克隆抗体。Siplizumab 在体外选择性地消耗效应记忆 T 细胞并促进同种异体反应性调节性 T 细胞的相对扩增。Siplizumab 可用于治疗斑块状银屑病。
T9901A-005	Zolbetuximab IMAB362	Others	Others
	Zolbetuximab(IMAB362) 是一种特异性靶向 Claudin-18.2 的单克隆抗体。Zolbetuximab 具有潜在的抗肿瘤活性，通过免疫效应机制介导对 Claudin-18.2 阳性细胞的杀伤作用。Zolbetuximab 可用于研究胃肠道腺癌和胰腺肿瘤。
T77370	Ianalumab VAY-736	Others	Others
	Ianalumab (VAY-736) 是一种脱羧化针对 BAFF-R 的人源化抗体。Ianalumab 能够抑制 BAFF 与 BAFF-R 之间的相互作用，抑制 BAFF 介导的凋亡保护。Ianalumab 具有抗体依赖性细胞毒性 (ADCC)，通过激活免疫受体酪氨酸激活基序 (ITAM) 介导的效应细胞来发挥作用。
T19888	6BrW 6-BrW,6 BrW
	6BrW is an analog of tryptophan effector.
T32439	L 35 L-35,L35
	L 35 is kind of a negative effector of hemoglobin.
T24707	RBC6 RBC-6,RBC 6
	RBC6 is an inhibitor of the binding of Ral to its effector RALBP1.
T9184	Compound 3344	Ras	GPCR/G Protein; MAPK
	Compound 3344 是 KRAS-效应器相互作用的抑制剂，亲和力为126nm。
T68408	AMG-1
	AMG-1 is a specific CRAC channel inhibitor. AMG-1 blocks the function of effector T cells, but not regulatory T cells in vitro and it attenuates the progression and severity of EAE in vivo.
T37965	4-Epitetracycline hydrochloride
	Epitetracycline is an epimer of the antibiotic tetracycline . Epimers of tetracycline form without catalysis and are considered degradation products. Epitetracycline has decreased activity as an antibiotic or a Tet repressor effector but may have stronger toxic effects in animals.
T10210	A-9758	ROR	Metabolism
	A-9758 is a RORγ ligand and a selective RORγt inverse agonist (IC50: 5 nM) and exhibits robust potency against IL-17A release. It is effective in suppressing both Th17 differentiation and Th17 effector function. A-9758 significantly attenuates IL-23 drive
T31396	Dexbrompheniramine maleate D-Brompheniramine,Brompheniramine d-,Dexbrompheniraminum,Disophrol,Drixoral
	Dexbrompheniramine is an antihistamine with anticholinergic properties. It is used to treat allergic diseases such as hay fever or urticaria. It can compete with histamine for H1 receptor sites on effector cells of the gastrointestinal tract, blood vessel
TP1075	AUNP-12 TFA (1353563-85-5 free base) AUNP-12 TFA,NP-12 TFA
	AUNP-12 TFA (NP-12 TFA) is a polypeptide antagonist in the pd-1 signaling pathway, which has the same antagonistic effect on pd-l1 and pd-l2, and can protect the proliferation and effector function of lymphocytes.
T70291	PCC0208018
	PCC0208018 is a novel activator of effector T cells, enhancing T cell proliferation and activation to release interferon gamma (IFN-γ) and interleukin-2 (IL-2) without blocking the programmed cell death 1 (PD-1)/programmed cell death-ligand 1 (PD-L1) binding and not directly affecting tumor cell viability in vitro.
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
T10382	AS2863619 free base	CDK	Cell Cycle/Checkpoint
	AS2863619 free base enables the conversion of antigen-specific effector/memory T cells into Foxp3+ regulatory T (Treg) cells. It is a potent, orally active CDK8 and CDK19 inhibitor (IC50s: 0.61 nM and 4.28 nM). STAT5 activation enhanced by AS2863619 free base inhibition of CDK8/19, which consequently activates the Foxp3 gene.
T77182	Rimteravimab
	Rimteravimab (XVR011) 是具强大中和活性、高稳定性及广泛覆盖范围的二价VHH-Fc抗体，并具备沉默Fc效应器功能，可用于对抗SARS-CoV-2 引发的疾病。
T68594	NFAT:AP-1 inhibitor-10
	NFAT:AP-1 inhibitor-10 is a novel inhibitor of the NFAT:AP-1:DNA interaction on the ARRE-2 element, binding to DNA in a sequence-selective manner and inhibiting the transcription of the Il2 gene and several other cyclosporin A-sensitive cytokine genes important for the effector immune response.
T75815	WKYMVM-NH2 TFA
	WKYMVM-NH2 TFA 是一种高效的 N-甲酰肽受体 FPR1 与 FPRL1/2 激动剂，具备激活白细胞功效特性，包括趋化性、补体受体-3 的激活以及 NADPH 氧化酶的激活。
T39548	Amustaline dihydrochloride S-303 dihydrochloride
	Amustaline (S-303) dihydrochloride is a nucleic acid-targeted alkylator recognized for its efficacy as a pathogen inactivation agent in blood components containing red blood cells. This compound comprises three key elements: an acridine anchor (a non-covalently bonding intercalator targeting nucleic acids), an effector (a bis-alkylator group that interacts with nucleophiles), and a linker (a flexible carbon chain with a labile ester bond, hydrolyzing at neutral pH to non-reactive products).
T36236	5-cis Carbaprostacyclin
	5-cis Carbaprostacyclin is a stable analog of PGI2 and an isomer of carbaprostacyclin. It is a weak inhibitor of human platelet aggregation with an IC50 of 2.8 μM compared to 0.3 μM for carbaprostacyclin. 5-cis Carbaprostacyclin is a much weaker effector of rabbit mesenteric artery relaxation with an EC50 of 104 μM compared to 5.9 μM for carbaprostacyclin. It even antagonizes the adenylate cyclase activation induced by carbaprostacyclin.
T83076	Anticancer agent 93
	Anticanceragent 93, 一种4-羟基香豆素衍生物，能够抑制肺癌细胞的侵袭与迁移，其机制为调节上皮间质转化（EMT）效应子的表达。
T71890	F5446
	F5446 is a SUV39H1 inhibitor. F5446 has an EC50 of 0.496 μmol/L for SUV39H1 enzymatic activity. H3K9me3 was enriched in the promoters of GZMB, PRF1, FASLG, and IFNG in quiescent T cells. F5446 inhibited H3K9me3, thereby upregulating expression of these effectors in tumor-infiltrating CTLs and suppressing colon carcinoma growth in a CD8+ CTL-dependent manner in vivo. Our data indicate that SUV39H1 represses CTL effector gene expression and, in doing so, confers colon cancer immune escape.
T36492	CMC2.24
	CMC2.24 (TRB-N0224) is an orally active tricarbonylmethane agent that demonstrates effectiveness in inhibiting Ras activation and the downstream effector ERK1/2 pathway, thus effectively combating pancreatic tumor formation in mice. Additionally, CMC2.24 exerts potent inhibitory effects on zinc-dependent MMPs, with IC50s ranging from 2.0-69 μM. Furthermore, CMC2.24 aids in alleviating the progression of osteoarthritis by restoring cartilage homeostasis and inhibiting chondrocyte apoptosis throug...
T76936	Budigalimab
	Budigalimab (ABBV 181; PR 1648817) 是一种人源 IgG1单克隆抗体，靶向程序性细胞死亡 1 (PD-1) 受体。Budigalimab 具有 Fc 突变，从而减少了 Fc 受体相互作用和效应因子的抑制作用。
T77096	Nemvaleukin alfa
	Nemvaleukin alfa (ALKS 4230) 为一种IL-2融合蛋白，专门针对中等亲和力IL-2R进行选择性结合。该化合物作为NK及效应T细胞的活化剂，主要应用于癌症研究领域。
T76677	Dacetuzumab
	Dacetuzumab (SGN-40) 是一种人源化的 IgG1，抗 CD40单克隆抗体，具有抗淋巴瘤活性。Dacetuzumab 通过免疫效应作用(抗体依赖性细胞毒性和吞噬作用[ADCC/ADCP]) 杀死肿瘤细胞。Dacetuzumab ((SGN-40) 可用于多发性骨髓瘤研究。
T77061	Letolizumab
	Letolizumab (BMS-986004) 是一种靶向CD40L 的单克隆抗体，其产生是为了表达缺乏效应器功能的突变IgG1，包括 Fc 结合和补体固定。Letolizumab 降低了排斥反应、血栓栓塞，延长了存活时间。
T37755	Phenylacetyl-Coenzyme A (sodium salt)
	Phenylacetyl-coenzyme A (CoA) is a key intermediate in aerobic catabolism of phenylacetate in bacteria such asPseudomonas, when cultured in minimal media using phenylacetate as the sole carbon source.1It is a precursor in the synthesis of the antibiotic penicillin G found in industrial strains ofP. chrysogenum. Phenylacetyl-CoA also acts as an effector molecule of the TetR family transcriptional repressor PaaR inT. thermophilusand the GntR family transcriptional regulator PaaX inE. coliandPseudo...
T35539	IHR-Cy3 IHR-Cy3
	Potent fluorescent Smo antagonist (IC50 = 100 nM). Non-fluorescent analog also available. Fan et al (2014) The Hedgehog pathway effector smoothened exhibits signaling competency in the absence of ciliary accumulation. Chem.Biol. 21 1680 PMID:25484239
T36641	RAS inhibitor Abd-7
	RAS inhibitor Abd-7 is a powerful compound (Kd=51 nM) that binds to RAS and inhibits the protein-protein interaction (PPI) between RAS and its effectors. By interacting with RAS within cells, RAS inhibitor Abd-7 hinders RAS-effector interactions and suppresses endogenous RAS-dependent signaling. Additionally, RAS inhibitor Abd-7 disrupts the PPI of different mutant KRAS proteins with PI3K, CRAF, RALGDS, as well as NRAS Q61H and HRAS G12V[1].
T36189	CAY10406
	CAY10406 is a trifluoromethyl analog of an isatin sulfonamide compound that selectively inhibits caspases 3 and 7. The non-trifluoromethyl compound exhibits Ki values of 1.2 nM and 6 nM for caspases 3 and 7, respectively. For all of the other caspases tested, it is 100 to 1,000 times less potent. Caspases 3 and 7 are 'effector caspases' that are downstream from the initiating steps of apoptosis, and are implicated in the main proteolytic processing of the apoptotic signal. No data is currently a...
T38384	Nexinhib20
	Nexinhib20 is an inhibitor of the protein-protein interaction between the small GTPase Rab27a and its effector JFC1 (IC50 = 2.6 μM).[1] It inhibits myeloperoxidase (MPO) secretion induced by granulocyte macrophage colony-stimulating factor (GM-CSF) and fMLP in isolated human neutrophils (IC50 = 0.33 μM). Nexinhib20 (30 mg/kg) reduces LPS-induced increases in plasma MPO levels, as well as LPS-induced hepatic and renal neutrophil infiltration in a mouse model of endotoxin-induced systemic inflamma...
TP2222	APTSTAT3-9R	Others	Others
	APTSTAT3-9R-9R is a STAT3 inhibitor (Ki: 231 nmol/L). STAT3 has been reported to promote the proliferation, survival, metastasis, immune escape, as well as drug resistance of cancer cells, making it a promising target for various diseases. However, though
T82508	Eciskafusp alfa	PD-1/PD-L1	Apoptosis; Cell Cycle/Checkpoint; Immunology/Inflammation
	Eciskafusp alfa是一种针对程序性细胞死亡1(PDCD1，亦称PD-1)的顺式靶向IL2v免疫细胞因子。它优先选择抗原特异性干细胞样PD-1+ TCF-1+ CD8+ T细胞，并促使这些细胞分化成更高效的效应器细胞。Eciskafusp alfa主要用于癌症与慢性感染的研究领域。
T76020	AUNP-12 TFA
	AUNP-12 (NP-12) TFA 是 PD-1信号通路的一种多肽拮抗剂，在抑制淋巴细胞增殖和效应功能方面对 PD-L1和 PD-L2 具有等效的拮抗作用。AUNP-12 TFA 具有免疫激活作用、良好的抗肿瘤活性，具有更好的研究免疫相关不良事件 (irAEs) 的潜力。
T71163	Pimasertib HCl
	Pimasertib HCl is an orally bioavailable small-molecule inhibitor of MEK1 and MEK2 (MEK1/2) with potential antineoplastic activity. Pimasertib selectively binds to and inhibits the activity of MEK1/2, preventing the activation of MEK1/2-dependent effector proteins and transcription factors, which may result in the inhibition of growth factor-mediated cell signaling and tumor cell proliferation. MEK1/2 (MAP2K1/K2) are dual-specificity threonine/tyrosine kinases that play key roles in the activati...
T75131	RMC-6291
	RMC-6291 是一种口服有效的KRASG12C(ON)共价抑制剂。RMC-6291 在 KRASG12C(ON) 和亲环蛋白 A (CypA) 之间的肿瘤细胞内形成三复合物。因此，RMC-6291 通过空间阻断RAS 效应子结合来阻止 KRASG12C(ON) 发出信号。RMC-6291 在 KRASG12C 肿瘤模型中对RAS 通路活性产生了深度和持久抑制。
T21819	Psora 4
	Psora-4，一种有效的Kv1.3(电压门控钾通道)选择性抑制剂，EC50值为3 nM。该化合物显示出免疫抑制活性，在体外能够抑制人类及大鼠髓鞘组织特异性效应记忆T细胞的增殖，展现出治疗自身免疫性疾病的潜力。

化合物

Cat.No: T5210

Target: Apoptosis, BCL

Cat.No: T10826

Target: HIV Protease, Microtubule Associated

L-5-BromoTryptophan

Cat.No: T19889

Synonym: L-5-溴色氨酸,5-BrW,5 BrW

Target: Others

Acetylcholine bromide

Cat.No: T20344

Target: Others

Ser-Asn-Thr-Arg

Cat.No: TP2506

Compound 3344 hydrochloride

Cat.No: T9184L

Synonym: 4-(2,3-dihydro-1,4-benzodioxin-5-yl)-~{N}-[3-[(dimethylamino)methyl]phenyl]-2-methoxy-aniline hydrochloride(2368246-78-8 free base),Compound 3344 hydrochloride (2368246-78-8 free base)

Target: Ras

Cat.No: T24706

Synonym: RBC 10,RBC-10

Target: GTPase

Cat.No: T11718

Synonym: JI-051

Target: Gamma-secretase

Cat.No: T6738

Target: SARS-CoV, Cysteine Protease

Cat.No: T6634

Target: GTPase, Ras

AUNP-12 acetate

Cat.No: TP1076L

Synonym: AUNP-12 acetate (1353563-85-5 Free base)

Target: PD-1/PD-L1

Cat.No: T77471

Synonym: BAY 1834942

Cat.No: T77170

Synonym: MEDI-507

Target: Others

Cat.No: T9901A-005

Synonym: IMAB362

Target: Others

Cat.No: T77370

Synonym: VAY-736

Target: Others

Cat.No: T19888

Synonym: 6-BrW,6 BrW

Cat.No: T32439

Synonym: L-35,L35

Cat.No: T24707

Synonym: RBC-6,RBC 6

Cat.No: T9184

Target: Ras

Cat.No: T68408

4-Epitetracycline hydrochloride

Cat.No: T37965

Cat.No: T10210

Target: ROR

Dexbrompheniramine maleate

Cat.No: T31396

Synonym: D-Brompheniramine,Brompheniramine d-,Dexbrompheniraminum,Disophrol,Drixoral

AUNP-12 TFA (1353563-85-5 free base)

Cat.No: TP1075

Synonym: AUNP-12 TFA,NP-12 TFA

Cat.No: T70291

Cat.No: T16578

Target: Others

AS2863619 free base

Cat.No: T10382

Target: CDK

Cat.No: T77182

NFAT:AP-1 inhibitor-10

Cat.No: T68594

Cat.No: T75815

Amustaline dihydrochloride

Cat.No: T39548

Synonym: S-303 dihydrochloride

5-cis Carbaprostacyclin

Cat.No: T36236

Anticancer agent 93

Cat.No: T83076

Cat.No: T71890

Cat.No: T36492

Cat.No: T76936

Nemvaleukin alfa

Cat.No: T77096

Cat.No: T76677

Cat.No: T77061

Phenylacetyl-Coenzyme A (sodium salt)

Cat.No: T37755

Cat.No: T35539

Synonym: IHR-Cy3

RAS inhibitor Abd-7

Cat.No: T36641

Cat.No: T36189

Cat.No: T38384

Cat.No: TP2222

Target: Others

Eciskafusp alfa

Cat.No: T82508

Target: PD-1/PD-L1

Cat.No: T76020

Cat.No: T71163

Cat.No: T75131

Cat.No: T21819

Cat. No.	Product Name	Target	Signaling Pathways
T6751	Acetylcholine iodide Acetylcolina	Others	Others
	Acetylcholine iodide (Acetylcolina) 是一种在中枢和外周神经系统中常见的神经递质。
T4973	Paraxanthine 1,7-二甲基黄嘌呤,1,7-DIMETHYLXANTHINE	Endogenous Metabolite	Metabolism
	Paraxanthine (1,7-dimethylxanthine) 是一种 caffeine 的代谢物，能够刺激Ryanodine 受体通道来抑制多巴胺能细胞的死亡。
T21033	Adenanthin Adenanthin A,Adenanthin-A,AdenanthinA
	Adenanthin, a natural inhibitor of thiol-dependent antioxidant enzymes, impairs the effector functions of human natural killer cells.
T38331	Commendamide
	Commendamide is a natural bacterial product that was discovered in a screen for commensal bacteria effector genes (Cbegs). Cbeg12 is a bacterial effector gene that encodes for its production. Commendamide is structurally similar to long-chain N-acyl-amides, which commonly signal, in mammals, through G protein-coupled receptors. Commendamide activates GPR132 (also known as G2A) with an EC50 value of 11.8 μM.
TN1862	Licoflavonol	Antifection	Microbiology/Virology
	Licoflavonol is a novel natural inhibitor of Salmonella T3SS, could be a promising candidate for novel type of anti-virulence drugs, it exhibits a strong inhibitory effect on the secretion of the SPI-1 effector proteins via regulating the transcription of
T66078	Cardamonin
	Cardamonin, a chalcone extracted from cardamom spice with anti-inflammatory and anti-tumor activities. Cardamonin decreased viability of NPC(Nasopharyngeal carcinoma ) cells in a concentration-dependent manner. The IC50 values were 16.22 μM(CNE-1), 14.34 μM (CNE-2), 16.50 μM (HONE-1), and 68.12 μM (SUNE-1). Moreover, the expression level of the proapoptotic effector protein Bax and Bid was also markedly increased after treatment with cardamonin（15μM） in CNE-2 cells.In vivo, cardamonin (25 mg/kg ...

天然产物

Acetylcholine iodide

Cat.No: T6751

Synonym: Acetylcolina

Target: Others

Cat.No: T4973

Synonym: 1,7-二甲基黄嘌呤,1,7-DIMETHYLXANTHINE

Target: Endogenous Metabolite

Cat.No: T21033

Synonym: Adenanthin A,Adenanthin-A,AdenanthinA

Cat.No: T38331

Cat.No: TN1862

Target: Antifection

Cat.No: T66078

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