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27

抑制剂 & 化合物

14

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T11696	Ivachtin Caspase-3 Inhibitor VII	Caspase	Apoptosis; Proteases/Proteasome
	Ivachtin (Caspase-3 Inhibitor VII) 是一种非肽，非竞争性和可逆的caspase-3抑制剂，IC50为 23 nM。它是其余胱天蛋白酶的适度抑制剂。
T12617L	(R)-CR8 (R)-CR8,(R)-Isomer,(2R)-2-[[9-异丙基-6-[[[4-(2-吡啶基)苯基]甲基]氨基]-9H-嘌呤-2-基]氨基]-1-丁醇,CR8	Apoptosis; CDK	Apoptosis; Cell Cycle/Checkpoint
	(R)-CR8 ((R)-Isomer) 是 Roscovitine 类似物，是CDK1/2/5/7/9抑制剂。它作为一种分子胶降解剂来消耗细胞周期蛋白 K。它诱导细胞凋亡并具有神经保护作用。
T36819	Ac-FLTD-CMK	Caspase	Apoptosis; Proteases/Proteasome
	Ac-FLTD-CMK 是由消皮素 D (GSDMDD) 衍生的抑制剂，具有对炎症性 caspases 特异性的抑制作用。Ac-FLTD-CMK 对 Ac-FLTD-CMK 对 caspases-1、caspases-4和 caspases-11有抑制作用，IC50分别为为 46.7 nM、 1.49 μM 和 329 nM。 Ac-FLTD-CMK 对 caspases-1、caspases-4、 caspases-11均表现出有效性，但对凋亡相关的 caspase-3 无效。
T7020	Z-VAD-FMK Z-VAD(OH)-FMK,Caspase Inhibitor VI,Z-VAD	Caspase	Apoptosis; Proteases/Proteasome
	Z-VAD-FMK (Caspase Inhibitor VI) 是一种 caspase 的广谱抑制剂，具有不可逆性。Z-VAD-FMK 与活化的 caspase 结合，从而抑制细胞凋亡。
T6013	Z-VAD(OMe)-FMK Z-VAD-FMK,Z-Val-Ala-Asp(OMe)-FMK	Caspase	Apoptosis; Proteases/Proteasome
	Z-VAD(OMe)-FMK (Z-Val-Ala-Asp(OMe)-FMK) 是一种 caspase 的广谱抑制剂，具有细胞渗透性和不可逆性。Z-VAD(OMe)-FMK 与活化的 caspase 结合，从而抑制细胞凋亡。
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。
T22812	GRI977143 GRI 977143	LPA Receptor	GPCR/G Protein
	GRI977143 是 LPA2 的选择性非脂质激动剂 (EC50 = 3.3 μM)。 GRI977143 抑制半胱天冬酶 3、7、8 和 9 的激活，并减少 DNA 片段化。
T6007	Birinapant TL32711,比瑞那帕	Apoptosis; IAP; HIV Protease	Apoptosis; Microbiology/Virology; Proteases/Proteasome
	Birinapant (TL32711) 是一种二价 Smac 模拟物，是 XIAP 和 cIAP1的强效拮抗剂，Kd 值分别为 45 nM 和小于 1 nM。它靶向与 TRAF2 相关的 cIAP，并消除 TNF 诱导的 NF-κB 活化。
T9118	KEA1-97	Apoptosis; Others; Caspase	Apoptosis; Others; Proteases/Proteasome
	KEA1-97 是一种选择性硫氧还蛋白-半胱天冬酶 3相互作用干扰剂，IC50为10 μM。它在不影响硫氧还蛋白活性的情况下, 破坏硫氧还蛋白与 caspase 3 的相互作用，激活半胱天冬酶，诱导细胞凋亡。
T8866	GW779439X	Apoptosis; Antibacterial; CDK; Aurora Kinase	Apoptosis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Microbiology/Virology
	GW779439X 属于吡唑并吡啶类，是一种金黄色葡萄球菌 PASTA 激酶 Stk1抑制剂。它是一种AURKA 抑制剂，可通过 caspases 3/7 诱导细胞凋亡。
T36493	CMLD-2	Apoptosis; HuR	Apoptosis; Chromatin/Epigenetic
	CMLD-2是一种 HuR-ARE 相互作用的抑制剂（Ki：350 nM），能竞争性地结合 HuR 蛋白并破坏其与富含腺嘌呤元素（ARE）的 mRNA 目标的相互作用。CMLD-2诱导细胞凋亡并通过 MAD2下调表现出抗肿瘤作用。CMLD-2 (1-75 μM ; 24-72 h) 对甲状腺癌细胞的活力具有抑制作用.CMLD-2 (20-30 μM ; 24-48 h) 激活 Caspases 并诱导H1299和A549细胞凋亡.CMLD-2 (30 μM ; 24-48 h) 诱导H1299和A549细胞的G1细胞周期停止和线粒体扰动。 CMLD-2（30μM；24-48小时）减少H1299细胞中HuR 和HuR 调节的mRNAs 和蛋白质的表达.CMLD-2（35μM；72小时）降低SW1736、8505C、BCPAP 和K1细胞的定向迁移能力。CMLD-2诱导SW1736、8505C、BCPAP 和K1细胞中的MAD2 mRNA 水平强烈下降。
T0859	Fenbufen 芬布芬,CL-82204,Lederfen	ATPase; Caspase; COX	Apoptosis; Immunology/Inflammation; Membrane transporter/Ion channel; Neuroscience; Proteases/Proteasome
	Fenbufen (Lederfen) 是一种非甾体抗炎药，主要用于治疗骨关节炎、强直性脊柱炎和肌腱炎的炎症。它还可用于缓解背痛、扭伤和骨折，具有 caspases 的抑制活性。它对 COX-1和 COX-2具有抑制活性，其 IC50分别为 3.9 μM 和 8.1 μM。
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...
T26242	SW IV-52 SW-IV-52,SW IV52,SW IV 52,SWIV52
	SW IV-52 is an XIAP-inhibitor that acts as a second mitochondria-derived activator of caspases (SMAC) mimetic.
T10548	Biotin-VAD-FMK	Caspase	Apoptosis; Proteases/Proteasome
	Biotin-VAD-FMK is a cell-permeable, irreversible biotin-labeled inhibitor of caspase. It is used to identify active caspases in cell lysates.
T36658	Boc-Glu-OBzl
	Boc-Glu-OBzl is an amino acid building block.1,2It has been used in the synthesis of peptide-based inhibitors of human caspases and human rhinovirus (HRV) 3C protease that have enzyme inhibitory activityin vitro. 1.Garcia-Calvo, M., Peterson, E.P., Leiting, B., et al.Inhibition of human caspases by peptide-based and macromolecular inhibitorsJ. Biol. Chem.273(49)32608-32613(1998) 2.Dragovich, P.S., Webber, S.E., Babine, R.E., et al.Structure-based design, synthesis, and biological evaluation of i...
T68869	TP-110
	TP-110 is a new proteasome inhibitor, which shows potent growth inhibition in various tumor cell lines. Treatment with TP-110 for 24 h in vitro induced apoptosis in multiple myeloma cell line RPMI8226. TP-110 reduced the intrinsic inhibitor of apoptosis proteins (IAPs), cIAP-1 and XIAP, that suppress executioner caspases.
T36331	Z-AEVD-FMK Z-AEVD-FMK,Z-Ala-Glu-Val-Asp-Fluoromethyl Ketone
	Z-AEVD-FMK is an irreversible inhibitor of caspase-10 and related caspases.[1] At 10 &#181M, it can prevent the initiation of Fas signaling by caspase-10 in Jurkat T lymphoma cells, preventing Bid cleavage into its active form, caspase cascade activation, and apoptosis.[2]
T80537	Ac-AAVALLPAVLLALLAP-LEHD-CHO	Caspase	Apoptosis; Proteases/Proteasome
	Ac-AAVALLPAVLLALLAP-LEHD-CHO 是半胱天冬酶4、5和9的抑制剂，能够对Neocarzinostatin处理的MCF-7细胞展现保护效果。
T70430	XK469
	XK489 is a synthetic quinoxaline phenoxypropionic acid derivative with proapoptotic and antiproliferative activities. R(+)XK469 selectively inhibits topoisomerase II-beta, blocks activation of MEK/MAPK signaling kinases, stimulates caspases, and upregulates p53-dependent proteins, including cyclins A and B1, thereby arresting cancer cells in the G2/M phase of the cell cycle. Both R(+) and S(-) isomers of this agent are cytotoxic, although the R-isomer is more potent.
T68262	AEG40826
	AEG40826 (HGS1029) is the hydrochloride salt of a small-molecule inhibitor of IAP (Inhibitor of Apoptosis Protein) family proteins with potential antineoplastic activity. IAP inhibitor HGS1029 selectively inhibits the biological activity of IAP proteins, which may restore apoptotic signaling pathways; this agent may work synergistically with cytotoxic drugs to overcome tumor cell resistance to apoptosis. IAPs are overexpressed by many cancer cell types, suppressing apoptosis by binding and inhib...
T69632	VRT-043198
	VRT-043198 是 VX-765 (Belnacasan) 的活性代谢物，是有效的、选择性的、能透过血脑屏障的caspase-1的抑制剂。VRT-043198 对caspase-1和 caspase-4 的 Ki 值分别为 0.8 nM 和 0.6 nM。
T41240	Verrucarin A
	Verrucarin A (Muconomycin A) 是一种 D 型大环真菌毒素。Verrucarin A 是一种蛋白质合成 (protein synthesis) 的抑制剂，来源于Myrothecium verrucaria，可抑制白血病细胞系生长，并激活巨噬细胞 caspases、凋亡和炎症信号。Verrucarin A 能有效提高 p38 MAPK 的磷酸化，降低 ERK/Akt 的磷酸化。Verrucarin A 通过 p21 和 p53 的诱导引起细胞周期调控的解除。
T29060	UNBS-1450 UNBS 1450,UBS1450,UBS-1450,UBS 1450
	UNBS-1450 is a sodium channel antagonist. UNBS-1450 is a hemi-synthetic cardenolide derived from 2″-oxovorusharin, it is effective against various cancer cell types with an excellent differential toxicity. At low nanomolar concentrations, UNBS-1450 induce
T79482	Anticancer agent 137	PI3K	PI3K/Akt/mTOR signaling
	Anticanceragent 137 (8q) 是一种高效的 PI3k 抑制剂，展现出广谱的抗肿瘤活性。它能够诱导 G2/M 阶段的细胞周期阻滞与细胞凋亡（apoptosis），并促进 PARP、caspase 3 和 caspase 7 的裂解。该化合物主要用于癌症相关的生物医学研究。
T73683	AC-VEID-CHO TFA
	AC-VEID-CHO (TFA) 是一种源自多肽的半胱天冬酶抑制剂，针对Caspase-6、Caspase-3和Caspase-7展示出优异的抑制效果，其IC50值分别为16.2 nM、13.6 nM和162.1 nM。该化合物常用于研究阿尔茨海默病、亨廷顿病等神经退行性疾病。
T61673	Anticancer agent 56
	Anticancer agent 56 (compound 4d) is a powerful anti-cancer compound with favorable drug-like properties. It shows significant anticancer activity against multiple cancer cell lines, with an IC50 value of less than 3 μM. Anticancer agent 56 exerts its effects by causing cell cycle arrest at the G2/M phase and activating the mitochondrial apoptosis pathway. Mechanistically, it induces the accumulation of reactive oxygen species (ROS), upregulates BAX, downregulates Bcl-2, and triggers the activat...

化合物

Cat.No: T11696

Synonym: Caspase-3 Inhibitor VII

Target: Caspase

Cat.No: T12617L

Synonym: (R)-CR8,(R)-Isomer,(2R)-2-[[9-异丙基-6-[[[4-(2-吡啶基)苯基]甲基]氨基]-9H-嘌呤-2-基]氨基]-1-丁醇,CR8

Target: Apoptosis, CDK

Cat.No: T36819

Target: Caspase

Cat.No: T7020

Synonym: Z-VAD(OH)-FMK,Caspase Inhibitor VI,Z-VAD

Target: Caspase

Cat.No: T6013

Synonym: Z-VAD-FMK,Z-Val-Ala-Asp(OMe)-FMK

Target: Caspase

Cat.No: T6738

Target: SARS-CoV, Cysteine Protease

Cat.No: T22812

Synonym: GRI 977143

Target: LPA Receptor

Cat.No: T6007

Synonym: TL32711,比瑞那帕

Target: Apoptosis, IAP, HIV Protease

Cat.No: T9118

Target: Apoptosis, Others, Caspase

Cat.No: T8866

Target: Apoptosis, Antibacterial, CDK, Aurora Kinase

Cat.No: T36493

Target: Apoptosis, HuR

Cat.No: T0859

Synonym: 芬布芬,CL-82204,Lederfen

Target: ATPase, Caspase, COX

Cat.No: T36189

Cat.No: T26242

Synonym: SW-IV-52,SW IV52,SW IV 52,SWIV52

Cat.No: T10548

Target: Caspase

Cat.No: T36658

Cat.No: T68869

Cat.No: T36331

Synonym: Z-AEVD-FMK,Z-Ala-Glu-Val-Asp-Fluoromethyl Ketone

Ac-AAVALLPAVLLALLAP-LEHD-CHO

Cat.No: T80537

Target: Caspase

Cat.No: T70430

Cat.No: T68262

Cat.No: T69632

Cat.No: T41240

Cat.No: T29060

Synonym: UNBS 1450,UBS1450,UBS-1450,UBS 1450

Anticancer agent 137

Cat.No: T79482

Target: PI3K

AC-VEID-CHO TFA

Cat.No: T73683

Anticancer agent 56

Cat.No: T61673

Cat. No.	Product Name	Target	Signaling Pathways
TN3681	Clerosterol	BCL; Caspase	Apoptosis; Proteases/Proteasome
	Clerosterol as a precursor of cyasterone, isocyasterone and 29-norcyasterone in biosynthesis of phytoecdysteroids of Ajuga hairy roots. Clerosterol exerts its cytotoxic effect in A2058 human melanoma cells by caspases-dependent apoptosis.
T13818	Phytohemagglutinin PHA-M,植物血球凝集素,PHA,植物血凝素	Apoptosis	Apoptosis
	Phytohemagglutinin (PHA-M) 是一种普通豆菜豆的主要种子凝集素，聚集在子叶的薄壁细胞中。它是一种 T 细胞激活剂，能够刺激人单核白细胞，可诱导 ChAT mRNA 表达，增强 ACh 合成。
T6185	Gambogic Acid 藤黄酸,Beta-Guttiferrin,藤黄酸 A,Guttatic Acid,Guttic Acid	BCL; Autophagy	Apoptosis; Autophagy
	Gambogic Acid (Guttic Acid) 是来自藤黄树的一种藤黄树脂，抑制 Bcl-XL、Bcl-2、Bcl-W、Bcl-B、Bfl-1和 Mcl-1，IC50分别为 1.47 μM、1.21 μM、2.02 μM、0.66 μM、1.06 μM 和 0.79 μM。
T3867	Alpinetin 山姜素,(-)-alpinetin	BCL; PPAR	Apoptosis; DNA Damage/DNA Repair; Metabolism
	Alpinetin ((-)-alpinetin) 是从草豆蔻中分离得到的一种黄酮类天然产物，能够活化PPAR-γ，具有抗炎、抗菌活性。它通过抑制增殖、调节 Bcl-2 家族和 XIAP 表达、释放细胞色素 c 和激活 caspase 具有很强的抗肝癌和胰腺癌细胞作用。
T3894	Polyphyllin II 重楼皂苷 II,Chonglou Saponin II	Apoptosis; Others	Apoptosis; Others
	Polyphyllin II (Chonglou Saponin II) 是重楼中重要的一种皂苷，具有止血、祛痰、抑菌、抗细胞毒和抗孕杀精作用。它通过 caspases 激活和细胞周期停滞诱导细胞凋亡。
T5S2358	Dehydrocorydaline Dehydrocorydalin,脱氢紫堇碱,13-Methylpalmatine	BCL; PARP; p38 MAPK; Caspase; Parasite; Autophagy	Apoptosis; Autophagy; Chromatin/Epigenetic; DNA Damage/DNA Repair; MAPK; Microbiology/Virology; Proteases/Proteasome
	Dehydrocorydaline (13-Methylpalmatine) 是一种生物碱。它调节Bax，Bcl-2蛋白表达，激活caspase-7，caspase-8，并使PARP 失活。它能增强p38 MAPK 活化，具有抗炎、抗癌等功效。它具有强大的抗疟疾作用，并具低细胞毒性。
T2966	Beta-Sitosterol Cupreol,谷甾醇,Beta-Sitosterol,β-Sitosterol,Azuprostat,SKF 14463,beta-谷甾醇,22,23-Dihydrostigmasterol,Betaprost	Apoptosis; Lipase; Endogenous Metabolite	Apoptosis; Metabolism
	Beta-Sitosterol (SKF 14463) 是一种植物甾醇，干扰细胞周期、细胞凋亡、增殖、存活、侵袭、血管生成和炎症等多种细胞信号通路。
T3923	Calycosin Cyclosin,3'-Hydroxyformononetin,异黄酮,毛异黄酮	Apoptosis; Tyrosinase	Apoptosis; Proteases/Proteasome
	Calycosin (Cyclosin) 是一抗氧化和抗炎症活性天然产物。
T5574	Guggulsterone Guggulsterone E&Z,香胶甾酮	Apoptosis; FXR; Akt; Caspase; JNK; Autophagy	Apoptosis; Autophagy; Cytoskeletal Signaling; MAPK; Metabolism; PI3K/Akt/mTOR signaling; Proteases/Proteasome
	Guggulsterone (Guggulsterone E&Z) E&Z 是来自Commiphora wightii 树中树胶脂的植物甾醇。它通过下调抗细胞凋亡基因产物，调节细胞周期蛋白，激活caspases，JNK，抑制Akt，抑制多种肿瘤细胞的生长并诱导细胞凋亡。它是法尼醇 X 受体拮抗剂，可降低 CDCA 诱导的 FXR 活化。
T14003	15-Acetoxyscirpenol	Caspase	Apoptosis; Proteases/Proteasome
	15-Acetoxyscirpenol, a member of the acetoxyscirpenol moiety mycotoxins (ASMs), potently induces apoptosis and inhibits the growth of Jurkat T cells in a dose-dependent manner. This effect is mediated through the activation of caspases independent of caspase-3[1].
TN3682	Clerosterol glucoside	Others	Others
	Clerosterol exerts its cytotoxic effect in A2058 human melanoma cells by caspases-dependent apoptosis.
T71784	Asukamycin
	Asukamycin is polyketide isolated from the S. nodosus subspecies asukaensis that demonstrates a broad range of antibiotic functions. It has been shown to inhibit growth of various tumor cell lines by activating caspases 8 and 3.
TN5201	Uncarinic acid E	BCL; MEK; Caspase; PI3K; Antifection; p53	Apoptosis; MAPK; Microbiology/Virology; PI3K/Akt/mTOR signaling; Proteases/Proteasome
	Uncarinic acid E has anti-cancer activity, it induces apoptosis in HepG2 cells via accumulation of p53, alters the Bax/Bcl-2 ratio, and activates caspases, resulting in cytochrome c release from the mitochondria. A mixture of uncarinic acid E and 27-O-p-(
TN1139	Dehydrocavidine Dehydrocorydaline,岩黄连碱	BCL; PARP	Apoptosis; Chromatin/Epigenetic; DNA Damage/DNA Repair
	Dehydrocavidine (Dehydrocorydaline) 具有抗肿瘤活性，它通过诱导调节 Bax/Bcl-2 介导的细胞凋亡、激活半胱天冬酶以及切割 PARP 来抑制 MCF-7 细胞增殖。

天然产物

Cat.No: TN3681

Target: BCL, Caspase

Phytohemagglutinin

Cat.No: T13818

Synonym: PHA-M,植物血球凝集素,PHA,植物血凝素

Target: Apoptosis

Cat.No: T6185

Synonym: 藤黄酸,Beta-Guttiferrin,藤黄酸 A,Guttatic Acid,Guttic Acid

Target: BCL, Autophagy

Cat.No: T3867

Synonym: 山姜素,(-)-alpinetin

Target: BCL, PPAR

Cat.No: T3894

Synonym: 重楼皂苷 II,Chonglou Saponin II

Target: Apoptosis, Others

Dehydrocorydaline

Cat.No: T5S2358

Synonym: Dehydrocorydalin,脱氢紫堇碱,13-Methylpalmatine

Target: BCL, PARP, p38 MAPK, Caspase, Parasite, Autophagy

Beta-Sitosterol

Cat.No: T2966

Synonym: Cupreol,谷甾醇,Beta-Sitosterol,β-Sitosterol,Azuprostat,SKF 14463,beta-谷甾醇,22,23-Dihydrostigmasterol,Betaprost

Target: Apoptosis, Lipase, Endogenous Metabolite

Cat.No: T3923

Synonym: Cyclosin,3'-Hydroxyformononetin,异黄酮,毛异黄酮

Target: Apoptosis, Tyrosinase

Cat.No: T5574

Synonym: Guggulsterone E&Z,香胶甾酮

Target: Apoptosis, FXR, Akt, Caspase, JNK, Autophagy

15-Acetoxyscirpenol

Cat.No: T14003

Target: Caspase

Clerosterol glucoside

Cat.No: TN3682

Target: Others

Cat.No: T71784

Uncarinic acid E

Cat.No: TN5201

Target: BCL, MEK, Caspase, PI3K, Antifection, p53

Dehydrocavidine

Cat.No: TN1139

Synonym: Dehydrocorydaline,岩黄连碱

Target: BCL, PARP

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