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35

抑制剂 & 化合物

4

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T2470	MDL-28170 Calpain Inhibitor III	Cysteine Protease; Proteasome	Proteases/Proteasome; Ubiquitination
	MDL-28170 (Calpain Inhibitor III) 是一种选择性的、有效的、具有膜渗透性的半胱氨酸蛋白酶 (calpain)抑制剂，可在全身给药后迅速穿过血脑屏障。它还能阻断γ-secretase。
T6583	MG-101 ALLN,Ac-LLnL-CHO,Calpain inhibitor I,Calpain inhibitor-1,MG101,钙蛋白酶抑制剂I	Cysteine Protease; Proteasome	Proteases/Proteasome; Ubiquitination
	MG-101 (Calpain inhibitor I) 是一种有效的半胱氨酸蛋白酶抑制剂，能够抑制钙蛋白酶I (Ki:190 pM)，钙蛋白酶II (Ki:220 pM)，组织蛋白酶B (Ki:150 pM)和组织蛋白酶L (Ki:500 pM)。
T38931	Calpain Inhibitor-1
	Calpain Inhibitor-1 (compound 36) is a highly potent and selective inhibitor of Calpain 1 (Cal1), which is a cysteine protease. It exhibits an IC50 value of 100 nM and a Ki value of 2.89 μM.
T21949	Calpain Inhibitor XII
	(Rac)-Calpain Inhibitor XII是一种可逆的，选择性抑制钙蛋白酶I（calpain I; μ-calpain）的化合物，具有19 nM的Ki值。其对钙蛋白酶II（calpain II; m-calpain; Ki=120 nM）和组织蛋白酶B（cathepsin B; Ki=750 nM）显示出较低的抑制亲和力。(Rac)-Calpain Inhibitor XII用于研究钙蛋白酶在多种生理过程中的角色，如嗜中性粒细胞趋化性、神经元信号传导和心脏对损伤的响应。
T28786	SJA6017 SJA-6017,Calpain Inhibitor VI,Calpain-In-4,SJA 6017,Calpain Inhibitor 4
	SJA6017 is a inhibitor of calpain-1 (IC50 = 7.5 nM) and calpain-2 ( IC50 = 78 nM). SJA6017 also inhibits cathepsins B (IC50s = 15 nM) and cathepsins L (IC50s = 1.6 nM). SJA6017 reduces apoptotic cell death, preserves spinal cord tissue and improves functi
T72439	Calpain Inhibitor XI
	Calpain Inhibitor XI，一种可逆的calpain-1共价抑制剂，适用于神经退行性疾病的研究。
T14187	ALLM Calpain inhibitor II	Others	Others
	ALLM (Calpain inhibitor II), a potent calpain and cathepsin protease inhibitor, not only prevents neuronal cell death but also enhances chronic neurological function following spinal cord injury (SCI)[1][2].
T78632	Z-LLY-FMK Calpain Inhibitor IV	Proteasome	Proteases/Proteasome; Ubiquitination
	Z-LLY-FMK (Calpain Inhibitor IV) 为一种钙蛋白酶抑制剂，涉及调控多个细胞系统的凋亡过程。该化合物能够抑制胆总管结扎所引起的肠细胞凋亡(apoptosis)。
T63708	Calpain-2-IN-1
	Calpain-2-IN-1是选择性的钙蛋白酶-2抑制剂，能够延长 ERK 激活，进而增强学习和记忆。
T80551	Calpain inhibitor V Mu-Val-HPh-FMK	Antibiotic	Microbiology/Virology
	Calpain inhibitor V (Mu-Val-HPh-FMK) 为具抗衣原体活性的细胞渗透性不可逆钙蛋白酶抑制剂。
T63391	Calpain Inhibitor-2
	Calpain Inhibitor-2 是具有亲脂性的钙蛋白酶抑制剂，与黑色素瘤细胞系（A-375和B-16F1）和PC-3前列腺癌细胞相比，他们在体外具有中等到良好的抗增殖效果。Calpain Inhibitor-2 中的化合物3，在基质胶细胞侵袭测定中以2μM 浓度能够抑制了80%的DU-145细胞侵袭。
T2154	MG-132 Z-LLL-al,Z-Leu-Leu-Leu-CHO	Apoptosis; Proteasome; Autophagy	Apoptosis; Autophagy; Proteases/Proteasome; Ubiquitination
	MG-132 (Z-Leu-Leu-Leu-al) 是一种 26S 蛋白酶体抑制剂 (IC50=100 nM)，具有细胞渗透性、可逆性。MG-132 可作为自噬激活剂，可诱导凋亡。
T9710	Dazcapistat	Cysteine Protease	Proteases/Proteasome
	Dazcapistat 是一种有效的 calpain 抑制剂，对 calpain 1、calpain 2 和 calpain 9 的 IC50 值均 <3 μM。
T2493	PD 151746	Cysteine Protease; Proteasome	Proteases/Proteasome; Ubiquitination
	PD151746 is a calpain inhibitor with a 20-fold selectivity for u-calpain (Ki = 0.26 ± 0.03 μM) over m-calpain (Ki = 5.33 ± 0.77 μM). Its IC50 values are 0.26 ± 0.03 μM (Ki for μ-calpain) and 5.33 ± 0.77 μM (Ki for m-calpain) [1]. In vitro, PD151746 targets calpain and reduces oxLDL-induced cytotoxicity [2].
T6432	Calpeptin	Apoptosis; Cysteine Protease; Proteasome	Apoptosis; Proteases/Proteasome; Ubiquitination
	Calpeptin 是一种具有细胞穿透性的calpain 抑制剂，也是cathepsin K 抑制剂，其对人血小板 Calpain I 的ID50值为40 nM。
T3525	PD150606	Cysteine Protease	Proteases/Proteasome
	PD150606 是一种具有选择性的非肽 calpain 抑制剂，具有神经保护活性，抑制 μ-calpains 和 m-calpains ，抑制红藻氨酸诱导的 Ca2+ 内流，干扰兴奋性毒性依赖性运动神经元死亡。
TP2056L	Acetyl-Calpastatin (184-210)(human) acetate Acetyl-Calpastatin (184-210) (human) acetate(123714-50-1 Free base )	Cysteine Protease	Proteases/Proteasome
	Acetyl-Calpastatin (184-210)(human) acetate 是一种有效，选择性和可逆的钙蛋白酶 (calpain) 抑制剂，对 μ-钙蛋白酶和组织蛋白酶 L 的 Ki 值分别为 0.2 nM 和 6 μM。
T60150	(1S,2R)-Alicapistat	Cysteine Protease	Proteases/Proteasome
	(1S,2R)-Alicapistat ((1S,2R)-ABT-957) is a highly efficient, orally active compound that selectively inhibits human calpains 1 and 2, with promising implications for Alzheimer's disease (AD) therapy [1]. This compound effectively addresses the metabolic liability associated with carbonyl reduction, while demonstrating potent inhibition of calpain 1 with an IC50 value of 395 nM [2].
T36352	Suc-Leu-Tyr-AMC
	Suc-Leu-Tyr-AMC 是钙蛋白酶 I 和 II 以及木瓜蛋白酶（另一种半胱氨酸蛋白酶）的荧光底物，用于测量 20S 蛋白酶体的糜蛋白酶样肽酶活性（Ex-max：360 nm；Em-max：460 nm）。Suc-Leu-Tyr-AMC 也能被大肠杆菌的 Ti 蛋白酶裂解。
T6040	Aloxistatin E64d,Loxistatin,阿洛司他丁,E64c ethyl ester	SARS-CoV; Cysteine Protease	Microbiology/Virology; Proteases/Proteasome
	Aloxistatin (E64d) 是一种不可逆的、可透过膜的溶酶体和细胞溶质半胱氨酸蛋白酶抑制剂，能够抑制完整血小板中的钙蛋白酶活性。它是一种半胱氨酸蛋白酶抑制剂，具有血小板聚集抑制活性。
T23598	A-953227 A 953227,A953227
	A-953227 is a highly effective and selective inhibitor of calpain. A-953227 features enhanced selectivity versus related cysteine protease cathepsins, favorable microsomal stability, and efficacy in cellular assays.
T68728	EP 459
	EP 459 is a thiol and calpain protease inhibitor.
T13486	Neurodegenerative Disorder-Targeting Compound 1	Others	Others
	Neurodegenerative Disorder-Targeting Compound 1 是一种靶向 calpain 的抑制剂。
T80103	Z-Leu-Tyr-Chloromethylketone
	Z-Leu-Tyr-Chloromethylketone是一种抑制剂，专门针对钙蛋白酶(calpain)活性。
T25011	AK-295 CX295,CX 295,AK295,CX-295
	AK 295, also known as CX 295, is a dipeptide inhibitor of alpha-ketoamide calpain.
T25009	AK 275 AK275,AK-275
	AK 275 is a calpain inhibitor that prevents degradation of cytoskeletal and myelin proteins in spinal cord in vitro.
T76364	Ac-Leu-Leu-Norleucinol
	Ac-Leu-Leu-Norleucinol 是钙蛋白酶抑制剂，可用于研究对 Acetaminophen 引起的急性肝损伤，并能够降低诱导引发的谷草转氨酶 (ALT) 和谷丙转氨酶 (AST) 水平。
T83527	(Rac)-Neurodegenerative Disorder-Targeting Compound 1
	(Rac)-Neurodegenerative Disorder-Targeting Compound 1为一种针对神经退行性疾病的化合物，具有calpain抑制活性。
TP2056	Acetyl-Calpastatin(184-210)(human) Acetyl-Calpastatin (184-210) (human)
	Selective calpain inhibitor. Strongly inhibits calpain I (Ki = 0.2 nM) and II but does not inhibit papain, trypsin and cathepsin L (Ki = 6 μM). Increases secretion of amyoid β-protein (Aβ) 42, Aβ40 and Aβ42 ratio.
T80241	Calpastatin subdomain B	Proteasome	Proteases/Proteasome; Ubiquitination
	Calpastatin subdomain B为具有生物活性的肽，其作用为抑制钙蛋白酶活性。
T23596	A-933548 A933548,A 933548
	A-933548 is a potent Calpain inhibitor. A-933548 features enhanced selectivity versus related cysteine protease cathepsins, favorable microsomal stability, and efficacy in cellular assays.
T75794	Acetyl-Calpastatin(184-210)(human) TFA
	Acetyl-Calpastatin(184-210)(human) TFA 是一种有效，选择性和可逆的钙蛋白酶 (calpain) 抑制剂，对 μ-钙蛋白酶和组织蛋白酶 L 的Ki 值分别为 0.2 nM 和 6 μM。
T36854	Pheleuin
	Pheleuin is a pyrazinone derivative synthesized from a dipeptide aldehyde. Although the biological activity of this compound has not been reported, similar diketopiperazines are known to inhibit calpain and/or regulate S. aureus virulence factor expression.
T68547	SNJ-1945
	SNJ-1945 is a calpain inhibitor with more favorable retinal penetration, high oral bioavailability, and long half-life. SNJ1945 rescued defective function in lissencephaly. SNJ-1945 protects SH-SY5Y cells against MPP(+) and rotenone. SNJ-1945 reduces murine retinal cell death in vitro and in vivo. SNJ-1945 has good aqueous solubility, can prevents the heart from KCl arrest-reperfusion injury associated with the impairment of total Ca(2+) handling by inhibiting the proteolysis of alpha-fodrin a...
T83406	2,3-Diphospho-D-glyceric acid pentasodium salt 2,3-DPG pentasodium salt
	2,3-Diphospho-D-glyceric acid pentasodium salt 是一种聚磷化合物，具有明显的阴离子性质。它在红细胞的凹中心起作用，通过结合血红蛋白降低氧亲和力。作为血管钙化 (VC) 的内源性选择性抑制剂，2,3-Diphospho-D-glyceric acid 能显著推迟结晶钙蛋白颗粒 (CPP) 的生成，并在小鼠血管平滑肌细胞系 (MOVAS) 中抑制钙化作用，同时不引起细胞毒性。

化合物

Cat.No: T2470

Synonym: Calpain Inhibitor III

Target: Cysteine Protease, Proteasome

Cat.No: T6583

Synonym: ALLN,Ac-LLnL-CHO,Calpain inhibitor I,Calpain inhibitor-1,MG101,钙蛋白酶抑制剂I

Target: Cysteine Protease, Proteasome

Calpain Inhibitor-1

Cat.No: T38931

Calpain Inhibitor XII

Cat.No: T21949

Cat.No: T28786

Synonym: SJA-6017,Calpain Inhibitor VI,Calpain-In-4,SJA 6017,Calpain Inhibitor 4

Calpain Inhibitor XI

Cat.No: T72439

Cat.No: T14187

Synonym: Calpain inhibitor II

Target: Others

Cat.No: T78632

Synonym: Calpain Inhibitor IV

Target: Proteasome

Calpain-2-IN-1

Cat.No: T63708

Calpain inhibitor V

Cat.No: T80551

Synonym: Mu-Val-HPh-FMK

Target: Antibiotic

Calpain Inhibitor-2

Cat.No: T63391

Cat.No: T2154

Synonym: Z-LLL-al,Z-Leu-Leu-Leu-CHO

Target: Apoptosis, Proteasome, Autophagy

Cat.No: T9710

Target: Cysteine Protease

Cat.No: T2493

Target: Cysteine Protease, Proteasome

Cat.No: T6432

Target: Apoptosis, Cysteine Protease, Proteasome

Cat.No: T3525

Target: Cysteine Protease

Acetyl-Calpastatin (184-210)(human) acetate

Cat.No: TP2056L

Synonym: Acetyl-Calpastatin (184-210) (human) acetate(123714-50-1 Free base )

Target: Cysteine Protease

(1S,2R)-Alicapistat

Cat.No: T60150

Target: Cysteine Protease

Suc-Leu-Tyr-AMC

Cat.No: T36352

Cat.No: T6040

Synonym: E64d,Loxistatin,阿洛司他丁,E64c ethyl ester

Target: SARS-CoV, Cysteine Protease

Cat.No: T23598

Synonym: A 953227,A953227

Cat.No: T68728

Neurodegenerative Disorder-Targeting Compound 1

Cat.No: T13486

Target: Others

Z-Leu-Tyr-Chloromethylketone

Cat.No: T80103

Cat.No: T25011

Synonym: CX295,CX 295,AK295,CX-295

Cat.No: T25009

Synonym: AK275,AK-275

Ac-Leu-Leu-Norleucinol

Cat.No: T76364

(Rac)-Neurodegenerative Disorder-Targeting Compound 1

Cat.No: T83527

Acetyl-Calpastatin(184-210)(human)

Cat.No: TP2056

Synonym: Acetyl-Calpastatin (184-210) (human)

Calpastatin subdomain B

Cat.No: T80241

Target: Proteasome

Cat.No: T23596

Synonym: A933548,A 933548

Acetyl-Calpastatin(184-210)(human) TFA

Cat.No: T75794

Cat.No: T36854

Cat.No: T68547

2,3-Diphospho-D-glyceric acid pentasodium salt

Cat.No: T83406

Synonym: 2,3-DPG pentasodium salt

Cat. No.	Product Name	Target	Signaling Pathways
T37753	Aureusimine B	Cysteine Protease; Antibacterial	Microbiology/Virology; Proteases/Proteasome
	Aureusimine B 是一种钙蛋白酶抑制剂，由金黄色葡萄球菌生物膜产生，可能是金黄色葡萄球菌生物膜感染的潜在生物标志物。
T19384	Isovalerylcarnitine	Apoptosis; Cysteine Protease	Apoptosis; Proteases/Proteasome
	Isovalerylcarnitine (3-methylbutyrylcarnitine) 是 L-亮氨酸分解代谢和异戊酸的积累产生的小分子化合物，也是一种具有选择性和有效性的钙蛋白酶 (calpain) 激活剂，可促使细胞凋亡，与异戊酸血症有关，可作为异戊酸血症的标志。
T36931	Penicillide
	Penicillide is a fungal metabolite originally isolated from Penicillium that has diverse biological activities. It is an inhibitor of calpain 2/m-calpain (IC50 = 7.1 μM) and acyl-coenzyme A:cholesterol acyltransferase (ACAT; IC50 = 22.9 μM). It is also an antagonist of oxytocin receptors (IC50 = 67 μM). Penicillide inhibits RNA synthesis in P388 murine leukemia cells.
TN1086	Dehydrotrametenolic acid Dehydroeburicoic acid,去氢齿孔酸,松苓新酸	Apoptosis; TNF; NOS; Caspase; NO Synthase	Apoptosis; Immunology/Inflammation; Proteases/Proteasome
	Dehydrotrametenolic acid (Dehydroeburicoic acid) 是从茯苓的菌核中分离的一种甾醇，具有抗肿瘤活性、抗炎和抗糖尿病作用。它通过 caspase-3途径诱导细胞凋亡。

天然产物

Cat.No: T37753

Target: Cysteine Protease, Antibacterial

Isovalerylcarnitine

Cat.No: T19384

Target: Apoptosis, Cysteine Protease

Cat.No: T36931

Dehydrotrametenolic acid

Cat.No: TN1086

Synonym: Dehydroeburicoic acid,去氢齿孔酸,松苓新酸

Target: Apoptosis, TNF, NOS, Caspase, NO Synthase

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