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19

抑制剂 & 化合物

2

天然产物

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Cat. No. Product Name Target Signaling Pathways
T17011 TCH-165

Proteasome Proteases/Proteasome; Ubiquitination
TCH-165 是一种蛋白酶体组装的小分子调节剂,可增加游离 20S 水平,进而增强 IDP 蛋白水解。
T8362 Benzamidine hydrochloride

Benzamidine HCl,苄脒盐酸盐

Serine/threonin kinase; Serine Protease Cell Cycle/Checkpoint; Metabolism; Proteases/Proteasome
Benzamidine hydrochloride (Benzamidine HCl) 是可逆的胰蛋白酶样丝氨酸蛋白酶 (trypsin-like serine proteases) 竞争性抑制剂,对 uPA、类胰蛋白酶、胰蛋白酶和 Xa 因子作用的Ki 分别为 97 µM、20 µM、21 µM 和 110 µM。
T7016 VR23

Apoptosis; Proteasome; Caspase Apoptosis; Proteases/Proteasome; Ubiquitination
VR23 是一种蛋白酶体抑制剂,对胰蛋白酶样蛋白酶体、糜蛋白酶样蛋白酶体和半胱天冬酶样蛋白酶体的 IC50 分别是1 nM、50-100 nM 和3 μM。
T2122 Ixazomib

艾沙佐米,MLN2238

Proteasome; Caspase; Autophagy Apoptosis; Autophagy; Proteases/Proteasome; Ubiquitination
Ixazomib (MLN2238) 含硼肽蛋白酶体抑制剂(PI),可抑制 20S 蛋白酶体的糜蛋白酶样蛋白水解 (β5) 位点,IC50为 3.4 nM,Ki 为 0.93 nM。它还抑制半胱天冬酶样 (β1) 和胰蛋白酶样 (β2) 蛋白水解位点,IC50值为 31和3500 nM。
T63321 20S Proteasome activator 1

Proteasome Proteases/Proteasome; Ubiquitination
20S Proteasome activator 1 是一种 20S 蛋白酶激活剂,对胰蛋白酶样位点、胰凝乳蛋白酶样位点和半胱天冬酶位点的 IC50 分别为 0.3 μM、0.7 μM 和 1.8 μM。20S Proteasome activator 1 通过在细胞系统中翻译来防止致病性 α-synuclein A53T 突变体积累从而减少疾病发生的概率。20S Proteasome activator 1 可用于研究神经退行性疾病。
T6941 PI-1840

PI 1840

PARP; Proteasome Chromatin/Epigenetic; DNA Damage/DNA Repair; Proteases/Proteasome; Ubiquitination
PI-1840 是一种高效的、选择性的蛋白酶体chymotrypsin-like (CT-L)抑制剂,IC50=27nM。
T16169 N-alpha-Tosyl-L-lysine chloromethyl ketone hydrochloride

N-alpha-Tosyl-L-lysine_chloromethyl_ketone_hydrochloride

Others; Proteasome; COX Immunology/Inflammation; Neuroscience; Others; Proteases/Proteasome; Ubiquitination
N-alpha-Tosyl-L-lysine chloromethyl ketone hydrochloride (N-alpha-Tosyl-L-lysine_chloromethyl_ketone_hydrochloride) 是胰蛋白酶样蛋白酶的抑制剂。 N-alpha-Tosyl-L-lysine chloromethyl ketone hydrochloride 对 IFN-γ 活性具有抑制作用。
T78409L Boc-Val-Pro-Arg-MCA TFA

Boc-Val-Pro-Arg-MCA TFA 是一种敏感性荧光底物,是凝血酶底物,可用于测定胰蛋白酶样丝氨酸蛋白酶活性。
T2391 Camostat mesylate

FOY-S980,甲磺酸卡莫司他,FOY305,Camostat mesilate

Serine/threonin kinase; SARS-CoV; Sodium Channel Cell Cycle/Checkpoint; Membrane transporter/Ion channel; Metabolism; Microbiology/Virology
Camostat mesylate (FOY-S980) 是口服活性合成的丝氨酸蛋白酶抑制剂,用于慢性胰腺炎。它是TMPRSS2的抑制剂,对SARS-CoV-2具有抗病毒活性。它抑制前列腺素、胰蛋白酶和苦参多糖的活性。
T78409 Boc-Val-Pro-Arg-MCA hydrochloride

Boc-Val-Pro-Arg-MCA HCl

Boc-Val-Pro-Arg-MCA hydrochloride (Boc-Val-Pro-Arg-MCA HCl) 为测定胰蛋白酶样丝氨酸蛋白酶 (trypsin-like serine proteases) 活性的敏感荧光底物。
T19580 Thrombin (MW 37kDa)

凝血酶,Thrombin

Thrombin Proteases/Proteasome
Thrombin (MW 37kDa) 是一种 Na+激活的胰蛋白酶样别构丝氨酸蛋白酶。它能够利用凝血酶识别序列对融合蛋白进行位点特异性切割,并可用于消化 GST 标记的蛋白。
T37011 Boc-LRR-AMC

Boc-LRR-AMC is a fluorogenic substrate for the trypsin-like activity of the 26S proteasome or 20S proteolytic core. Upon enzymatic cleavage by the 26S proteasome or 20S proteolytic core, amino-4-methylcoumarin (AMC) is released and its fluorescence can be used to quantify 26S proteasome or 20S proteolytic core trypsin-like activity. AMC displays excitation/emission maxima of 340-360/440-460 nm, respectively.
T77221 Benzenecarboximidamide, hydrochloride, hydrate (1:1:x)

Benzenecarboximidamide, hydrochloride, hydrate (1:1:x) (Benzamidine hydrochloride hydrate) 是一种可逆的竞争性胰蛋白酶样丝氨酸蛋白酶 (trypsin-like serine proteases) 抑制剂,对 Tryptase、Trypsin、uPA、Factor Xa、Thrombin 和 tPA 的Ki 值分别为 20、21、97、110、320 和 750 μM。
T39029 APC-6860

APC-6860 is a trypsin-like serine proteases inhibitor with k i values of 0.21, 0.44, 1.5, 16.8, 20, 30 μM for uPA, trypsin, tryptase, tPA, thrombin and factor Xa, respectively. APC-6860 has a selectivity ratio for tPA versus uPA of 80. APC-6860 has k i values of 0.1, 0.082 μM for human and murine urokinases, respectively. APC-6860 can be used for the research of cancer.
T80211 Ac-KQL-AMC

Ac-KQL-AMC是量化蛋白酶体样活性的荧光底物,其被裂解时释放可检测的荧光信号。
T78625 Z-Ala-Arg-Arg-AMC

Z-ARR-AMC,Fluorogenic Proteasome Substrate

Proteasome Proteases/Proteasome; Ubiquitination
Z-Ala-Arg-Arg-AMC (FluorogenicProteasomeSubstrate) 作为荧光底物,专用于检测蛋白酶体中的胰蛋白酶样活性。
TP2234 coagulation factor II (thrombin) B chain fragment [Homo sapiens]

Others Others
Thrombin is a "trypsin-like" serine protease that is encoded by the F2 gene in humans. Thrombin is produced by the enzymatic cleavage of two sites on prothrombin by activated Factor X (Xa). Thrombin in turn acts as a serine protease that converts soluble
T38052 CRA-2059 TFA

CRA-2059 is a highly specific and selective tryptase inhibitor, with a Ki of 620 pM for recombinant human tryptase-β (rHTβ)[1][2]. Tryptase is a trypsin-like serine protease found as a major protein component in human mast cell secretory granules. CRA-2059 has the potential for inflammatory bowel disease research[1]. [1]. Tremaine WJ, et al. Treatment of mildly to moderately active ulcerative colitis with a tryptase inhibitor (APC 2059): an open-label pilot study. Aliment Pharmacol Ther. 2002;16...
T38051 CRA-2059 hydrochloride

CRA-2059 hydrochloride is a highly specific and selective tryptase inhibitor, with a Ki of 620 pM for recombinant human tryptase-β (rHTβ)[1][2]. Tryptase is a trypsin-like serine protease found as a major protein component in human mast cell secretory granules. CRA-2059 hydrochloride has the potential for inflammatory bowel disease research[1]. [1]. Tremaine WJ, et al. Treatment of mildly to moderately active ulcerative colitis with a tryptase inhibitor (APC 2059): an open-label pilot study. Ali...

化合物

TCH-165
Cat.No: T17011
Synonym:
Target: Proteasome
Benzamidine hydrochloride
Cat.No: T8362
Synonym: Benzamidine HCl,苄脒盐酸盐
Target: Serine/threonin kinase, Serine Protease
VR23
Cat.No: T7016
Synonym:
Target: Apoptosis, Proteasome, Caspase
Ixazomib
Cat.No: T2122
Synonym: 艾沙佐米,MLN2238
Target: Proteasome, Caspase, Autophagy
20S Proteasome activator 1
Cat.No: T63321
Synonym:
Target: Proteasome
PI-1840
Cat.No: T6941
Synonym: PI 1840
Target: PARP, Proteasome
N-alpha-Tosyl-L-lysine chloromethyl ketone hydrochloride
Cat.No: T16169
Synonym: N-alpha-Tosyl-L-lysine_chloromethyl_ketone_hydrochloride
Target: Others, Proteasome, COX
Boc-Val-Pro-Arg-MCA TFA
Cat.No: T78409L
Synonym:
Target:
Camostat mesylate
Cat.No: T2391
Synonym: FOY-S980,甲磺酸卡莫司他,FOY305,Camostat mesilate
Target: Serine/threonin kinase, SARS-CoV, Sodium Channel
Boc-Val-Pro-Arg-MCA hydrochloride
Cat.No: T78409
Synonym: Boc-Val-Pro-Arg-MCA HCl
Target:
Thrombin (MW 37kDa)
Cat.No: T19580
Synonym: 凝血酶,Thrombin
Target: Thrombin
Boc-LRR-AMC
Cat.No: T37011
Synonym:
Target:
Benzenecarboximidamide, hydrochloride, hydrate (1:1:x)
Cat.No: T77221
Synonym:
Target:
APC-6860
Cat.No: T39029
Synonym:
Target:
Ac-KQL-AMC
Cat.No: T80211
Synonym:
Target:
Z-Ala-Arg-Arg-AMC
Cat.No: T78625
Synonym: Z-ARR-AMC,Fluorogenic Proteasome Substrate
Target: Proteasome
coagulation factor II (thrombin) B chain fragment [Homo sapiens]
Cat.No: TP2234
Synonym:
Target: Others
CRA-2059 TFA
Cat.No: T38052
Synonym:
Target:
CRA-2059 hydrochloride
Cat.No: T38051
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T16012 Marizomib

NPI-0052,Salinosporamide A,ML858

Proteasome Proteases/Proteasome; Ubiquitination
Marizomib (ML858) 是一种新型不可逆的脑渗透性泛蛋白酶体 (proteasome) 抑制剂,对 20S 蛋白酶体的 CT-L (β5)、CT-T-laspase 样 (C-L, β1) 和胰蛋白酶样 (T-L, β2) 具有抑制作用, IC50 分别为 3.5, 28, 430 nM。
T6S0071 Fraxinellone

HIF/HIF Prolyl-Hydroxylase; STAT; PD-1/PD-L1 Apoptosis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Immunology/Inflammation; JAK/STAT signaling; Metabolism; Stem Cells
Fraxinellone 是从白鲜的根皮中分离出来的一种天然产物,是PD-L1抑制剂,可抑制HIF-1α蛋白质合成。它通过靶向 PD-L1,有用于癌症免疫的潜力。

天然产物

Marizomib
Cat.No: T16012
Synonym: NPI-0052,Salinosporamide A,ML858
Target: Proteasome
Fraxinellone
Cat.No: T6S0071
Synonym:
Target: HIF/HIF Prolyl-Hydroxylase, STAT, PD-1/PD-L1
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