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13

抑制剂 & 化合物

2

天然产物

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Cat. No. Product Name Target Signaling Pathways
T67897 GRP78-IN-3

HSP Cytoskeletal Signaling; Metabolism
GRP78-IN-3(化合物8)是一种有效的Hsp70底物结合的小分子竞争性抑制剂,是一种选择性的Grp78 (HSPA5)抑制剂,IC50为0.59 μM。GRP78-IN-3对HspA5的选择性是HspA9的7倍(IC50为4.3 μM),对HspA5的选择性是HspA2的20倍(IC50为13.9 μM)。
T63243 GRP78-IN-2

GRP78-IN-2 是葡萄糖调节蛋白 78 (GRP78) 抑制剂,能够优先靶向细胞表面 GRP78,具有显著的的抗血管生成和抗癌作用,且不影响其他正常细胞。
T61106 GRP78-IN-1

GRP78-IN-1 displays interactions with specific residues on the GRP78 protein with a binding energy of -8.07 kcal/mol. This compound possesses potent cytotoxic and anti-proliferative effects on cancer cells, particularly demonstrating promising apoptosis in breast cancer cells and wound healing properties [1].
T30480 BiP inducer X

BIX

Apoptosis Apoptosis
BiP inducer X (BIX) 是免疫球蛋白重链结合蛋白 (BiP)/GRP78 的选择性诱导剂和 ER 伴侣诱导剂。 BiP inducer X 可防止神经元和视网膜细胞系中的细胞死亡。
T8901 YUM70

Apoptosis; GPR; HSP Apoptosis; Cytoskeletal Signaling; Endocrinology/Hormones; GPCR/G Protein; Metabolism
YUM70 是一种选择性葡萄糖调节蛋白 78 抑制剂,抑制全长蛋白的 GRP78 ATPase 活性的IC50值为 1.5 μM。它在胰腺癌中诱导内质网应激介导的细胞凋亡。
T7010 VER-155008

VER155008

GPR; HSP; Autophagy Autophagy; Cytoskeletal Signaling; Endocrinology/Hormones; GPCR/G Protein; Metabolism
VER-155008 是一种Hsp70的抑制剂,对Hsp70、Hsc70 和 Grp7 的IC50值分别为 0.5 μM、2.6 μM 和 2.6 μM,对Hsp70的Kd 值为 0.3 μM,比 HSP90 选择性高 100 倍以上。
T67717L Questiomycin A derivatives 18 TFA

Questiomycin A derivatives 18 TFA 是一种Questiomycin A 衍生物,Questiomycin A 具有抗菌和抗癌活性 ,对细胞保护性 ER 伴侣蛋白 GRP78 的表达具有抑制作用。
T6855 HA15

Apoptosis; GPR; Others; HSP; Autophagy Apoptosis; Autophagy; Cytoskeletal Signaling; Endocrinology/Hormones; GPCR/G Protein; Metabolism; Others
HA15 是一种高效特异性内质网伴侣蛋白BiP/GRP78/HSPA5抑制剂,抑制 BiP 的 ATP 酶活性,具有抗肿瘤活性。
T38471 HM03 trihydrochloride

HM03 trihydrochloride is a potent and selective inhibitor of HSPA5, also known as Bip or Grp78. It exhibits anticancer activity.
T39423 Palmitic acid-13C sodium

Sodium palmitate-13C is the 13C-labeled variant of palmitic acid, a long-chain saturated fatty acid prevalent in animals and plants. This compound has been shown to induce the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer-binding protein homologous protein (CHOP) in mouse granulosa cells.
T40980 Palmitic acid-13C2

Palmitic acid-13C2

Palmitic acid-13C2 is the 13C-labeled Palmitic acid. Palmitic acid is a long-chain saturated fatty acid commonly found in both animals and plants. Palmitic acid can induce the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer binding protein homologous protein (CHOP) in in mouse granulosa cells.
T40141 Palmitic acid-13C16 sodium

Palmitic acid-13C16 sodium

Palmitic acid-13C16 sodium, a 13C-labeled form of the naturally occurring saturated fatty acid Palmitic acid sodium, is prevalent in animals and plants. This compound can trigger the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer binding protein homologous protein (CHOP) in mouse granulosa cells.
T72543 BOLD-100 free base

NKP-1339 free base ; IT-139 free base ; KP-1339 free base,KP-1339 free base,NKP-1339 free base,IT-139 free base

BOLD-100 (NKP-1339; IT-139) free base 是一款钌基抗癌药物。作为GRP78应激诱导上调的抑制剂,它破坏内质网(ER)的稳态,从而诱发ER应激和未折叠蛋白反应(UPR)。此外,BOLD-100 free base 干预了内质网应激反应、溶酶体动力学以及细胞自噬(autophagy)间的复杂交互作用。

化合物

GRP78-IN-3
Cat.No: T67897
Synonym:
Target: HSP
GRP78-IN-2
Cat.No: T63243
Synonym:
Target:
GRP78-IN-1
Cat.No: T61106
Synonym:
Target:
BiP inducer X
Cat.No: T30480
Synonym: BIX
Target: Apoptosis
YUM70
Cat.No: T8901
Synonym:
Target: Apoptosis, GPR, HSP
VER-155008
Cat.No: T7010
Synonym: VER155008
Target: GPR, HSP, Autophagy
Questiomycin A derivatives 18 TFA
Cat.No: T67717L
Synonym:
Target:
HA15
Cat.No: T6855
Synonym:
Target: Apoptosis, GPR, Others, HSP, Autophagy
HM03 trihydrochloride
Cat.No: T38471
Synonym:
Target:
Palmitic acid-13C sodium
Cat.No: T39423
Synonym:
Target:
Palmitic acid-13C2
Cat.No: T40980
Synonym: Palmitic acid-13C2
Target:
Palmitic acid-13C16 sodium
Cat.No: T40141
Synonym: Palmitic acid-13C16 sodium
Target:
BOLD-100 free base
Cat.No: T72543
Synonym: NKP-1339 free base ; IT-139 free base ; KP-1339 free base,KP-1339 free base,NKP-1339 free base,IT-139 free base
Target:
Cat. No. Product Name Target Signaling Pathways
T36818 Questiomycin A

GPR; Antibacterial Endocrinology/Hormones; GPCR/G Protein; Microbiology/Virology
Questiomycin A 是一种在鲜奶油中生产的抗生素,具有抗菌和抗癌活性。 Questiomycin A 抑制细胞保护性 ER 伴侣蛋白 GRP78 的表达。
TN2371 Isoliquiritin

新异甘草苷,Neoisoliquiritin

Others Others
Neoisoliquiritigenin, isolated from Spatholobus suberectus, inhibits cell proliferation and induces cell apoptosis in breast cancer by directly binding to GRP78 to regulate the β-catenin pathway

天然产物

Questiomycin A
Cat.No: T36818
Synonym:
Target: GPR, Antibacterial
Isoliquiritin
Cat.No: TN2371
Synonym: 新异甘草苷,Neoisoliquiritin
Target: Others
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