HSP (HSP90)
信号通路图
研究领域
抑制剂选择性比较
HSP (HSP90)产品
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1141 |
Tanespimycin (17-AAG)Tanespimycin (17-AAG, CP127374, NSC-330507, KOS 953) 是一种有效的HSP90抑制剂，无细胞试验中IC50为5 nM，作用于来自肿瘤细胞的HSP90比作用于来自正常细胞HSP90结合亲和力高100倍。Tanespimycin (17-AAG)可诱导细胞凋亡、坏死、自噬和线粒体自噬。Phase 3。 |
SKBR3 cells were treated with FW-04-806 at 10, 20, 40 uM for 24 h; 17AAG was used as a positive control at 1 and 2 uM. Hsp70, Hsp90, and Cdc37 protein level were analyzed with western blotting using relevant antibodies.
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| S1069 |
Luminespib (NVP-AUY922)Luminespib (AUY-922, NVP-AUY922, VER-52296)是一种高效的HSP90抑制剂，无细胞试验中作用于HSP90α/β的IC50为13 nM /21 nM，对HSP90家族成员GRP94和TRAP-1具有稍弱的作用，与任何小分子HSP90配体均可紧密结合。Luminespib (AUY-922, NVP-AUY922)可有效下调并使IGF-1Rβ蛋白不稳定，从而导致抑制生长、自噬和凋亡。Phase 2。 |
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| S1142 |
Alvespimycin (17-DMAG) HClAlvespimycin (17-DMAG, NSC 707545, BMS 826476, KOS 1022) HCl是一种有效的HSP90抑制剂，无细胞试验中IC50为62 nM。 Phase 2。 |
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| S1159 |
Ganetespib (STA-9090)Ganetespib (STA-9090)是一种HSP90抑制剂，在OSA 8种细胞中IC50为4 nM，诱导OSA细胞凋亡，而不影响正常的成骨细胞；是STA-1474的活性代谢物。Phase 3。 |
Breast cancer (MDA-MB-231), pancreatic cancer (PaTu2), lung cancer (A549), colon cancer HCT-116, and acute myeloid leukemia (SKM1) cell lines were incubated with increasing amounts of PU-H71 and STA-9090 as indicated. Western blot analysis with PRKD2, cleaved PARP, and cleaved caspase-9 antibodies is depicted.
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| S9806New |
DTHIBDTHIB (Direct Targeted HSF1 InhiBitor) 是一种直接的 heat shock factor 1 (HSF1) 的选择性抑制剂，其Kd值为160 nM，用于DTHIB与HSF1 DNA结合域(DBD)的结合。DTHIB 具有强大的抗癌活性。 |
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| S7428New |
RocaglamideRocaglamide (Roc-A) 是从Aglaia物种中分离出来的一种有效的 heat shock factor 1 (HSF1) 活化的抑制剂，对HSF1的IC50值约为50 nM。Rocaglamide 可抑制翻译起始因子 eIF4A 的功能。Rocaglamide 还抑制 NF-κB 的活性。Rocaglamide 具有抗肿瘤活性。 |
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| S1175 |
BIIB021BIIB021 (CNF2024)是一种口服有效的，全部人工合成的，小分子HSP90抑制剂，Ki和EC50分别为1.7 nM和38 nM。Phase 2. |
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| S1163 |
Onalespib (AT13387)Onalespib (AT13387)是一种有效的，选择性Hsp90抑制剂，在A375细胞中IC50为18 nM，具有长持续性抗肿瘤活性。Phase 2。 |
IC50 determinations of compound S1 and S13 on heat shock poteins ATPase activity using ADP fluorescence assay. (A)
inhibition of HSP70 (B) inhibition of HSP90 The test compounds were diluted from mother plates (10 mM in 100% (v/v) DMSO) into series of
concentration (in 2.0% (v/v) DMSO). AT13387 and 17-DMAG were used as positive controls in each assay. Data were performed in triplicate and
analyzed by GraphPad.Prism.
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| S1498 |
NVP-BEP800NVP-BEP800 (VER82576) 是一种新型的，全部人工合成的HSP90β抑制剂，IC50为58 nM，比作用于Hsp90家族成员Grp94和Trap-1选择性高70倍以上。 |
Growth curves of the MPNST cell line S462 treated with two different HSP90 inhibitors (500nM IPI-504 and 500nM BEP800). |
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| S2713 |
Geldanamycin (NSC 122750)Geldanamycin (NSC 122750) 是一种天然的HSP90抑制剂，Kd为1.2 μM，特异性干扰糖皮质激素受体(GR)/HSP联合。Geldanamycin 通过减少宿主的炎症反应来减轻病毒感染引起的ALI(急性肺损伤)/ARDS(急性呼吸窘迫综合征)。 |
Phenotypic effect of Genetic or Pharmacologic Compromise of the 477 Hsp70-StiA-Hsp90 Complex. The impact of each genetic modification on radial growth, conidiation, and response to various stress conditions was assessed after inoculation of a suspension of 104 conidia on glucose minimal medium (GMM) agar plates and incubation at 37ºC for 5 days.
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| S2639 |
SNX-2112 (PF-04928473)SNX-2112 (PF-04928473)选择性结合到HSP90α和HSP90β的ATP结合袋中，Ka分别为30 nM和30 nM，比17-AAG更有效。 |
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| S2656 |
PF-04929113 (SNX-5422)PF-04929113 (SNX-5422)是一种有效的，选择性的HSP90抑制剂，Kd为41 nM，且诱导Her-2降解，IC50为37 nM。Phase 1/2。 |
Effect of SNX-2112 on E. histolytica morphology. Trophozoites were treated with 3 uM SNX-2112 for 48 h. (A) E. histolytica trophozoites treated with 0.5% DMSO. Arrow indicates live trophozoite. Magnification, x 10. (B) E. histolytica trophozoites treated with 3 uM SNX-2112. Treatment caused complete lysis of trophozoites (arrow). Magnification, x 10. Trophozoites were imaged under phase-contrast microscope.
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| S2685 |
KW-2478KW-2478是一种非Ansamycin的HSP90抑制剂，IC50为3.8 nM。Phase 1。 |
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| S7122 |
XL888XL888一种ATP竞争性的HSP90抑制剂，IC50为24 nM。Phase 1 |
B, XL888 (1 mmol/L, 144 hours) is effective at blocking the growth and survival of vemurafenib-resistant melanoma cell lines grown as 3D collagen-implanted spheroids. Staining shows cell viability, in which green corresponds to live cells and red: dead cells. Magnification×4.
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| S2930 |
Pifithrin-μPifithrin-μ (NSC 303580, PFTμ, 2-Phenylethynesulfonamide) 是一种特异性的p53抑制剂，通过降低其与Bcl-xL和Bcl-2的亲和力而发挥作用，也抑制HSP70功能和细胞自噬。 |
Effect of pifithrin-μ (the inhibitor of mitochondrial translocation of p53) on MEG3-induced apoptosis in TGF-β1-treated LX-2 cells. The inhibitor pifithrin-μ attenuated cleavage of caspase 3 which blocked apoptosis. The results are expressed as relative expression against control expression without treatment.
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| S7282 |
NMS-E973NMS-E973 是一种强效的选择性的Hsp90抑制剂，其结合于Hsp90的 DC50小于10 nM , 对一系列52种其他不同蛋白激酶没有抑制活性。 |
(D) Representative images of paraffin-embedded tumor sections were analyzed by active caspase-3 staining. (E) Representative images of paraffin-embedded tumor sections analyzed by TUNEL staining.
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| S8039 |
PU-H71PU-H71 (NSC 750424)是有效的选择性HSP90抑制剂，IC50为51 nM。 |
Effects of low-level HSP90 inhibition (by ganetespib, 2-5 nM; PU-H71, 40-70 nM) or febrile-range temperature (39 ℃) on HSP70 and HSP90 protein levels in FANCA wild-type cells. High-level HSP90 inhibition (ganetespib, 25 nM; PU-H71, 300 nM) as well as proteotoxic proteasomal inhibition (MG132, 2.5 mM) induced the expression of HSP70. Constitutive (upper band: C) and inducible forms (lower band: I) of HSP70 are indicated. HSP90 levels are shown for comparison.
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| S5369 |
EthoxyquinEthoxyquin (Santoquin, Santoflex, Quinol) is an antioxidant used as a food preservative. |
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| S8365 |
ApoptozoleApoptozole (Apoptosis Activator VII) 是热激蛋白HSP70和Hsc70的抑制剂，与HSP70和Hsc70的Kd值分别为0.14 μM和0.21 μM。它能够诱导caspase依赖性的凋亡反应。 |
Representative images of platelets preincubated with FITC-conjugated CD41 before treated with negative control, pitstop 2, dynasore, A23, or apoptozole spreading on immobilized Fg for 10, 30, and 60 minutes, respectively. Images were taken under oil immersion with magnification × 100. Scale bar, 5 μm.
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| S8402 |
KRIBB11KRIBB11 抑制热激诱导的荧光素酶活性，IC50为1.2 μM。它是转录因子热休克因子1(HSF1)的抑制剂。KRIBB11 可诱导生长阻滞和凋亡。 |
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| S7750 |
KNK437KNK437 是一种泛-HSP 抑制剂，其抑制诱导型HSPs，包括 HSP105，HSP72，和 HSP40的合成。 |
Western blots of lysates from BaF3 JAK2 V617F cells.
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| S7458 |
VER-49009VER-49009 (CCT0129397) 是一种强效的HSP90抑制剂，其IC50为 47 nM。 |
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| S7716 |
TAS-116TAS-116是一种新型的HSP90小分子抑制剂，HSP90α和HSP90β的Ki值分别为34.7 nmol/L和21.3 nmol/L。TAS-11并不抑制其他ATP酶，如HSP70(IC50 >200 μmol/L)。 |
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| S7340 |
CH5138303CH5138303 是口服有效的Hsp90抑制剂，其Kd为 0.48 nM。 |
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| S7459 |
VER-50589VER-50589 是强效的HSP90抑制剂，对HSP90β的IC50为21 nM。 |
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| S3604 |
Triptolide (PG490)Triptolide (PG490, NSC 163062)是一种三环氧二萜类化合物,是从中草药雷公藤中提取的免疫抑制剂。它是一种NF-κB抑制剂，抑制NF-κB转录活性，破坏p65/CBP的相互作用，减少p65蛋白。Triptolide (PG490) 可抑制 heat shock transcription factor 1 (HSF1) 的反式激活。Triptolide 可抑制 MDM2 并通过一个p53非依赖性通路来诱导凋亡。 |
Spironolactone (sp.) and triptolide inhibit NER in myeloma cells. RPMI8226 cells were incubated with dimethyl sulfoxide (DMSO), spironolactone (10 μm) or triptolide (1 μm) for 6 h before NER evaluation. The figure represents the persistence of DNA-damage signal 150 min after exposure to UV (AFU: arbitrary fluorescent unit). Figure 4a shows representative merged pictures of DAPI and DDB2 proteo-probe signal (b).
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| S7751 |
VER155008VER155008 (C07)是一种有效的Hsp70家族抑制剂，无细胞试验中对HSP70，HSC70，和 GRP78 (HSPA5, Bip) 的IC50分别为0.5 μM，2.6 μM，和 2.6 μM，比作用于HSP90选择性高100多倍。VER155008 可抑制自噬并导致HSP90客户蛋白水平降低。 |
(D) Microglial cultures treated with 300 μM H2O2 alone or 100 μM SNAP plus 300 μM H2O2 for 24 h in the absence or presence of a chemical inhibitor (20 μM VER-155008 or 20 μM SnPP) were subjected to the determination of cell viability (MTT reduction assay). ∗p < 0.05 vs. H2O2 (300 μM) alone. +p < 0.05 vs. SNAP (100 μM) plus H2O2 (300 μM). |
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| S6721 |
JG98JG-98 是 Hsp70 的变构抑制剂，它与Hsp70家族成员保守的深袋紧密结合。JG-98 可诱导经典的凋亡特征，包括与程序性细胞死亡和膜联蛋白染色阳性相符的形态变化。JG-98 具有抗癌的活性。 |
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| S7097 |
HSP990 (NVP-HSP990)HSP990 (NVP-HSP990) 是一种新型有效的选择性 HSP90抑制剂，对HSP90α/β的IC50分别为0.6 nM和0.8 nM。NVP-HSP990可诱导细胞周期阻滞和凋亡。 |
Expression of CD24 and CD44 in HSP90 inhibitor‐treated, shRNA‐transduced HCC1937 cells was analyzed by flow cytometry.
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| S1972 |
Tamoxifen (ICI 46474) CitrateTamoxifen Citrate (ICI 46474) 是一种雌激素受体 estrogen receptor 调节剂 (SERM)，通过竞争性抑制雌激素结合发挥作用。Tamoxifen Citrate 也是一种有效的 Hsp90 激活剂，可增强Hsp90分子伴侣ATPase的活性。Tamoxifen 可诱导凋亡与自噬。 |
Effects of DPN, LY500307, Raloxifene and Tamoxifen on cell viability in BSO-treated FRDA fibroblasts. BSO concentration was 1 mM and all steroid concentrations were 100 nM. Depicted are mean ± SD for n= 8 per group. * indicated p<0.05 versus BSO alone-treated cells. |
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| S0279 |
DimethylenastronDimethylenastron 是一种有效的、特异性的、可逆的 kinesin Eg5 (kinesin-5/kinesin spindle protein, KSP) 抑制剂，其IC50值为200 nM。Dimethylenastron 可诱导人多发性骨髓瘤细胞的有丝分裂停滞和凋亡并上调 Hsp70 的表达。 |
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| S0294 |
HSF1AHSF1A 是一种可透过细胞的 heat shock transcription factor 1 (HSF1) 的激活剂。HSF1A 可保护细胞免受压力诱导的凋亡，结合TRiC亚基并抑制TRiC活性，而不会干扰ATP水解。 |
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| S6568 |
ML346ML346是Hsp70激活剂，是一种新型的蛋白质稳定状态调节剂。 |
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| S1238 |
Tamoxifen (ICI 46474)Tamoxifen (ICI 46474, (Z)-Tamoxifen, trans-Tamoxifen) 作用于乳腺组织，是一种雌激素受体estrogen receptor调节剂 (SERM)。Tamoxifen可增强Hsp90分子伴侣ATPase的活性。Tamoxifen可诱导凋亡。 |
E, Analysis of BrCSC viability upon treatment with tamoxifen (tam) and fulvestrant (fulv) at the indicated doses. The experiments were performed in triplicates. ** P<0.01. |
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| S1052 |
Elesclomol (STA-4783)Elesclomol (STA-4783)是一种新型有效的oxidative stress诱导剂，在肿瘤细胞中引起促凋亡作用。Phase 3。 |
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| S8305 |
TRC051384TRC051384是heat shock protein 70 (HSP70)的诱导物，同时也是有效的抗炎药。 |
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| S8299 |
HA15HA15 是一种特异靶向 HSPA5 (Heat shock 70kDa protein 5) 也可称为 BiP (Immunoglobulin heavy-chain-binding protein) 或 Grp78 (glucose-regulated protein 78) 的小分子。在所检测的黑色素瘤细胞中具有抗肿瘤活性，包括从病人中分离得到的细胞和对BRAF抑制剂具有耐药性的细胞。 |
SP cells in inhibitor-treated, shRNA-transduced HCC1937 cells analyzed by flow cytometry using Hoechst 33342 dye. Data are shown as mean±SD. ****P<.0001, ***P<.001, **P<.01, *P<.05.
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| S5006 |
TeprenoneTeprenone，也被称作tetraprenylacetone或geranylgeranylacetone，是一种抗溃疡药，在临床上用于治疗胃炎。 |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1141 |
Tanespimycin (17-AAG)Tanespimycin (17-AAG, CP127374, NSC-330507, KOS 953) 是一种有效的HSP90抑制剂，无细胞试验中IC50为5 nM，作用于来自肿瘤细胞的HSP90比作用于来自正常细胞HSP90结合亲和力高100倍。Tanespimycin (17-AAG)可诱导细胞凋亡、坏死、自噬和线粒体自噬。Phase 3。 |
SKBR3 cells were treated with FW-04-806 at 10, 20, 40 uM for 24 h; 17AAG was used as a positive control at 1 and 2 uM. Hsp70, Hsp90, and Cdc37 protein level were analyzed with western blotting using relevant antibodies.
|
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| S1069 |
Luminespib (NVP-AUY922)Luminespib (AUY-922, NVP-AUY922, VER-52296)是一种高效的HSP90抑制剂，无细胞试验中作用于HSP90α/β的IC50为13 nM /21 nM，对HSP90家族成员GRP94和TRAP-1具有稍弱的作用，与任何小分子HSP90配体均可紧密结合。Luminespib (AUY-922, NVP-AUY922)可有效下调并使IGF-1Rβ蛋白不稳定，从而导致抑制生长、自噬和凋亡。Phase 2。 |
|
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| S1142 |
Alvespimycin (17-DMAG) HClAlvespimycin (17-DMAG, NSC 707545, BMS 826476, KOS 1022) HCl是一种有效的HSP90抑制剂，无细胞试验中IC50为62 nM。 Phase 2。 |
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| S1159 |
Ganetespib (STA-9090)Ganetespib (STA-9090)是一种HSP90抑制剂，在OSA 8种细胞中IC50为4 nM，诱导OSA细胞凋亡，而不影响正常的成骨细胞；是STA-1474的活性代谢物。Phase 3。 |
Breast cancer (MDA-MB-231), pancreatic cancer (PaTu2), lung cancer (A549), colon cancer HCT-116, and acute myeloid leukemia (SKM1) cell lines were incubated with increasing amounts of PU-H71 and STA-9090 as indicated. Western blot analysis with PRKD2, cleaved PARP, and cleaved caspase-9 antibodies is depicted.
|
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| S9806New |
DTHIBDTHIB (Direct Targeted HSF1 InhiBitor) 是一种直接的 heat shock factor 1 (HSF1) 的选择性抑制剂，其Kd值为160 nM，用于DTHIB与HSF1 DNA结合域(DBD)的结合。DTHIB 具有强大的抗癌活性。 |
||
| S7428New |
RocaglamideRocaglamide (Roc-A) 是从Aglaia物种中分离出来的一种有效的 heat shock factor 1 (HSF1) 活化的抑制剂，对HSF1的IC50值约为50 nM。Rocaglamide 可抑制翻译起始因子 eIF4A 的功能。Rocaglamide 还抑制 NF-κB 的活性。Rocaglamide 具有抗肿瘤活性。 |
||
| S1175 |
BIIB021BIIB021 (CNF2024)是一种口服有效的，全部人工合成的，小分子HSP90抑制剂，Ki和EC50分别为1.7 nM和38 nM。Phase 2. |
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| S1163 |
Onalespib (AT13387)Onalespib (AT13387)是一种有效的，选择性Hsp90抑制剂，在A375细胞中IC50为18 nM，具有长持续性抗肿瘤活性。Phase 2。 |
IC50 determinations of compound S1 and S13 on heat shock poteins ATPase activity using ADP fluorescence assay. (A)
inhibition of HSP70 (B) inhibition of HSP90 The test compounds were diluted from mother plates (10 mM in 100% (v/v) DMSO) into series of
concentration (in 2.0% (v/v) DMSO). AT13387 and 17-DMAG were used as positive controls in each assay. Data were performed in triplicate and
analyzed by GraphPad.Prism.
|
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| S1498 |
NVP-BEP800NVP-BEP800 (VER82576) 是一种新型的，全部人工合成的HSP90β抑制剂，IC50为58 nM，比作用于Hsp90家族成员Grp94和Trap-1选择性高70倍以上。 |
Growth curves of the MPNST cell line S462 treated with two different HSP90 inhibitors (500nM IPI-504 and 500nM BEP800). |
|
| S2713 |
Geldanamycin (NSC 122750)Geldanamycin (NSC 122750) 是一种天然的HSP90抑制剂，Kd为1.2 μM，特异性干扰糖皮质激素受体(GR)/HSP联合。Geldanamycin 通过减少宿主的炎症反应来减轻病毒感染引起的ALI(急性肺损伤)/ARDS(急性呼吸窘迫综合征)。 |
Phenotypic effect of Genetic or Pharmacologic Compromise of the 477 Hsp70-StiA-Hsp90 Complex. The impact of each genetic modification on radial growth, conidiation, and response to various stress conditions was assessed after inoculation of a suspension of 104 conidia on glucose minimal medium (GMM) agar plates and incubation at 37ºC for 5 days.
|
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| S2639 |
SNX-2112 (PF-04928473)SNX-2112 (PF-04928473)选择性结合到HSP90α和HSP90β的ATP结合袋中，Ka分别为30 nM和30 nM，比17-AAG更有效。 |
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| S2656 |
PF-04929113 (SNX-5422)PF-04929113 (SNX-5422)是一种有效的，选择性的HSP90抑制剂，Kd为41 nM，且诱导Her-2降解，IC50为37 nM。Phase 1/2。 |
Effect of SNX-2112 on E. histolytica morphology. Trophozoites were treated with 3 uM SNX-2112 for 48 h. (A) E. histolytica trophozoites treated with 0.5% DMSO. Arrow indicates live trophozoite. Magnification, x 10. (B) E. histolytica trophozoites treated with 3 uM SNX-2112. Treatment caused complete lysis of trophozoites (arrow). Magnification, x 10. Trophozoites were imaged under phase-contrast microscope.
|
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| S2685 |
KW-2478KW-2478是一种非Ansamycin的HSP90抑制剂，IC50为3.8 nM。Phase 1。 |
||
| S7122 |
XL888XL888一种ATP竞争性的HSP90抑制剂，IC50为24 nM。Phase 1 |
B, XL888 (1 mmol/L, 144 hours) is effective at blocking the growth and survival of vemurafenib-resistant melanoma cell lines grown as 3D collagen-implanted spheroids. Staining shows cell viability, in which green corresponds to live cells and red: dead cells. Magnification×4.
|
|
| S2930 |
Pifithrin-μPifithrin-μ (NSC 303580, PFTμ, 2-Phenylethynesulfonamide) 是一种特异性的p53抑制剂，通过降低其与Bcl-xL和Bcl-2的亲和力而发挥作用，也抑制HSP70功能和细胞自噬。 |
Effect of pifithrin-μ (the inhibitor of mitochondrial translocation of p53) on MEG3-induced apoptosis in TGF-β1-treated LX-2 cells. The inhibitor pifithrin-μ attenuated cleavage of caspase 3 which blocked apoptosis. The results are expressed as relative expression against control expression without treatment.
|
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| S7282 |
NMS-E973NMS-E973 是一种强效的选择性的Hsp90抑制剂，其结合于Hsp90的 DC50小于10 nM , 对一系列52种其他不同蛋白激酶没有抑制活性。 |
(D) Representative images of paraffin-embedded tumor sections were analyzed by active caspase-3 staining. (E) Representative images of paraffin-embedded tumor sections analyzed by TUNEL staining.
|
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| S8039 |
PU-H71PU-H71 (NSC 750424)是有效的选择性HSP90抑制剂，IC50为51 nM。 |
Effects of low-level HSP90 inhibition (by ganetespib, 2-5 nM; PU-H71, 40-70 nM) or febrile-range temperature (39 ℃) on HSP70 and HSP90 protein levels in FANCA wild-type cells. High-level HSP90 inhibition (ganetespib, 25 nM; PU-H71, 300 nM) as well as proteotoxic proteasomal inhibition (MG132, 2.5 mM) induced the expression of HSP70. Constitutive (upper band: C) and inducible forms (lower band: I) of HSP70 are indicated. HSP90 levels are shown for comparison.
|
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| S5369 |
EthoxyquinEthoxyquin (Santoquin, Santoflex, Quinol) is an antioxidant used as a food preservative. |
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| S8365 |
ApoptozoleApoptozole (Apoptosis Activator VII) 是热激蛋白HSP70和Hsc70的抑制剂，与HSP70和Hsc70的Kd值分别为0.14 μM和0.21 μM。它能够诱导caspase依赖性的凋亡反应。 |
Representative images of platelets preincubated with FITC-conjugated CD41 before treated with negative control, pitstop 2, dynasore, A23, or apoptozole spreading on immobilized Fg for 10, 30, and 60 minutes, respectively. Images were taken under oil immersion with magnification × 100. Scale bar, 5 μm.
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| S8402 |
KRIBB11KRIBB11 抑制热激诱导的荧光素酶活性，IC50为1.2 μM。它是转录因子热休克因子1(HSF1)的抑制剂。KRIBB11 可诱导生长阻滞和凋亡。 |
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| S7750 |
KNK437KNK437 是一种泛-HSP 抑制剂，其抑制诱导型HSPs，包括 HSP105，HSP72，和 HSP40的合成。 |
Western blots of lysates from BaF3 JAK2 V617F cells.
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| S7458 |
VER-49009VER-49009 (CCT0129397) 是一种强效的HSP90抑制剂，其IC50为 47 nM。 |
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| S7716 |
TAS-116TAS-116是一种新型的HSP90小分子抑制剂，HSP90α和HSP90β的Ki值分别为34.7 nmol/L和21.3 nmol/L。TAS-11并不抑制其他ATP酶，如HSP70(IC50 >200 μmol/L)。 |
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| S7340 |
CH5138303CH5138303 是口服有效的Hsp90抑制剂，其Kd为 0.48 nM。 |
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| S7459 |
VER-50589VER-50589 是强效的HSP90抑制剂，对HSP90β的IC50为21 nM。 |
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| S3604 |
Triptolide (PG490)Triptolide (PG490, NSC 163062)是一种三环氧二萜类化合物,是从中草药雷公藤中提取的免疫抑制剂。它是一种NF-κB抑制剂，抑制NF-κB转录活性，破坏p65/CBP的相互作用，减少p65蛋白。Triptolide (PG490) 可抑制 heat shock transcription factor 1 (HSF1) 的反式激活。Triptolide 可抑制 MDM2 并通过一个p53非依赖性通路来诱导凋亡。 |
Spironolactone (sp.) and triptolide inhibit NER in myeloma cells. RPMI8226 cells were incubated with dimethyl sulfoxide (DMSO), spironolactone (10 μm) or triptolide (1 μm) for 6 h before NER evaluation. The figure represents the persistence of DNA-damage signal 150 min after exposure to UV (AFU: arbitrary fluorescent unit). Figure 4a shows representative merged pictures of DAPI and DDB2 proteo-probe signal (b).
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| S7751 |
VER155008VER155008 (C07)是一种有效的Hsp70家族抑制剂，无细胞试验中对HSP70，HSC70，和 GRP78 (HSPA5, Bip) 的IC50分别为0.5 μM，2.6 μM，和 2.6 μM，比作用于HSP90选择性高100多倍。VER155008 可抑制自噬并导致HSP90客户蛋白水平降低。 |
(D) Microglial cultures treated with 300 μM H2O2 alone or 100 μM SNAP plus 300 μM H2O2 for 24 h in the absence or presence of a chemical inhibitor (20 μM VER-155008 or 20 μM SnPP) were subjected to the determination of cell viability (MTT reduction assay). ∗p < 0.05 vs. H2O2 (300 μM) alone. +p < 0.05 vs. SNAP (100 μM) plus H2O2 (300 μM). |
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| S6721 |
JG98JG-98 是 Hsp70 的变构抑制剂，它与Hsp70家族成员保守的深袋紧密结合。JG-98 可诱导经典的凋亡特征，包括与程序性细胞死亡和膜联蛋白染色阳性相符的形态变化。JG-98 具有抗癌的活性。 |
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| S7097 |
HSP990 (NVP-HSP990)HSP990 (NVP-HSP990) 是一种新型有效的选择性 HSP90抑制剂，对HSP90α/β的IC50分别为0.6 nM和0.8 nM。NVP-HSP990可诱导细胞周期阻滞和凋亡。 |
Expression of CD24 and CD44 in HSP90 inhibitor‐treated, shRNA‐transduced HCC1937 cells was analyzed by flow cytometry.
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| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1972 |
Tamoxifen (ICI 46474) CitrateTamoxifen Citrate (ICI 46474) 是一种雌激素受体 estrogen receptor 调节剂 (SERM)，通过竞争性抑制雌激素结合发挥作用。Tamoxifen Citrate 也是一种有效的 Hsp90 激活剂，可增强Hsp90分子伴侣ATPase的活性。Tamoxifen 可诱导凋亡与自噬。 |
Effects of DPN, LY500307, Raloxifene and Tamoxifen on cell viability in BSO-treated FRDA fibroblasts. BSO concentration was 1 mM and all steroid concentrations were 100 nM. Depicted are mean ± SD for n= 8 per group. * indicated p<0.05 versus BSO alone-treated cells. |
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| S0279 |
DimethylenastronDimethylenastron 是一种有效的、特异性的、可逆的 kinesin Eg5 (kinesin-5/kinesin spindle protein, KSP) 抑制剂，其IC50值为200 nM。Dimethylenastron 可诱导人多发性骨髓瘤细胞的有丝分裂停滞和凋亡并上调 Hsp70 的表达。 |
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| S0294 |
HSF1AHSF1A 是一种可透过细胞的 heat shock transcription factor 1 (HSF1) 的激活剂。HSF1A 可保护细胞免受压力诱导的凋亡，结合TRiC亚基并抑制TRiC活性，而不会干扰ATP水解。 |
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| S6568 |
ML346ML346是Hsp70激活剂，是一种新型的蛋白质稳定状态调节剂。 |
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| S1238 |
Tamoxifen (ICI 46474)Tamoxifen (ICI 46474, (Z)-Tamoxifen, trans-Tamoxifen) 作用于乳腺组织，是一种雌激素受体estrogen receptor调节剂 (SERM)。Tamoxifen可增强Hsp90分子伴侣ATPase的活性。Tamoxifen可诱导凋亡。 |
E, Analysis of BrCSC viability upon treatment with tamoxifen (tam) and fulvestrant (fulv) at the indicated doses. The experiments were performed in triplicates. ** P<0.01. |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1052 |
Elesclomol (STA-4783)Elesclomol (STA-4783)是一种新型有效的oxidative stress诱导剂，在肿瘤细胞中引起促凋亡作用。Phase 3。 |
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| S8305 |
TRC051384TRC051384是heat shock protein 70 (HSP70)的诱导物，同时也是有效的抗炎药。 |
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| S8299 |
HA15HA15 是一种特异靶向 HSPA5 (Heat shock 70kDa protein 5) 也可称为 BiP (Immunoglobulin heavy-chain-binding protein) 或 Grp78 (glucose-regulated protein 78) 的小分子。在所检测的黑色素瘤细胞中具有抗肿瘤活性，包括从病人中分离得到的细胞和对BRAF抑制剂具有耐药性的细胞。 |
SP cells in inhibitor-treated, shRNA-transduced HCC1937 cells analyzed by flow cytometry using Hoechst 33342 dye. Data are shown as mean±SD. ****P<.0001, ***P<.001, **P<.01, *P<.05.
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| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S5006 |
TeprenoneTeprenone，也被称作tetraprenylacetone或geranylgeranylacetone，是一种抗溃疡药，在临床上用于治疗胃炎。 |
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