Search Result
Results for "
HSPs
" in MedChemExpress (MCE) Product Catalog:
4
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-W014102
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-
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- HY-B0779A
-
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(5E,9E,13E)-Geranylgeranylacetone
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HSP
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Metabolic Disease
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(5E,9E,13E)-Teprenone ((5E,9E,13E)-Geranylgeranylacetone) is an isomer of Teprenone with antiulcer activity. (5E,9E,13E)-Teprenone induces transcriptional activation of HSP genes that may increase gastric mucosal defense at conditions of stress .
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- HY-100110
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KNK437
2 Publications Verification
Heat Shock Protein Inhibitor I
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HSP
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Cancer
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KNK437 is a HSP inhibitor, and inhibits the induction of HSP105, HSP70, and HSP40.
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- HY-113574
-
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HSP
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Cancer
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HSP90-IN-29 (Compound 13), a benzoxazole derivative, is a potent and selective HSP-90 inhibitor with an IC50 value of 30 nM. HSP90-IN-29 has antitumor activity .
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- HY-19399
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(-)-BRX 005; (-)-BRX 235
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p38 MAPK
HSP
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Cardiovascular Disease
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Iroxanadine (BRX 005) is a vasculoprotector. Iroxanadine is a p38 kinase and HSP protein dual activator. Iroxanadine has the potential for atherosclerosis and vascular diseases research .
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- HY-19399D
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(-)-BRX 005 hydrochloride; (-)-BRX 235 hydrochloride
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p38 MAPK
HSP
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Cardiovascular Disease
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Iroxanadine (BRX 005) hydrochloride is a vasculoprotector. Iroxanadine is a p38 kinase and HSP protein dual activator. Iroxanadine hydrochloride has the potential for atherosclerosis and vascular diseases research .
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- HY-19399C
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(-)-BRX 005 hydrobromide; (-)-BRX 235 hydrobromide
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p38 MAPK
HSP
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Cardiovascular Disease
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Iroxanadine hydrobromide (BRX 005) is a vasculoprotector. Iroxanadine is a p38 kinase and HSP protein dual activator. Iroxanadine hydrobromide has the potential for atherosclerosis and vascular diseases research .
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- HY-19399A
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BRX 005; BRX 235
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p38 MAPK
HSP
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Cardiovascular Disease
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(±)-Iroxanadine (BRX 005; BRX 235), a vasculoprotector, is a p38 kinase and HSP protein activator. (±)-Iroxanadine has the potential for atherosclerosis and vascular diseases research .
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- HY-W014102R
-
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Endogenous Metabolite
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Metabolic Disease
Inflammation/Immunology
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L-Alanyl-L-glutamine (Standard) is the analytical standard of L-Alanyl-L-glutamine. This product is intended for research and analytical applications. L-Alanyl-L-glutamine, a glutamine dipeptide, is benefit for the antioxidant system, attenuating inflammation, and may modulate the heat shock protein (HSP) response in catabolic situations .
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- HY-167827
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HSP
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Cancer
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Hsp90-IN-34 (compound HAM-1) is a compound that inhibits the Aha1-Hsp90 chaperone complex with a high affinity for Hsp90/Aha1 (KDapp=23.5 µM). Hsp90-IN-34 modulates the ATPase activity of Hsp90 by affecting the interaction between Hsp90 and Aha1 .
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- HY-151337
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- HY-152027
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- HY-152028
-
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HSP
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Infection
Neurological Disease
Inflammation/Immunology
Cancer
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HSP90-IN-19 is an effective heat shock protein 90 (Hsp90) inhibitor. HSP90-IN-19 has effective Hsp90 inhibitory activity with an IC50 value of 0.27 μM. HSP90-IN-19 can be used for the research of viral infection, neurodegenerative disease, and inflammation .
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- HY-144724
-
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HSP
Apoptosis
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Cancer
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HSP90-IN-10 (Compound 16s) is a potent inhibitor of HSP90. HSP90-IN-10 exhibits high antiproliferative potency against HCC1954 breast cancer cells with the IC50 value of 6 µM. HSP90-IN-10 does not inhibit the growth of normal epithelial cells. HSP90-IN-10 also induces apoptosis .
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- HY-146325
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HSP
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Cancer
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HSP90-IN-11 (Compound 12c) is a potent inhibitor of HSP90. HSP90-IN-11 displays potent HSP90α inhibition comparable to AUY-922 (Luminespib). HSP90-IN-11 shows significant antiproliferative activity in CRC and NSCLC cells in a double digit nM range. HSP90-IN-11 leads to rapid degradation of client proteins EGFR and Akt in NSCLC cells. HSP90-IN-11 induces significant accumulation of a sub-G1 phase population .
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- HY-150655
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HSP
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Cancer
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Hsp90-IN-15 is an Hsp90 inhibitor with anticancer activity. Hsp90-IN-15 induces cell apoptosis, arrests the cell cycle at S phase and decreases the expression level of Hsp90 in Hela cell .
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- HY-18406
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HSP
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Cancer
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HSP70-IN-4 (Compound YM-01) is an Hsp70 inhibitor with an IC50 of 3.2 μM. HSP70-IN-4 is not BBB permeable .
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- HY-149531
-
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HSP
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Cancer
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HSP90-IN-25 (compound 4a) is an HSP90 inhibitor that specifically inhibits the ATPase activity of HSP90 .
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- HY-148963
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HSP
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Cancer
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HSP90-IN-20 (compound 78p) is a potent HSP90 inhibitor with an IC50 of ≤10 μM. HSP90-IN-20 has the potential for cancers research .
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- HY-145814
-
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HSP
Fungal
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Infection
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HSP90-IN-9 is a potent and selective HSP90 inhibitor. HSP90-IN-9 displays a fungicidal effect in a dose-dependent manner. HSP90-IN-9 inhibits fungal biofilm formation and fungal morphological changes after being combined with FLC. HSP90-IN-9 recovers FLC resistance by down-regulating the expression of related genes (ERG11, CDR1 and CDR2) .
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- HY-168205
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HSP
Apoptosis
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Cancer
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HSP90-IN-33 (compound 24e) is a potent Hsp90 inhibitor with Kd values of ≥200, 7.3 µM for Hsp90α, Hsp90β, respectively. HSP90-IN-33 induces apoptosis and cell cycle arrest at G0/G1 phase. HSP90-IN-33 decreases the protein expression of ERα, CDK4 and Akt .
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- HY-149891
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HSP
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Cancer
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HSP90-IN-23 (Comp 12-1) is an inhibitor of heat shock protein 90(HSP90) with an IC50 of 9 nM. HSP90-IN-23 induces apoptosis of tumor cells and arrests the tumor cell cycle in G0/G1 phase. HSP90-IN-23 can be used for cancer research .
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- HY-W854649
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HSP
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Cancer
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[Au(TPP)]Cl inhibits the refolding activity of the Hsp60-Hsp10 complex with significant anticancer activities .
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![[Au(TPP)]Cl](//file.medchemexpress.eu/product_pic/hy-w854649.gif)
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- HY-156779
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HSP
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Cancer
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HSP90-IN-27 (compound 19) is an HSP90 inhibitor .
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- HY-151137
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mTOR
HSP
Apoptosis
Autophagy
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Cancer
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HSP90/mTOR-IN-1 is a potent and orally active Hsp90 and mTOR inhibitor with IC50 values of 69 nM and 29 nM, respectively. HSP90/mTOR-IN-1 suppresses the proliferation of SW780 cells through the over-activation of the PI3K/AKT/mTOR pathway. HSP90/mTOR-IN-1 induces apoptosis and autophagy via selective Hsp90 and mTOR inhibition. HSP90/mTOR-IN-1 also has considerable in vivo anti-tumor activity. HSP90/mTOR-IN-1 can be used for researching bladder cancer .
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- HY-159484
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HSP
Guanylate Cyclase
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Cardiovascular Disease
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Hsp110/sGC-modulator-1 (compound 17i), an orally active Hsp110/sGC dual-target regulator, exhibits optimal Hsp110 and sGC molecular activities as well as remarkable cell malignant phenotypes inhibitory and vasodilatory effects. Hsp110/sGC-modulator-1 (compound 17i) attenuates pulmonary vascular remodeling and right ventricular hypertrophy via Hsp110 suppression .
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- HY-144650
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Apoptosis
HSP
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Cancer
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Hsp90-Cdc37-IN-3 (Compound 9) is a novel celastrol−imidazole derivative with anticancer activity. Hsp90-Cdc37-IN-3 inhibits Hsp90−Cdc37 by covalent-binding, and induces apoptosis .
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- HY-120909
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HSP
Apoptosis
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Cancer
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YK5 is a potent and selective Hsp70 inhibitor. YK5 selectively and tightly binds to the cytosolic Hsp70s in cancer cells. YK5 has biological activity partly by interfering with the formation of active oncogenic Hsp70/Hsp90/client protein complexes .
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- HY-168178
-
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HSP
STAT
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Cardiovascular Disease
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Hsp110-STAT3 interaction-IN-2 (compound 10b) is a Hsp110-STAT3 interaction disruptor. Hsp110-STAT3 interaction-IN-2 can be used in pulmonary arterial hypertension (PAH) related research .
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- HY-161427
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HSP
HIF/HIF Prolyl-Hydroxylase
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Cancer
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HSP90-IN-30 (compound 3e) inhibits HSP90 chaperone activity. HSP90-IN-30 inhibits the activity of HIF-1 transcriptional under hypoxia with an IC50 value of 2.16 μM .
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- HY-111414
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HSP
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Cancer
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Hsp90-Cdc37-IN-1 is an Hsp90-Cdc37 interaction disruptor that inhibit cell migration and reverse agent resistance, with an IC50 of 140 nM.
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- HY-163288
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Histone Methyltransferase
HSP
Apoptosis
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Cancer
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EZH2/HSP90-IN-29 is a dual inhibitor for EZH2 and HSP90, with IC50s of 6.29 nM and 60.1 nM, for EZH2 and HSP90, respectively. EZH2/HSP90-IN-29 increases apoptosis/necrosis-related gene expression, induces cell cycle arrest at M phase and inhibits reactive oxygen species (ROS) catabolism pathway. EZH2/HSP90-IN-29 is able to cross the blood-brain-barrier (BBB) .
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- HY-158131
-
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FKBP
HSP
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Neurological Disease
Cancer
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FKBP51-Hsp90-IN-2 (Compound E08) is a selective FKBP51-Hsp90 protein-protein interaction inhibitor with IC50 values of 0.4 µM and 5 µM for FKBP51 and FKBP52, respectively. FKBP51-Hsp90-IN-2 also effectively stimulates cellular energy metabolism and neurite growth. FKBP51-Hsp90-IN-2 can be used in research on neurodegenerative diseases and cancer .
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- HY-149637
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Sirtuin
HSP
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Cancer
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HSP70/SIRT2-IN-1 (Compounds 2a) is a dual inhibitor for SIRT2 and HSP70, with IC50 of 17.3±2.0 μM for SIRT2. HSP70/SIRT2-IN-1 has antitumor activity .
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- HY-149638
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Sirtuin
HSP
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Cancer
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HSP70/SIRT2-IN-2 (Compounds 1a) is a dual inhibitor for SIRT2 and HSP70, with IC50 of 45.1±5.0 μM for SIRT2. HSP70/SIRT2-IN-2 has antitumor activity .
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- HY-15190
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HSP-990
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HSP
Apoptosis
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Cancer
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NVP-HSP990 is a potent, selective and orally active Hsp90 inhibitor, with IC50 values of 0.6, 0.8, and 8.5 nM for Hsp90α, Hsp90β, and Grp94, respectively.
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- HY-10214
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PF-04928473
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HSP
Autophagy
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Cancer
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SNX-2112 (PF 04928473) is an orally active Hsp90 inhibitor, with a Kd of 16 nM for Hsp90 and IC50s of 30 nM, 30 nM for Hsp90 α and Hsp90 β, also induces Her-2 degradation, and inhibits Grp94 and Trap-1, with IC50s of 10 nM, 4.275 μM and 0.862 μM, respectively . SNX-2112 (PF 04928473) binds Hsp90 isoforms Hsp90α, Hsp90β and Hsp90b1/Grp94 with Kds of 4 nM, 6 nM and 484 nM, respectively .
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- HY-150774
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HDAC
HSP
Apoptosis
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Cancer
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HDAC6/HSP90-IN-2 (compound 6e) is a dual inhibitor of HDAC6 and Hsp90, with IC50s of 105.7 and 61 nM, respectively. HDAC6/HSP90-IN-2 can be used for the research of cancer .
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- HY-146228
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HSP
Apoptosis
Topoisomerase
EGFR
VEGFR
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Cancer
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HSP90-IN-13 (compound 5k) is a highly potent HSP90 pan inhibitor with an IC50 value of 25.07 nM. HSP90-IN-13 has multi-target activity against EGFR, VEGFR-2 and Topoisomerase-2. HSP90-IN-13 causes cell cycle arrest at G2/M phase and induces apoptosis of MCF-7 cells through mitochondrial-mediated pathway .
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- HY-151335
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HSP
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Cancer
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KU-177 is a potent inhibitor of Hsp90 ATPase homologue 1 (Aha1), ablates Aha1-driven enhancement of Hsp90-dependent tau aggregation. KU-177 also disrupts Aha1/Hsp90 interactions (IC50=4.08 μM) without inhibition of Hsp90’s ATPase activity. KU-177 can be used for tauopathies research .
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- HY-169098
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HSP
Histone Demethylase
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Cancer
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HSP90/LSD1-IN-1 (compound 6) is a HSP90/LSD1 dual inhibitor. HSP90/LSD1-IN-1 inhibits the proliferation of prostate cancer cell lines PC-3 and DU145, with GI50 values of 0.24 and 0.30 μM, respectively .
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- HY-148215
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HSP
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Cancer
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Hsp90-IN-17 (Example 5) is an HSP90 inhibitor that can be used in the study of proliferative diseases, such as cancer and neurodegenerative diseases .
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- HY-148215A
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HSP
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Cancer
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Hsp90-IN-17 (Example 5) hydrochloride is an HSP90 inhibitor that can be used in the study of proliferative diseases, such as cancer and neurodegenerative diseases .
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- HY-158130
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FKBP
HSP
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Neurological Disease
Metabolic Disease
Cancer
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FKBP51-Hsp90-IN-1 (Compound D10) is a selective inhibitor of the FKBP51-Hsp90 protein-protein interaction, with an IC50 value of 0.1 μM against FKBP51. FKBP51-Hsp90-IN-1 can be used in the research of stress-related diseases, Alzheimer's disease, and metabolic disorders .
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- HY-12622
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HSP
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Cancer
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HSP70-IN-1 is a heat shock protein (HSP) inhibitor; inhibits the growth of Kasumi-1 cells with an IC50 of 2.3 μM.
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- HY-146212
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HDAC
HSP
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Cancer
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These compounds have strong hdac and hsp90 inhibitory activities. Compound 20 (HDAC ic50 = 194 nm; Hsp90 α < b> Ic50 = 153 nm) and compound 26 ((HDAC ic50= 360 nm; Hsp90 α < b> Ic50 = 77 nm) shows the strongest HDAC and HSP90 α Inhibitory activity. Both compounds can induce hsp90 expression and down regulate hsp90 client proteins, which play an important role in regulating the survival and invasion of cancer cells.
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- HY-163854
-
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HSP
Bcl-2 Family
Apoptosis
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Cancer
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HSP70-IN-6 (Compound JL-15) is an inhibitor of Hsp70-Bim protein-protein interaction (PPI) (IC50: 70 nM). HSP70-IN-6 induces apoptosis in chronic myeloid leukemia (CML) cells, with EC50s of 0.43 μM(BV173), 0.88 μM (K562), 0.19 μM (K562-R3) .
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- HY-146293
-
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HDAC
HSP
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Cancer
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HDAC6/HSP90-IN-1 (compound 17) is a potent and selective dual inhibitor of HDAC6 and HSP90, with IC50 values of 4.3 and 46.8 nM, respectively. HDAC6/HSP90-IN-1 down-regulates PD-L1 expression in INF-γ treated H1975 lung cancer cells. HDAC6/HSP90-IN-1 inhibits tumor growth in human H1975 xenograft mice .
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- HY-10215
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VER-52296; AUY922; NVP-AUY922
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HSP
Autophagy
Apoptosis
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Cancer
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Luminespib (VER-52296) is a potent HSP90 inhibitor with IC50s of 7.8 and 21 nM for HSP90α and HSP90β, respectively .
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- HY-P1896
-
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HSP
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Infection
Neurological Disease
Cancer
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Hsp70-derived octapeptide is a conserved octapeptide of the C-terminal end of Hsp70, which physically interacts with tetratricopeptide repeat (TPR) motifs .
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- HY-13469
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CUDC-305
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HSP
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Cancer
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Debio 0932 (CUDC-305) is an orally active HSP90 inhibitor, with IC50s of 100 and 103 nM for HSP90α and HSP90β, respectively .
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- HY-124653
-
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J2
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HSP
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Cancer
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HSP27 inhibitor J2 (J2) is a HSP27 inhibitor, which significantly induces abnormal HSP27 dimer formation and inhibits a production of HSP27 giant polymers, thereby having an effect of inhibiting a chaperone function of the HSP27 and reducing a cell protection function thereof. HSP27 inhibitor J2 (J2) remarkably enhances the antiproliferative activity of 17-AAG and sensitizes cisplatin-induced lung cancer cell growth inhibition .
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- HY-126601
-
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Parasite
HSP
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Infection
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Malonganenone A is an antimalarial marine alkaloid that disrupts the interaction between PfHsp70-x and Hsp40. Malonganenone A inhibits plasmodial and not human Hsp70 ATPase activity (Hsp40-stimulated), and hindered the aggregation suppression activity of PfHsp70-x .
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- HY-18669
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ML346
3 Publications Verification
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HSP
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Cancer
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ML346 is an activator of Hsp70 expression and HSF-1 activity, with an EC50 of 4.6 μM for Hsp70. ML346 restores protein folding in conformational disease models, without significant cytotoxicity or lack of specificity. ML346 induces specific increases in genes and protein effectors of the heat shock response (HSR), including chaperones such as Hsp70, Hsp40, and Hsp27 .
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- HY-162900
-
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HSP
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Cancer
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HSP90-IN-32 is a Hsp90 C-terminal inhibitor that displays anti-proliferative activities against SKMel173, SKMel103, SKMel19 and A375 cells with IC50 values of 1.01 μM, 0.782 μM, 0.607 μM and 1.413 μM , respectively. HSP90-IN-32 is promising for research of anti-cancer agents .
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- HY-107599
-
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JNK
Apoptosis
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Neurological Disease
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AEG3482 is a potent antiapoptotic compound that inhibits Jun kinase (JNK) activity through induced expression of heat shock protein 70 (HSP70). AEG3482 directly binds HSP90, thereby facilitating HSF1-dependent expression of HSP70 and HSP25 .
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- HY-161833
-
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Interleukin Related
TNF Receptor
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Inflammation/Immunology
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HSP90-IN-31 (compound Be01) causes reduction of CD80 and CD86 expression on dendritic cells (DCs). HSP90-IN-31 decreases the production of pro-inflammatory cytokines (IL-6, TNF-α, and IL-1β) in BMDC and peritoneal macrophages stimulated by LPS (HY-D1056). Under the delayed-type hypersensitivity (DTH) mice model, HSP90-IN-31 reduces ear swelling and pro-inflammatory cytokines in the spleen .
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- HY-130624
-
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HSP
Apoptosis
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Cancer
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Hsp90-Cdc37-IN-2 (Compound 41) is an inhibitor for the interaction between heat shock protein 90 (Hsp90) and cyclin 37 (Cdc37). Hsp90-Cdc37-IN-2 inhibits the proliferation of cancer cell A549, MCF-7, HOS and HepG2 with IC50 of 0.41-0.94 μM. Hsp90-Cdc37-IN-2 decreases the mitochondrial membrane potential, induces apoptosis, and arrest cell cycle at G0/G1 phase in A549 .
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- HY-125759
-
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HSP
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Cancer
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3-Phenyltoxoflavin, a derivative of Toxoflavin, is an Hsp90 inhibitor, with a Kd of 585 nM for the interaction of Hsp90-TPR2A. 3-Phenyltoxoflavin has anti-cancer activity .
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- HY-143400
-
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HSP
Hedgehog
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Cancer
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HSP70-IN-3 is a potent HSP70 inhibitor (IC50s of 1.1 and 1.9 μM in ASZ001 and C3H10T1/2, respectively). HSP70-IN-3 has anti-Hh (Hedgehog signaling) activity and anti-proliferative activity and reduces expression of the oncogenic transcription factor GLI1 .
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- HY-10210
-
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IPI-504
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HSP
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Cancer
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Retaspimycin Hydrochloride is a potent inhibitor of Hsp90 with EC50s of 119 nM for both Hsp90 and Grp9.
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- HY-10389
-
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17-DMAG; KOS-1022; NSC 707545
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HSP
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Cancer
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Alvespimycin (17-DMAG) is a potent inhibitor of Hsp90, binding to Hsp90 with an EC50 of 62 ± 29 nM.
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- HY-15263
-
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HSP
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Cancer
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Retaspimycin is a potent inhibitor of Hsp90, with EC50s of 119 nM for both Hsp90 and Grp9.
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- HY-15785
-
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TAS-116
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HSP
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Cancer
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Pimitespib (TAS-116) is an oral bioavailable, ATP-competitive, highly specific HSP90α/HSP90β inhibitor (Kis of 34.7 nM and 21.3 nM, respectively) without inhibiting other HSP90 family proteins such as GRP94 . Pimitespib demonstrates less ocular toxicity .
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- HY-147974
-
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HSP
Influenza Virus
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Infection
|
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HSP90-IN-14 (compound 4) is a potent Hsp90 (heat shock protein 90) inhibitor, with a Kd of 0.26 μM. HSP90-IN-14 shows anti-influenza virus activity in MDCK cells, with EC50 values of 2.6, 3.9, and 17 μM for influenza A/H3N2, A/H1N1, and B, respectively .
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- HY-115997
-
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PROTACs
HSP
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Cancer
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PROTAC HSP90 degrader BP3 is a potent and selective degradation of HSP90 in a CRBN-dependent fashion. PROTAC HSP90 degrader BP3 has a certain degradation effect on HSP90 protein in MCF-7 cells (DC50=0.99 μM). PROTAC HSP90 degrader BP3 inhibits the growth of breast cancer cell . PROTAC HSP90 degrader BP3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-117282
-
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HSP
Apoptosis
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Cancer
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JG-98, an allosteric heat shock protein 70 (Hsp70) inhibitor, which binds tightly to a conserved site on Hsp70 and disrupts the Hsp70-Bag3 interaction. JG-98 shows anti-cancer activities affecting both cancer cells and tumor-associated macrophages .
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- HY-10941
-
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HSP
Autophagy
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Neurological Disease
Cancer
|
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VER-155008 is an inhibitor of Hsp70, with IC50s of 0.5 μM, 2.6 μM, and 2.6 μM for Hsp70, Hsc70 and Grp7, respectively, and with a Kd of 0.3 μM for Hsp70.
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- HY-153588
-
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HSP
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Cancer
|
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HSP90-IN-22 (Compound 35) is an Hsp90 inhibitor with antiproliferative properties on cells with IC50 values of 3.65 μM for MCF7 breast cancer cells and 2.71 μM for SKBr3 breast cancer cells, respectively.
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- HY-12024
-
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17-DMAG hydrochloride; KOS-1022 hydrochloride; BMS 826476
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HSP
Apoptosis
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Cancer
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Alvespimycin hydrochloride (17-DMAG hydrochloride; KOS-1022; BMS 826476) is a potent inhibitor of Hsp90, binding to Hsp90 with EC50 of 62±29 nM.
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- HY-145722A
-
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OGX-427
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HSP
|
Cancer
|
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Apatorsen is an antisense oligonucleotide designed to bind to Hsp27 mRNA, resulting in the inhibition of the production of Hsp27 protein.
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- HY-12619
-
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HSP
|
Cancer
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DMT003096 is a HSP70 inhibitor. HSP70 has been reported to be upregulated in various cancers including breast, lung, colon, and cervix .
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- HY-12933
-
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HSP
|
Cancer
|
|
BIIB-028 is an orally active inhibitor for heat shock protein 90 (Hsp90). BIIB-028 targets the ATP-binding site of Hsp90, disrupts the function of Hsp90, leads to the degradation of client proteins, that are crucial for cancer cell survival and proliferation .
|
-
- HY-145722
-
|
OGX-427 sodium
|
HSP
|
Cancer
|
|
Apatorsen (sodium) is an antisense oligonucleotide designed to bind to Hsp27 mRNA, resulting in the inhibition of the production of Hsp27 protein.
|
-
- HY-155577
-
|
|
Monoamine Oxidase
HSP
|
Cancer
|
|
MAO A/HSP90-IN-1 (4-b) is a MAO A/HSP90 dual inhibitor with IC50 value of 1.77 μM and 0.019 μM in Glioblastoma (GBM) GL26 cells and HSP90α, respectively. MAO A/HSP90-IN-1 (4-b) can inhibit MAO A activity, HSP90 binding and the expression of HER2 and phospho-Akt to inhibit the growth of GBM, they also reduce PD-L1 expression, which inhibits T cell activation. MAO A/HSP90-IN-1 (4-b) have potential to inhibit tumor immune escape. MAO A/HSP90-IN-1 (4-b) can be used for brain tumor-related diseases research .
|
-
- HY-124805
-
|
|
HSP
|
Cancer
|
|
MAL3-101 is a potent HSP70 allosteric inhibitor. MAL3-101 inhibits HSP70 ATPase activity by blocking Hsp40 co-chaperone interaction. MAL3-101 can be used for researching muscle invasive bladder cancer (MIBC) .
|
-
- HY-130851
-
|
|
HSP
|
Cancer
|
|
HS-27, a fluorescently-tethered Hsp90 inhibitor, assays surface Hsp90 expression on intact tissue specimens. HS-27 is made up of the core elements of SNX-5422, an Hsp90 inhibitor, tethered via a PEG linker to a fluorescein derivative (fluorescein isothiocyanate or FITC), that binds to ectopically expressed Hsp90. HS-27 has potential use in a see-and-treat paradigm in breast cancer .
|
-
- HY-119906
-
|
FW-04-806
|
HSP
Apoptosis
|
Cancer
|
|
Conglobatin (FW-04-806), a macrolide dilactone, is isolated from the culture of Streptomyces conglobatus. Conglobatin is an orally active Hsp90 inhibitor. Conglobatin can bind to the N-terminal domain of Hsp90 and disrupt Hsp90-Cdc37 complex formation. Conglobatin induces apoptosis in human breast cancer cells and esophageal squamous cell carcinoma cells, and exhibits antitumor activity in vivo .
|
-
- HY-N0754
-
|
|
HSP
|
Inflammation/Immunology
|
|
Eupalinolide A, isolated from Eupatorium lindleyanum, induces the expression of HSP70 via the activation of HSF1 by inhibiting the interaction between HSF1 and HSP90 .
|
-
- HY-162008
-
|
|
HSP
Bcl-2 Family
|
Cancer
|
|
S1g-10 is a Hsp70/Bim inhibitor, and shows antitumor activity in chronic myeloid leukemia cells .
|
-
- HY-P10072A
-
|
Hsp25 kinase inhibitor acetate; Mk2 pseudosubstrate acetate
|
JNK
HSP
MAPKAPK2 (MK2)
p38 MAPK
ERK
|
Others
|
|
MK2-IN-5 (Hsp25 kinase inhibitor) acetate is a Mk2 pseudosubstrate (Ki= 8 μM). MK2-IN-5 acetate targets the protein interaction domain in the MAPK pathway. MK2-IN-5 acetate inhibits HSP25 and HSP27 phosphorylation .
|
-
- HY-11038D
-
|
PU-H71 formic
|
HSP
|
Cancer
|
|
Zelavespib formic (PU-H71 formic) is a potent Hsp90 inhibitor with an IC50 value of 51 nM for Hsp90 in MDA-MB-468 cells .
|
-
- HY-139301
-
|
|
HSP
|
Cancer
|
|
DDO-5936 is a potent and specific Hsp90-Cdc37 PPI inhibitor. DDO-5936 can be used for the research of colorectal cancer .
|
-
- HY-144694
-
|
|
HSP
HDAC
Fungal
|
Infection
|
|
HDAC/HSP90-IN-3 (compound J5) is a potent and selective fungal Hsp90 and HDAC dual inhibitor, with IC50 values of 0.83 and 0.91 μM, respectively. HDAC/HSP90-IN-3 shows antifungal activity against azole resistant C. albicans. HDAC/HSP90-IN-3 can suppress important virulence factors and down-regulate drug-resistant genes ERG11 and CDR1 .
|
-
- HY-124817
-
Col003
5 Publications Verification
|
HSP
|
Inflammation/Immunology
|
|
Col003 is a selective and potent inhibitor of Hsp47 and competitively binds to the collagen binding site on Hsp47 (IC50=1.8 μM). Col003 discourages the interaction of Hsp47 with collagen and inhibits collagen secretion by destabilizing the collagen triple helix. Col003 can be used for the investigation of fibrosis
|
-
- HY-107577
-
|
|
HSP
|
Infection
Inflammation/Immunology
Cancer
|
|
Gedunin is a limonoid with anti-cancer, anti-viral, anti-inflammatory and insecticidal activities. Gedunin acts as a potent Hsp90 inhibitor and induces the degradation of Hsp90-dependent client proteins. Geduni may obstructs the entry of SARS-CoV-2 virus into human host cells and can be used for COVID-19 research .
|
-
- HY-106723
-
|
|
HSP
|
Cancer
|
|
AMP-PCP is an ATP analogue and can bind to Hsp90 N-terminal domain with a Kd value of 3.8 μM. AMP-PCP binding favors the formation of the active homodimer of Hsp90 .
|
-
- HY-155113
-
|
|
PROTACs
HSP
|
Cancer
|
|
PROTAC Hsp90α degrader 1 (Compound X10g) is a selective PROTAC Hsp90α degrader. PROTAC Hsp90α degrader 1 can be used for breast cancer research. PROTAC Hsp90α degrader 1 inhibits the proliferation of MDA-MB-231, MDA-MB-468, MCF-7, MX-1 cells with IC50s of 51.48 μM, 16.46 μM, 8.93 μM, 11.95 μM respectively .
|
-
- HY-155580
-
|
|
Monoamine Oxidase
HSP
|
Cancer
|
|
MAO A/HSP90-IN-2 (compound 4-C) is a dual inhibitor of HSP90and MAO A with the IC50 values of 0.016 and 4.58 μM, respectively. MAO A/HSP90-IN-2 increases HSP70 expression and reduces HER2 and phospho-Akt expression, and decreases IFN-γ induced PD-L1 expression in GL26 cells. MAO A/HSP90-IN-2 inhibits the growth of Temozolomide (HY-17364) -sensitive and -resistant GBM cells, colon cancer, leukemia, non-small cell lung and other cancers, and has potential to inhibit tumor immune escape [1].
|
-
- HY-133705
-
|
|
HSP
|
Others
|
|
Geldanamycin-FITC, a Geldanamycin fluorescent probe, can be used in a fluorescence polarization assay for HSP90 inhibitors. Geldanamycin-FITC also can be used for detection of cell surface HSP90 .
|
-
- HY-Q43097
-
|
|
Others
|
Cardiovascular Disease
|
|
Row174336 (compound 29) is a potent inhibitor of Hsp110-STAT3 interaction that shows antiproliferative activity against HPAEC cell line, with the IC50 of 22.67 μM .
|
-
- HY-106723A
-
|
|
HSP
|
Cancer
|
|
AMP-PCP disodium is an ATP analogue and can bind to Hsp90 N-terminal domain with a Kd value of 3.8 μM. AMP-PCP disodium binding favors the formation of the active homodimer of Hsp90 .
|
-
- HY-114413
-
|
|
HSP
Apoptosis
|
Cancer
|
|
YZ129 is an inhibitor of the HSP90-calcineurin-NFAT pathway against glioblastoma, directly binding to heat shock protein 90 (HSP90) with an IC50 of 820 nM on NFAT nuclear translocation. YZ129-induced GBM cell-cycle arrest at the G2/M phase promotes apoptosis and inhibited tumor cell proliferation and migration .
|
-
- HY-RS06415
-
|
|
Small Interfering RNA (siRNA)
|
Others
|
|
HSP90AA1 Human Pre-designed siRNA Set A contains three designed siRNAs for HSP90AA1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
HSP90AA1 Human Pre-designed siRNA Set A
HSP90AA1 Human Pre-designed siRNA Set A
- HY-RS06416
-
|
|
Small Interfering RNA (siRNA)
|
Others
|
|
Hsp90aa1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Hsp90aa1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
Hsp90aa1 Mouse Pre-designed siRNA Set A
Hsp90aa1 Mouse Pre-designed siRNA Set A
- HY-RS06417
-
|
|
Small Interfering RNA (siRNA)
|
Others
|
|
Hsp90aa1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Hsp90aa1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
Hsp90aa1 Rat Pre-designed siRNA Set A
Hsp90aa1 Rat Pre-designed siRNA Set A
- HY-RS06418
-
|
|
Small Interfering RNA (siRNA)
|
Others
|
|
HSP90AB1 Human Pre-designed siRNA Set A contains three designed siRNAs for HSP90AB1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
HSP90AB1 Human Pre-designed siRNA Set A
HSP90AB1 Human Pre-designed siRNA Set A
- HY-RS06419
-
|
|
Small Interfering RNA (siRNA)
|
Others
|
|
HSP90B1 Human Pre-designed siRNA Set A contains three designed siRNAs for HSP90B1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
HSP90B1 Human Pre-designed siRNA Set A
HSP90B1 Human Pre-designed siRNA Set A
- HY-N7196
-
|
|
HSP
|
Inflammation/Immunology
|
|
Myrtucommulone A is a non-prenylated acylphloroglucinol that can be isolated from Myrtus communis (myrtle). Myrtucommulone A interacts with the HSP60 chaperone and inhibits HSP60 chaperone activity. Myrtucommulone A decreases the expression of LRP130, LONP .
|
-
- HY-10211
-
|
17-AAG; NSC 330507; CP 127374
|
HSP
Autophagy
Mitophagy
Bacterial
Apoptosis
Antibiotic
|
Infection
Cancer
|
|
Tanespimycin (17-AAG) is a potent HSP90 inhibitor with an IC50 of 5 nM, having a 100-fold higher binding affinity for tumour cell derived HSP90 than normal cell derived HSP90 . Tanespimycin depletes cellular STK38/NDR1 and reduces STK38 kinase activity. Tanespimycin also downregulates the stk38 gene expression .
|
-
- HY-110042
-
|
|
HSP
Apoptosis
|
Cancer
|
|
CCT018159, a 3,4-diaryl pyrazoleresorcinol, is a ATP-competitive HSP90 ATPase activity inhibitor with IC50s of 3.2 and 6.6 µM for human Hsp90β and yeast Hsp90, respectively. CCT018159 caused cell cytostasis associated with a G1 arrest and induces apoptosis. CCT018159 inhibits key endothelial and tumor cell functions implicated in invasion and angiogenesis .
|
-
- HY-162589
-
|
|
PROTACs
HSP
Apoptosis
|
Cancer
|
|
Lw13 is a Hsp90-targeting PROTAC and achieves maximum degradation at a concentration of 0.05 μM in Siha cells. Lw13 induces cell apoptosis and exhibits potent anti-tumor activity both in vitro and in vivo(Sturcture Note:(Blue: Cereblon ligand (HY-A0003), Black: linker；Pink: Hsp90 inhibitor SNX-5422 (HY-10213)) .
|
-
- HY-106443A
-
|
BRX-220
|
HSP
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
Arimoclomol maleate (BRX-220) is a co-inducer of heat shock proteins (HSP) . Arimoclomol protects motor neurons by enhancing Hsp expression, thus directly affecting protein aggregation and clearance of misfolded assemblies via the proteasome-ubiquitin system .
|
-
- HY-15986
-
|
CCT 129397
|
HSP
|
Cancer
|
|
VER-49009 is a Hsp90 inhibitor, with an IC50 of 25 nM and a Kd of 78 nM.
|
-
- HY-13757AS
-
|
ICI 47699-d5; (Z)-Tamoxifen-d5; trans-Tamoxifen-d5
|
Estrogen Receptor/ERR
HSP
Autophagy
Apoptosis
|
Cancer
|
|
Tamoxifen-d5 is a deuterium labeled Tamoxifen. Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM). Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity[1][2].
|
-
- HY-114664
-
|
|
HSP
|
Infection
Cancer
|
|
KNK423 is a specific heat shock protein (HSP) synthesis inhibitor. KNK423 improves the efficiency of Amphotericin B in inhibiting resistant Aspergillus terreus by blocking HSP70. KNK423 can be used in cancer and bacterial infection research .
|
-
- HY-149431
-
|
|
HSP
Potassium Channel
|
Cancer
|
|
NDNA4 (compound 17) is a selective inhibitor of Hsp90α (IC50: 0.34 μM). NDNA4 is a permanently charged analog with low membrane permeability and low cytotoxicity against Ovcar-8 and MCF-10A ((IC50 >100 μM)). NDNA4 prevents disruption of hERG channel maturation without generating a heat shock response or causing degradation of Hsp90α-dependent client proteins .
|
-
- HY-120625
-
|
|
HSP
|
Cancer
|
|
PU3 is a small molecule inhibitor of Hsp90 that competes with geldanamycin for Hsp90. PU3 induces degradation of proteins, including Her2, similar to geldanamycin. PU3 inhibits the growth of breast cancer cells, causing retinoblastoma protein hypophosphorylation, G1 arrest, and differentiation. PU3 represents a novel class of synthetic compounds that bind to Hsp90 and inhibit the proliferation of cancer cells. PU3 could provide a new strategy for the treatment of cancers .
|
-
- HY-106443
-
|
BRX-220 free base
|
HSP
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
Arimoclomol (BRX-220 free base) is a co-inducer of heat shock proteins (HSP) . Arimoclomol protects motor neurons by enhancing Hsp expression, thus directly affecting protein aggregation and clearance of misfolded assemblies via the proteasome-ubiquitin system .
|
-
- HY-15984
-
|
|
HSP
Apoptosis
|
Cancer
|
|
VER-50589 is a Hsp90 inhibitor, with an IC50 of 21 nM and a Kd of 4.5 nM.
|
-
- HY-B0779
-
-
- HY-U00398
-
|
|
HSP
|
Cardiovascular Disease
|
|
Bimoclomol is a heat shock protein (HSP) coinducer, used for treatment of cardiovascular diseases.
|
-
- HY-10940
-
-
- HY-148745
-
|
|
HSP
|
Cancer
|
|
JG-258 is an inactive negative control for Hsp70 inhibitors .
|
-
- HY-123035
-
|
|
HSP
Akt
EGFR
|
Endocrinology
|
|
Gamendazole, an indazole carboxylic acid (ICA), is an orally active, selective HSP90AB1 (HSP90BETA) and EEF1A1 (eEF1A) inhibitor. Gamendazole binds to the C-terminal nucleotide binding pocket of HSP90 and cause downregulation of clients AKT1 and ERBB2, but stabilizes the HSP90 heterocomplex. Gamendazole specifically inhibits the actin bundling function of EEF1A1, but does not bind to the nucleotide docking pocket nor inhibits the ribosome charging or protein translation functions of EEF1A1. Gamendazole, an antispermatogenic compound with antifertility effects, has the potential for reversible non-hormonal male contraceptive agent research .
|
-
- HY-117051
-
|
|
Others
|
Cancer
|
|
STA-2842 is a small molecule agent that inhibits heat shock protein 90 (HSP90) to treat autosomal dominant polycystic kidney disease (ADPKD). The disease is caused by inherited mutations in the PKD1 or PKD2 genes that aberrantly activate multiple signaling proteins and pathways that regulate cell proliferation. Through network construction, we found that many HSP90 client proteins associated with ADPKD are regulated by HSP90. STA-2842 induced degradation of these clients in Pkd1?/? primary kidney cells and in vivo. In experiments using conditional Cre-mediated in vivo knockout of Pkd1 in mice, we found that weekly administration of STA-2842 for 10 weeks significantly reduced initial renal cyst formation and kidney growth in mice and slowed disease progression in mice with pre-existing cysts. These improved disease phenotypes were accompanied by improvements in renal function markers and reductions in the expression and activity of HSP90 clients and their effectors, with the extent of this inhibition correlating with the extent of cyst expansion in individual animals. Pharmacokinetic analysis showed that HSP90 was overexpressed in cystic kidney tissue and HSP90 inhibitors were selectively retained in cystic tissue, which is similar to the situation in solid tumors. These results provide a preliminary basis for evaluating HSP90 inhibitors as therapeutic agents for ADPKD.
|
-
- HY-106443B
-
|
BRX-220 citrate
|
HSP
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
Arimoclomol citrate (BRX-220 citrate) is a co-inducer of heat shock proteins (HSP) . Arimoclomol citrate protects motor neurons by enhancing Hsp expression, thus directly affecting protein aggregation and clearance of misfolded assemblies via the proteasome-ubiquitin system .
|
-
- HY-164142
-
|
|
HSP
|
Cancer
|
|
ETB is a potent Hsp60 chaperone activity inhibitor. ETB blockes the chaperone activities of the wild-type protein and of the C237A and C447A mutant proteins. ETB binds to Hsp60 Cys 442 and shows the resistance of the C442A mutant to ETB inhibition .
|
-
- HY-18619
-
YL-109
2 Publications Verification
|
Aryl Hydrocarbon Receptor
|
Cancer
|
|
YL-109 is an antitumor agent that can induce carboxyl terminus of Hsp70-interacting protein (CHIP) expression through aryl hydrocarbon receptor (AhR) signaling. YL-109 has ability to inhibit breast cancer cell growth and invasiveness .
|
-
- HY-P10072
-
|
Hsp25 kinase inhibitor; Mk2 pseudosubstrate
|
ERK
JNK
p38 MAPK
HSP
MAPKAPK2 (MK2)
|
Others
|
|
MK2-IN-5 is a Mk2 pseudosubstrate (Ki= 8 μM). MK2-IN-5 targets the protein interaction domain in the MAPK pathway. MK2-IN-5 inhibits HSP25 and HSP27 phosphorylation .
|
-
- HY-122184
-
|
|
HSP
Apoptosis
|
Cancer
|
|
PET-16 is a selective HSP70 inhibitor that binds to an allosteric pocket of the substrate-binding domain. PET-16 inhibits the ability of HSP70 to cycle between ATP-bound and ADP-bound states. PET-16 induces apoptosis in multiple myeloma .
|
-
- HY-117395
-
|
|
HSP
|
Cancer
|
|
PU-H54, a Grp94-selective inhibitor, can be used for the research of breast cancer. Hsp90 chaperone family, comprised in humans of four paralogs, Hsp90α, Hsp90β, Grp94 and Trap-1, has important roles in malignancy . PU-H54 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-149432
-
|
|
HSP
Potassium Channel
|
Cancer
|
|
NDNA3 (compound 14) is a selective inhibitor of Hsp90α (IC50: 0.51 μM). NDNA3 is a permanently charged analog with low membrane permeability and low toxicity to Ovcar-8 (IC50: 12.66 μM) and MCF-10A (IC50: 11.72 μM) cells. NDNA3 prevents disruption of hERG channel maturation without generating a heat shock response or causing degradation of Hsp90α-dependent client proteins .
|
-
- HY-164399
-
|
|
HSP
EGFR
CDK
Akt
|
Cancer
|
|
SST0116CL1 is a HSP90 inhibitor (IC50: 0.21 μM). SST0116CL1 binds to the ATP binding pocket of Hsp90, and interferes with Hsp90 chaperone function thus resulting in client protein (EGFR, CDK4 and AKT) degradation. SST0116CL1 induces degradation of Her2 in BT-474 cell (IC50: 0.2 μM). SST0116CL1 has antiproliferative activity and inhibits tumor growth .
|
-
- HY-17547
-
|
|
HSP
|
Cancer
|
|
NMS-E973 is a potent and selective inhibitor of HSP90. NMS-E973 binds to the ATP binding site of Hsp90α with a DC50 of <10 nM. NMS-E973 is able to cross the blood-brain barrier (BBB). Antitumor efficacy .
|
-
- HY-14463
-
|
AT13387
|
HSP
|
Cancer
|
|
Onalespib (AT13387) is a long-acting second-generation Hsp90 inhibitor with a Kd of 0.71 nM.
|
-
- HY-13313
-
XL888
3 Publications Verification
|
HSP
|
Cancer
|
|
XL888 is a heat shock protein-90 (HSP90) inhibitor, with an IC50 of 24 nM.
|
-
- HY-145559
-
|
KU-596
|
HSP
|
Metabolic Disease
|
|
Cemdomespib (KU-596) is a highly bioavailable second-generation Hsp90 modulator. Cemdomespib has shown efficacy in improving sensory deficits in models of diabetic peripheral neuropathy. Cemdomespib induces Hsp70 levels and manifest neuroprotective activity through induction of the heat shock response .
|
-
- HY-124611
-
|
|
HSP
|
Cancer
|
|
JG-231 is an analogue of JG-98 with anticancer effects. JG-231 inhibits the interaction of Hsp70-BAG3. JG-231 inhibits MDA-MB-231 heterograft tumor models of triple negative breast cancer (TNBC) .
|
-
- HY-169133
-
|
|
PROTACs
Glutathione Peroxidase
Ferroptosis
|
Cancer
|
|
GDCNF-11 is a HIM-PROTAC GPX4 degrader based on the chaperone protein HSP90. GDCNF-11 promotes the ubiquitination and degradation of GPX4 through the HSP 90 chaperone complex, reduces endogenous GPX4 expression to induce ferroptosis in HT-1080 cells, and the DC50 value is 0.08 μM (Pink: Target protein ligand (HY-153748); Blue: HSP90 ligand (HY-10212); Black: Linker (HY-W169526)) .
|
-
- HY-10942
-
|
NVP-BEP800
|
HSP
|
Cancer
|
|
VER-82576 (NVP-BEP800) is a potent, orally available and selective Hsp90 inhibitor, with an IC50 of 58 nM for Hsp90β; VER-82576 also slightly blocks Grp94 and Trap-1, with IC50s of 4.1 and 5.5 μM, respectively.
|
-
- HY-147747
-
|
|
HSP
|
Cancer
|
|
Among vibsanin a analogues, vibsanin a analog C (VAC) showed anti proliferative effect on various cancer cell lines, and the anti proliferative activity was the strongest among vibsanin a analogues. In addition, VAC fluctuated the amount of hsp90 related proteins in cells and inhibited hsp90 mediated protein refolding of luciferase in vitro.
|
-
- HY-D2360
-
|
|
HIF/HIF Prolyl-Hydroxylase
HSP
|
Cancer
|
|
O-Carboranylphenoxyacetanilide is a HIF-1α inhibitor and inhibits HIF-1α activation. O-Carboranylphenoxyacetanilide inhibits transcriptional activity of HIF in HeLa cells (IC50: 0.74 μM). O-Carboranylphenoxyacetanilide inhibits HSP60 chaperone activity and HSP60 ATPase activity .
|
-
- HY-116279
-
-
- HY-153547
-
|
|
Parasite
|
Infection
Inflammation/Immunology
|
|
HSP90-IN-21 (5e) is an antiplasmodial agent, with IC50 values of 0.04, 0.17 and 2.91 μM against erythrocytic stage of P. falciparum (Pf3D7 and PfDd2 strains), cytotoxicity of human liver hepatocellular carcinoma cell line (HepG2), respectively .
|
-
- HY-163329
-
|
|
Others
|
Neurological Disease
|
|
BCH-HSP-C01 is a lead compound that restores AP-4-dependent protein trafficking in neuronal models of adapter protein complex 4 (AP-4)-associated hereditary spastic paraplegia. BCH-HSP-C01 can be used for the research of autophagy-associated diseases .
|
-
- HY-N6249
-
-
- HY-133571
-
|
AHGDM
|
HSP
ADC Cytotoxin
|
Cancer
|
|
Aminohexylgeldanamycin (AHGDM), a Geldanamycin derivative, is a potent HSP90 inhibitor. Aminohexylgeldanamycin shows antiangiogenic and antitumor activities .
|
-
- HY-133571A
-
|
AHGDM hydrochloride
|
HSP
ADC Cytotoxin
|
Cancer
|
|
Aminohexylgeldanamycin (AHGDM) hydrochloride, a Geldanamycin derivative, is a potent HSP90 inhibitor. Aminohexylgeldanamycin hydrochloride shows antiangiogenic and antitumor activities .
|
-
- HY-167731
-
|
|
Others
|
Infection
|
|
Monorden diacetate serves as a promising lead compound in the development of novel fungicides due to its potential as an Hsp90 inhibitor.
|
-
- HY-N1455
-
|
Panaxynol; Carotatoxin
|
HSP
Apoptosis
|
Cancer
|
|
Falcarinol (Panaxynol) is a natural, orally active Hsp90 inhibitor targeting both the N-terminal and C-terminal of Hsp90 with limited toxicities. Falcarinol (Panaxynol) induces apoptosis . Falcarinol is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-107553
-
|
|
HSP
Apoptosis
|
Cancer
|
|
Chetomin, an active component of Chaetomium globosum, is a heat shock protein 90/hypoxia-inducible factor 1 alpha (Hsp90/HIF1α) pathway inhibitor. Chetomin is a potent, nontoxic non-small cell lung cancer cancer stem cells (NSCLC CSC)-targeting molecule .
|
-
- HY-108248
-
-
- HY-121881
-
|
|
HSP
|
Cancer
|
|
PU3 is an Hsp90 inhibitor that competes with geldanamycin (GM) and others for the conserved ATP/ADP pocket of Hsp90. PU3 also induces degradation of proteins such as Her2 and inhibits breast cancer cell growth by causing retinoblastoma protein hypophosphorylation, G1 arrest, and cell differentiation. PU3 has the potential to be a cancer inhibitor. .
|
-
- HY-164372
-
|
17-DR
|
HSP
Apoptosis
|
Cancer
|
|
17-Demethoxy-reblastatin (17-DR) is an inhibitor for heat shock protein 90 (Hsp90), with an IC50 of 1.82 μM for yeast Hsp90 ATPase. 17-Demethoxy-reblastatin inhibits the proliferation of cancer cell HepG2 and SMMC7721, reduces the colony formation, and induces apoptosis through mitochondria and caspase mediated pathway .
|
-
- HY-11038B
-
|
PU-H71 hydrochloride
|
HSP
|
Cancer
|
|
Zelavespib (PU-H71) hydrochloride is a potent Hsp90 inhibitor, with an IC50 of 51 nM in MDA-MB-468 cells.
|
-
- HY-11038
-
|
PU-H71
|
HSP
|
Cancer
|
|
Zelavespib (PU-H71) is a potent Hsp90 inhibitor, with an IC50 of 51 nM in MDA-MB-468 cells.
|
-
- HY-10212
-
BIIB021
3 Publications Verification
CNF2024
|
HSP
Autophagy
|
Cancer
|
|
BIIB021 (CNF2024) is an orally active, fully synthetic inhibitor of HSP90 with a Ki and an EC50 of 1.7 nM and 38 nM, respectively .
|
-
- HY-102007
-
|
|
HSP
|
Cancer
|
|
Gamitrinib TPP is a Gamitrinib (GA) mitochondrial matrix inhibitor. Gamitrinib TPP is a mitochondrial targeted HSP90 inhibitor with anti-cancer activity.
|
-
- HY-13301
-
|
|
HSP
|
Cancer
|
|
MPC-3100 is an orally bioavailable, synthetic, second-generation small-molecule inhibitor of Hsp90 with potential antineoplastic activity .
|
-
- HY-116683
-
|
MAL2-11B
|
HSP
DNA/RNA Synthesis
|
Infection
Cancer
|
|
116-9e (MAL2-11B) is a Hsp70 co-chaperone DNAJA1 inhibitor. 116-9e inhibits Simian Virus 40 (SV40) replication and DNA synthesis. 116-9e inhibits tumor antigen (TAg)’s endogenous ATPase activity and the TAg-mediated activation of Hsp70 .
|
-
- HY-155064
-
|
|
HSP
|
Metabolic Disease
|
|
TRAP1-IN-2 (compound 36) is a selective degrader of TRAP1 downstream proteins without affecting Hsp90's cytoplasmic downstream proteins. TRAP1-IN-2 also inhibits OXPHOS and alters cellular glycolysis metabolism. TRAP1-IN-2 destabilizes TRAP1 tetramers and disrupts mitochondrial membrane potential.
|
-
- HY-B1425
-
|
|
HSP
Reactive Oxygen Species
|
Cancer
|
|
Ethoxyquin is an antioxidant which has been used in animal feed for many years and also an inhibitor of heat shock protein 90 (Hsp90).
|
-
- HY-133570
-
|
|
HSP
ADC Cytotoxin
|
Cancer
|
|
17-AEP-GA, an HSP90 antagonist, is a potent inhibitor of glioblastoma cell proliferation, survival, migration and invasion. ADCs Toxin .
|
-
- HY-137441
-
|
PU-HZ151
|
HSP
|
Neurological Disease
Cancer
|
|
Icapamespib (PU-HZ151) is a potent HSP90 inhibitor with an EC50 of 5 nM. Icapamespib is able to cross blood-brain barrier .
|
-
- HY-162767
-
|
|
HSP
|
Neurological Disease
|
|
KUNG65 is a selective inhibitor of Grp94, with a target Kd of 540 nM and at least 73 fold selectivity vs. the other Hsp90 isoforms .
|
-
- HY-137441A
-
|
PU-HZ151 hydrochloride
|
HSP
|
Neurological Disease
|
|
Icapamespib hydrochloride (PU-HZ151) is a potent HSP90 inhibitor with an EC50 of 5 nM. Icapamespib hydrochloride is able to cross blood-brain barrier .
|
-
- HY-13468
-
KW-2478
3 Publications Verification
|
HSP
|
Cancer
|
|
KW-2478 is an inhibitor of Hsp90α, with an IC50 of 3.8 nM, and has antitumor activity against various human hematological tumor cells.
|
-
- HY-102007A
-
|
|
HSP
|
Cancer
|
|
Gamitrinib TPP hexafluorophosphate is a Gamitrinib (GA) mitochondrial matrix inhibitor. Gamitrinib TPP hexafluorophosphate is a mitochondrial targeted HSP90 inhibitor with anti-cancer activity.
|
-
- HY-P1750
-
|
|
HSP
Survivin
|
Cancer
|
|
Shepherdin (79-87) is amino acids 79 to 87 fragment of Shepherdin. Shepherdin is a peptidomimetic antagonist of the complex between Hsp90 and Survivin. Anticancer activity .
|
-
- HY-B0779R
-
|
|
HSP
|
Neurological Disease
Cancer
|
|
Teprenone (Standard) is the analytical standard of Teprenone. This product is intended for research and analytical applications. Teprenone is an anti-ulcer agent, and works as an inducer of heat shock proteins (HSPs).
|
-
- HY-15098
-
|
Apoptosis Activator VII
|
HSP
Apoptosis
|
Cancer
|
|
Apoptozole (Apoptosis Activator VII) is an inhibitor of the ATPase domain of Hsc70 and Hsp70, with Kds of 0.21 and 0.14 μM, respectively, and can induce apoptosis.
|
-
- HY-107578
-
|
Macbecin I; NSC 330499
|
HSP
|
Cancer
|
|
Macbecin is a stable HSP90 inhibitor by binding to the ATP-binding site with an IC50 of 2 μM and a Kd of 0.24 μM. Macbecin exhibits antitumor and cytocidal activities .
|
-
- HY-N10393
-
|
|
PKC
HSP
|
Cancer
|
|
Vibsanin A, a protein kinase C (PKC) activator, exhibits anti-proliferative activity against human cancer cell lines. Vibsanin A is also a HSP90 inhibitor .
|
-
- HY-P1750A
-
|
|
HSP
Survivin
|
Cancer
|
|
Shepherdin (79-87) TFA is amino acids 79 to 87 fragment of Shepherdin. Shepherdin is a peptidomimetic antagonist of the complex between Hsp90 and Survivin. Anticancer activity .
|
-
- HY-149780
-
|
DiNap
|
HSP
|
Cancer
|
|
Flavokawain 1i (DiNap) is an Hsp90 inhibitor. Flavokawain 1i (DiNap) has anti-cell proliferation activity and can be used in cancer research .
|
-
- HY-136312
-
|
|
HSP
|
Cancer
|
|
17-DMAP-GA, a Geldanamycin (HY-15230) analogue, is an inhibitor of HSP90. 17-DMAP-GA causes cell cycle abnormalities .
|
-
- HY-138820
-
|
|
HSP
|
Neurological Disease
|
|
SW02 is a potent activator of ATPase activity of Hsp70, with an EC50 of 150 μM. SW02 leads to accumulation of both total tau and phosphorylated tau (pTau) .
|
-
- HY-P9962
-
|
|
Fungal
|
Infection
|
|
Efungumab is a monoclonal antibody with antifungal activity. Efungumab binds to HSP 90, preventing a conformational change needed for fungal viability. Efungumab can be used for research on invasive candidiasis (IC) .
|
-
- HY-19399B
-
|
(-)-BRX 005 sulfate; (-)-BRX 235 sulfate
|
p38 MAPK
HSP
|
Cardiovascular Disease
|
|
Iroxanadine (BRX 005) sulfate is a vasculoprotector. Iroxanadine is a p38 kinase and HSP protein dual activator. Iroxanadine sulfate has the potential for atherosclerosis and vascular diseases research .
|
-
- HY-111002
-
|
NSC375009
|
HSP
|
Others
|
|
Displurigen (NSC375009) disrupts human embryonic stem cell pluripotency by targeting HSPA8. Displurigen inhibits ATPase activity of HSP70 (IC50 = 225 μM) .
|
-
- HY-130997
-
|
|
ADC Cytotoxin
HSP
|
Infection
Cancer
|
|
17-GMB-APA-GA is an ADC Cytotoxin. 17-GMB-APA-GA is a potent HSP90 inhibitor and used for latent T. gondii infection research .
|
-
- HY-115499
-
|
|
HSP
|
Cancer
|
|
MPC-0767 is a potent, selective, and orally active hsp90 inhibitor. MPC-0767 is an L-alanine ester proagent of MPC-3100 with improved chemical stability .
|
-
- HY-132995
-
|
|
Drug Metabolite
|
Others
|
|
DP-1, a degradation product of SDC-TRAP-0063, is a fragment of Ganetespib. Ganetespib is a heat shock protein 90 (HSP90) inhibitor with anti-tumor activity .
|
-
- HY-162365
-
|
|
HSP
Apoptosis
Autophagy
|
Cancer
|
|
JD-02 is a novel Hsp90 inhibitor. JD-02 can induce autophagy and apoptosis. JD-02 increses the level of reactive oxygen species .
|
-
- HY-132995A
-
|
|
Drug Metabolite
|
Cancer
|
|
DP-1 hydrochloride, a degradation product of SDC-TRAP-0063, is a fragment of Ganetespib. Ganetespib is a heat shock protein 90 (HSP90) inhibitor with anti-tumor activity .
|
-
- HY-15230
-
-
- HY-10213
-
|
PF-04929113
|
HSP
|
Cancer
|
|
SNX-5422 (PF-04929113), a prodrug of SNX-2112, is an orally active Hsp90 inhibitor, with a Kd of 41 nM, and also induces Her-2 degradation, with an IC50 of 37 nM.
|
-
- HY-139144
-
-
- HY-162605
-
|
|
STAT
HSP
|
Cancer
|
|
CYD0682 is an analog of Oridonin (HY-N0004). CYD0682 attenuates STAT3 activation and ECM production via an HSP90 pathway in hepatic stellate cells .
|
-
- HY-164465
-
|
|
HSP
|
Cancer
|
|
C086, a novel potent Hsp90 inhibitor, could inhibit cell cycle progression and induce cell apoptosis and anti-metastasis by regulating various mechanisms in different cell types .
|
-
- HY-10213A
-
|
PF-04929113 mesylate
|
HSP
|
Cancer
|
|
SNX-5422 Mesylate (PF-04929113 Mesylate), a prodrug of SNX-2112, is an orally active Hsp90 inhibitor, with a Kd of 41 nM, and also induces Her-2 degradation, with an IC50 of 37 nM.
|
-
- HY-112910
-
|
|
HSP
|
Inflammation/Immunology
Cancer
|
|
Grp94 Inhibitor-1 is a potent, selective Grp94 inhibitor with an IC50 value of 2 nM, and over 1000-fold selectivity to Grp94 against Hsp90α .
|
-
- HY-122878
-
|
|
HSP
|
Cancer
|
HS-131, a near infrared dye tethered Hsp90 inhibitor, is able to detect oncogene-driven breast cancers, including multiple different molecular subtypes of human breast cancers .
|
-
- HY-B1434
-
|
7-ACA
|
Beta-lactamase
Bacterial
Antibiotic
|
Infection
|
|
7-aminocephalosporanic acid (7-ACA) is a HSP90β inhibitor and an antibiotic. 7-Aminocephalosporanic acid is the core chemical structure of the synthesis of cephalosporin antibiotics and an effective β-lactamase inhibitor .
|
-
- HY-101026
-
|
|
HSP
|
Cancer
|
|
CCT251236 is an orally available pirin ligand from a heat shock transcription factor 1 (hsf1) phenotypic screen with an IC50 of 19 nM for inhibition of HSF1-mediated HSP72 induction.
|
-
- HY-115781
-
|
Panvotinib-401; Pan-401
|
HSP
|
Cancer
|
|
DN401 is a potent TRAP1 inhibitor with an IC50 of 79 nM. DN401 shows a weak inhibition of Hsp90 (IC50 of 698 nM). DN401 inactivates mitochondrial TRAP1 and has potent anticancer activities .
|
-
- HY-B1425R
-
|
|
HSP
Reactive Oxygen Species
|
Cancer
|
|
Ethoxyquin (Standard) is the analytical standard of Ethoxyquin. This product is intended for research and analytical applications. Ethoxyquin is an antioxidant which has been used in animal feed for many years and also an inhibitor of heat shock protein 90 (Hsp90).
|
-
- HY-11039
-
|
|
HSP
|
Cancer
|
|
PU24FCl is a specific inhibitor of Hsp90. PU24FCl exhibits wide-ranging anti-cancer activities. PU24FCl accumulates in tumors while being rapidly cleared from normal tissue .
|
-
- HY-168566
-
|
|
HSP
|
Cancer
|
|
EV206 is a potent Hsp70 inhibitor. EV206 shows antiproliferative activity. EV206 induces apoptosis and increases the protein expression of cleaved PARP and caspase-3. EV206 shows antitumor activity .
|
-
- HY-100555
-
|
|
HSP
|
Infection
Cancer
|
|
CH5138303 is a potent and orally active Hsp90 inhibitor. CH5138303 shows high binding affinity for N-terminal Hsp90α, with Kd of 0.52 nM. CH5138303 shows potent anti-proliferative activity against human cancer cell lines (HCT116 and NCI-N87), with IC50 values of 0.098 and 0.066 μM, respectively. CH5138303 shows high oral bioavailability in mice (F=44.0%). CH5138303 shows potent antitumor efficacy in a human NCI-N87 gastric cancer xenograft model .
|
-
- HY-161781
-
|
|
HSP
EGFR
Akt
Survivin
|
Cancer
|
|
HVH-2930 is an inhibitor for heat shock protein 90 (HSP90). HVH-2930 inhibits cell viability of BT474 (Trastuzumab (HY-P9907) sensitive) and JIMT-1 (Trastuzumab (HY-P9907) resistant), with IC50 of 6.86 μM and 4.42 μM, through downregulation of HSP90 clients HER2, p-HER2, AKT, p-AKT, cyclin D1 and survivin. HVH-2930 exhibits antitumor efficacy in mouse models. HVH-2930 exhibits good pharmacokinetic characteristics in mice .
|
-
- HY-101712
-
|
|
HSP
|
Neurological Disease
|
|
TRC051384 is a potent inducer of heat shock protein 70 (HSP70). TRC051384 exhibits protective effects against neuronal trauma via inhibition of necroptosis. TRC051384 can be used for the research of ischemic stroke .
|
-
- HY-119552
-
|
LL-S490β
|
Endogenous Metabolite
Neurokinin Receptor
|
Neurological Disease
|
|
Acetylaszonalenin, a prenylated indole derivative, is a fungal metabolite.Acetylaszonalenin is a potent neurokinin-1 (NK1) receptor antagonist. Acetylaszonalenin shows inhibition of [ 3H]-SP binding to human astrocytoma cells with a Ki of 170 μM .
|
-
- HY-124109
-
|
|
HSP
|
Cardiovascular Disease
Neurological Disease
|
|
TRC051384 hydrochloride is a potent inducer of heat shock protein 70 (HSP70). TRC051384 hydrochloride exhibits protective effects against neuronal trauma via inhibition of necroptosis. TRC051384 hydrochloride can be used for the research of ischemic stroke .
|
-
- HY-B0510C
-
|
|
Antifolate
Bacterial
Antibiotic
|
Infection
Cancer
|
|
Trimethoprim lactate is a bacteriostatic antibiotic and an orally active dihydrofolate reductase inhibitor. Trimethoprim lactate is active against a wide range of Gram-positive and Gram-negative aerobic bacteria. Trimethoprim lactate has the potential for the research of urinary tract infections, Shigellosis and Pneumocystis pneumonia. Trimethoprim lactate can inhibit infection of Influenza A virus in chick embryo when combinated with zinc .
|
-
- HY-113314
-
|
|
Endogenous Metabolite
|
Cancer
|
|
AFMK, antioxidant metabolite of Melatonin, attenuates X-ray-induced oxidative damage to DNA, proteins and lipids in mice. AFMK is a poorer scavenger. The pKa of AFMK at physiological pH is 8.7. Antioxidant capacity . AFMK improves the anti-tumor effect of Gemcitabine in PANC-1 cells through the modulation of apoptotic pathway .
|
-
- HY-B0510A
-
|
|
Antifolate
Bacterial
Antibiotic
Influenza Virus
|
Infection
Cancer
|
|
Trimethoprim sulfate is a bacteriostatic antibiotic and an orally active dihydrofolate reductase inhibitor. Trimethoprim sulfate is active against a wide range of Gram-positive and Gram-negative aerobic bacteria. Trimethoprim sulfate has the potential for the research of urinary tract infections, Shigellosis and Pneumocystis pneumonia. Trimethoprim sulfate can inhibit infection of Influenza A virus in chick embryo when combinated with zinc .
|
-
- HY-162768
-
|
|
HSP
|
Cancer
|
|
Grp94 Inhibitor-2 (compound 23), a cyclopropane analog, exhibits high affinity for glucose-regulated protein 94 (Grp94) with a Kd of 0.48 µM and 0.65 µM for Grp94 and Hsp90α, respectively .
|
-
- HY-13757A
-
Tamoxifen
Maximum Cited Publications
114 Publications Verification
ICI 47699; (Z)-Tamoxifen; trans-Tamoxifen
|
Estrogen Receptor/ERR
HSP
Autophagy
Apoptosis
|
Cancer
|
|
Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells . Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively . Tamoxifen activates autophagy and induces apoptosis . Tamoxifen also can induce gene knockout of CreER(T2) transgenic mouse .
|
-
- HY-101508
-
|
|
Histone Methyltransferase
|
Cancer
|
|
GNA002 is a highly potent, specific and covalent EZH2 (Enhancer of zeste homolog 2) inhibitor with an IC50 of 1.1 μM. GNA002 can specifically and covalently bind to Cys668 within the EZH2-SET domain, triggering EZH2 degradation through COOH terminus of Hsp70-interacting protein (CHIP)-mediated ubiquitination. GNA002 efficiently reduces EZH2-mediated H3K27 trimethylation, reactivates polycomb repressor complex 2 (PRC2)-silenced tumor suppressor genes .
|
-
- HY-164548
-
|
|
HSP
Apoptosis
|
Cancer
|
|
WK88-1, a Hsp90 inhibitor, induces overall degradation of multiple oncogenic signaling molecules including EGFR, ErbB2 and ErbB3, leading to subsequent growth arrest and apoptosis in the Gefitinib-resistant H1975 cell line .
|
-
- HY-111524
-
|
|
HSP
Apoptosis
|
Cancer
|
|
CPUY201112 is a potent heat shock protein Hsp90 inhibitor with Kd of 27 nM. CPUY201112 induces p53-mediated apoptosis in MCF-7 cells, resulting in cell cycle arrest, which can be used in cancer research .
|
-
- HY-115467
-
|
|
HSP
|
Metabolic Disease
|
|
MitoBloCK-10 (MB-10) is the first small molecule modulator to attenuate protein-associated motor (PAM) complex activity. MitoBloCK-10 (MB-10) inhibits Tim44 (C-terminal domain) binding to the precursor and to Hsp70 .
|
-
- HY-149367
-
|
|
Apoptosis
|
Cancer
|
Anticancer agent 136 (compound 22), a C17-triazole analogue of Geldanamycin (GDM; HY-15230), has an IC50 of 3.38 μM for HDF and a Kd of 3.86 μM for Hsp90. Anticancer agent 136 is an apoptosis-inducing agent .
|
-
- HY-157085
-
|
|
HSP
|
Cancer
|
|
BX-2819 is a Hsp90 inhibitor with an IC50 value of 41 nM. BX-2819 inhibits the proliferation of cancer cells. BX-2819 can significantly inhibit the growth of NCI-N87 and HT-29 tumors in nude mice .
|
-
- HY-15230R
-
|
|
HSP
Bacterial
Influenza Virus
Antibiotic
|
Infection
Inflammation/Immunology
Cancer
|
|
Geldanamycin (Standard) is the analytical standard of Geldanamycin. This product is intended for research and analytical applications. Geldanamycin is a Hsp90 inhibitor with antimicrobial activity against many Gram-positive and some Gram-negative bacteria. Geldanamycin has anti-influenza virus H5N1 activities.
|
-
- HY-N3417
-
|
|
HSP
RIP kinase
Apoptosis
Necroptosis
|
Inflammation/Immunology
Cancer
|
|
Kongensin A is a natural product isolated from Croton kongensis. Kongensin A is an effective, covalent HSP90 inhibitor that blocks RIP3-dependent necroptosishas. Kongensin A is a potent necroptosis inhibitor and an apoptosis inducer. Kongensin A has potential anti-necroptosis and anti-inflammation applications .
|
-
- HY-18399
-
|
|
HSP
NO Synthase
|
Cancer
|
|
YM-1 is a stable and soluble MKT-077 (HY-15096) analog and an orally active Hsp70 inhibitor. YM-1 induces cell death of HeLa cells and up-regulates the level of p53 and p21 proteins .
|
-
- HY-13757
-
|
ICI 46474; (Z)-Tamoxifen Citrate; trans-Tamoxifen Citrate
|
Estrogen Receptor/ERR
HSP
Autophagy
Apoptosis
|
Cancer
|
|
Tamoxifen Citrate (ICI 46474) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells .Tamoxifen Citrate is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen Citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively . Tamoxifen Citrate activates autophagy and induces apoptosis .Tamoxifen Citrate also can induce gene knockout of CreER(T2) transgenic mouse .
|
-
- HY-W015445
-
|
|
p38 MAPK
|
Metabolic Disease
|
|
SD-169 is an orally active ATP-competitive inhibitor of p38α MAPK, with an IC50 of 3.2 nM. SD-169 also weakly inhibits p38β MAPK with an IC50 of 122 nM. SD-169 prevents the development and progression of diabetes by inhibiting T cell infiltration and activation .
|
-
- HY-161102
-
|
|
Autophagy
|
Cancer
|
|
[Ru(phen)2(xant)] hexafluorophosphate is an inducer of Autophagy. [Ru(phen)2(xant)] hexafluorophosphate eliminates CRC stem cells by targeting the chaperone Hsp90. [Ru(phen)2(xant)] hexafluorophosphate reduces cell migration and invasion .
|
-
![[Ru(phen)2(xant)] hexafluorophosphate](//file.medchemexpress.eu/product_pic/hy-161102.gif)
- HY-13757AS1
-
|
ICI 47699-d3; (Z)-Tamoxifen-d3; trans-Tamoxifen-d3
|
Estrogen Receptor/ERR
Apoptosis
Autophagy
HSP
|
Cancer
|
|
Tamoxifen-d3 is the deuterium labeled Tamoxifen[1]. Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells[2][3][4]. Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively[6]. Tamoxifen activates autophagy and induces apoptosis[5]. Tamoxifen also can induce gene knockout of CreER(T2) transgenic mouse[7].
|
-
- HY-13757AR
-
|
ICI 47699(Standard); (Z)-Tamoxifen(Standard); trans-Tamoxifen (Standard)
|
Estrogen Receptor/ERR
HSP
Autophagy
Apoptosis
|
Cancer
|
|
Tamoxifen (Standard) is the analytical standard of Tamoxifen. This product is intended for research and analytical applications. Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells . Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively . Tamoxifen activates autophagy and induces apoptosis . Tamoxifen also can induce gene knockout of CreER(T2) transgenic mouse .
|
-
- HY-B0425A
-
|
Albamycin sodium; Cathomycin sodium
|
Bacterial
Antibiotic
Orthopoxvirus
Apoptosis
DNA/RNA Synthesis
HSP
|
Infection
Cancer
|
|
Novobiocin (Albamycin) sodium is a potent and orally active antibiotic. Novobiocin sodium also is a DNA gyrase inhibitor and a heat shock protein 90 (Hsp90) antagonist. Novobiocin sodium has the potential for the research of highly beta-lactam-resistant pneumococcal infections. Novobiocin sodium shows anti-orthopoxvirus activity .
|
-
- HY-120548
-
|
|
HSP
|
Cancer
|
|
KBU2046 is an oral, highly selective inhibitor of cell motility and cell invasion in vitro. KBU2046 binds chaperone heterocomplexes, selectively alters binding of client proteins that regulate motility, and lacks all of the hallmarks of classical HSP90 inhibitors. KBU2046 inhibits cancer metastasis and prolongs life .
|
-
- HY-108486
-
|
|
Bacterial
Antibiotic
|
Infection
|
|
Herbimycin A, an ansamycin antibiotic, acts as a Src family kinase inhibitor. Herbimycin A binds to the SH domain and inhibits the activity of p60 v-src and p210 BCR-ABL Herbimycin A inhibits Hsp90 and impairs recovery from heat shock. Herbimycin A exhibits antiangiogenic activity in endothelial cells in vitro.
|
-
- HY-N10502
-
|
|
MDM-2/p53
HSP
|
Cancer
|
|
Colletofragarone A2 can be be isolated from the fungus Colletotrichum sp. (13S020). Colletofragarone A2 inhibits mutant p53 and HSP90 with anti-cancer activity. Colletofragarone A2 promotes degradation and aggregation of mutant p53 and suppressing tumor growth in vivo .
|
-
- HY-B0425
-
|
Albamycin; Cathomycin
|
Antibiotic
DNA/RNA Synthesis
HSP
Apoptosis
Bacterial
Orthopoxvirus
|
Infection
Cancer
|
|
Novobiocin (Albamycin) is a potent and orally active antibiotic. Novobiocin also is a DNA gyrase inhibitor and a heat shock protein 90 (Hsp90) antagonist. Novobiocin has the potential for the research of highly beta-lactam-resistant pneumococcal infections. Novobiocin shows anti-orthopoxvirus activity .
|
-
- HY-N1986
-
|
|
HSP
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Cucurbitacin D is the active ingredient in Trichosanthes kirilowii and can disrupt the interaction between Hsp90 and two co-chaperones, Cdc37 and p23. Cucurbitacin D is an inflammasome activator. Cucurbitacin D induces cell cycle arrest and cell apoptosis, exhibiting anti-tumor and anti-inflammatory effects .
|
-
- HY-119046
-
|
|
HSP
Parasite
|
Infection
|
|
SNX-0723 is a potent Hsp90 Inhibitor with anti-Plasmodium activity. SNX-0723 shows high binding affinity for HsHsp90 and PfHsp90 with Kis of 4.4 and 47 nM, respectively. SNX-0723 inhibits liver-stage P. berghei ANKA parasites with the EC50 of 3.3 μM .
|
-
- HY-105215
-
|
|
Neurokinin Receptor
|
Inflammation/Immunology
|
|
FK888 is a potent, selective, and high affinity dipeptide NK1 receptor antagonist. FK888 displaces [3H]-SP binding with a Ki value of 0.69 nM and 0.45 microM. FK888 also inhibits SP-induced airway oedema in guinea-pig after both intravenous and oral administration .
|
-
- HY-149814
-
|
|
PDHK
HSP
|
Cancer
|
|
PDK-IN-1 (compound 7o) is a pyruvate dehydrogenase kinase (PDK) inhibitor. PDK-IN-1 shows IC50 values of 0.03 and 0.1 μM for PDK1 and HSP90, respectively. PDK-IN-1 targets PDH/PDK axis thus reducing efficiently the tumor mass .
|
-
- HY-108483
-
|
|
Neurokinin Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
RP 67580 is a non-peptide antagonist of substance P (SP), competitively inhibits the binding of [3H]SP to neurokinin receptor 1 (NK1 receptor) in rat brain membranes with a Ki value of 4.16 nM. RP 67580 is a specific antagonist of NK1 receptors and can be used in the research of pain and neurogenic inflammation .
|
-
- HY-B1434R
-
|
|
Beta-lactamase
Bacterial
Antibiotic
|
Infection
|
|
7-Aminocephalosporanic acid (Standard) is the analytical standard of 7-Aminocephalosporanic acid. This product is intended for research and analytical applications. 7-aminocephalosporanic acid (7-ACA) is a HSP90β inhibitor and an antibiotic. 7-Aminocephalosporanic acid is the core chemical structure of the synthesis of cephalosporin antibiotics and an effective β-lactamase inhibitor .
|
-
- HY-13757S
-
|
ICI 46474-d3 hydrochloride; (Z)-Tamoxifen-d3 hydrochloride; trans-Tamoxifen-d3 hydrochloride
|
Apoptosis
Estrogen Receptor/ERR
Autophagy
HSP
Isotope-Labeled Compounds
|
Cancer
|
|
Tamoxifen-d3 hydrochloride is deuterated labeled Tamoxifen (Citrate) (HY-13757). Tamoxifen Citrate (ICI 46474) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells .Tamoxifen Citrate is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen Citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively . Tamoxifen Citrate activates autophagy and induces apoptosis .Tamoxifen Citrate also can induce gene knockout of CreER(T2) transgenic mouse .
|
-
- HY-13757R
-
|
|
Estrogen Receptor/ERR
HSP
Autophagy
Apoptosis
|
Cancer
|
|
Tamoxifen (Citrate) (Standard) is the analytical standard of Tamoxifen (Citrate). This product is intended for research and analytical applications. Tamoxifen Citrate (ICI 46474) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells .Tamoxifen Citrate is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen Citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively . Tamoxifen Citrate activates autophagy and induces apoptosis .Tamoxifen Citrate also can induce gene knockout of CreER(T2) transgenic mouse .
|
-
- HY-12143
-
|
GR 205171A
|
Neurokinin Receptor
|
Neurological Disease
Endocrinology
Cancer
|
|
Vofopitant dihydrochloride (GR 205171A) is a potent, selective and orally available tachykinin neurokinin 1(NK1) receptor antagonist, inhibits [ 3H]SP binding to the NK1 receptor with pKi values of 9.5 and 10.6 in rat and human membranes respectively, acts as a potential broad-spectrum anti-emetic agent .
|
-
- HY-149914
-
|
|
Androgen Receptor
|
Cancer
|
|
WCA-814 is an androgen receptor (AR) antagonist-Hsp90 inhibitor conjugate. WCA-814 induces the degradation of full-length and AR-V7. WCA-814 has cytotoxic effect in prostatic cancer cells (IC50: 171.2 nM, 26.5 nM for LNCaP, 22Rv1 cell) .
|
-
- HY-15205
-
|
STA-9090
|
HSP
Apoptosis
|
Cancer
|
|
Ganetespib (STA-9090) is a heat shock protein 90 (HSP90) inhibitor which exhibits potent cytotoxicity in a wide variety of hematological and solid tumor cell lines. Ganetespib has antiangiogenic effects in colorectal cancer mediated through inhibition of HIF-1α and STAT3 .
|
-
- HY-N6790
-
-
- HY-17504B
-
|
ZD 4522 Sodium; X-Plended Sodium; Crestor Sodium
|
HMG-CoA Reductase (HMGCR)
Potassium Channel
Autophagy
Bacterial
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
Rosuvastatin Sodium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC50 of 11 nM. Rosuvastatin Sodium potently blocks hERG current with an IC50 of 195 nM . Rosuvastatin Sodium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Sodium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .
|
-
- HY-161765
-
|
|
HSP
STAT
|
Cancer
|
|
iHSP110-33 is an inhibitor for heat shock protein 110 (HSP110). iHSP110-33 exhibits antitumor efficacy agaisnt large B-cell lymphoma and classical Hodgkin lymphoma. iHSP110-33 shows a synergistic effect with Selinexor (HY-17536), inhibits the STAT6 phosphorylation, and enhances its antitumor activity. .
|
-
- HY-B0425AR
-
|
|
Bacterial
Antibiotic
Orthopoxvirus
Apoptosis
DNA/RNA Synthesis
HSP
|
Infection
Cancer
|
|
Novobiocin (sodium) (Standard) is the analytical standard of Novobiocin (sodium). This product is intended for research and analytical applications. Novobiocin (Albamycin) sodium is a potent and orally active antibiotic. Novobiocin sodium also is a DNA gyrase inhibitor and a heat shock protein 90 (Hsp90) antagonist. Novobiocin sodium has the potential for the research of highly beta-lactam-resistant pneumococcal infections. Novobiocin sodium shows anti-orthopoxvirus activity .
|
-
- HY-B0425R
-
|
|
Antibiotic
DNA/RNA Synthesis
HSP
Apoptosis
Bacterial
Orthopoxvirus
|
Infection
Cancer
|
|
Novobiocin (Standard) is the analytical standard of Novobiocin. This product is intended for research and analytical applications. Novobiocin (Albamycin) is a potent and orally active antibiotic. Novobiocin also is a DNA gyrase inhibitor and a heat shock protein 90 (Hsp90) antagonist. Novobiocin has the potential for the research of highly beta-lactam-resistant pneumococcal infections. Novobiocin shows anti-orthopoxvirus activity [4] .
|
-
- HY-13425
-
|
(-)-Deguelin; (-)-cis-Deguelin
|
Akt
Autophagy
Apoptosis
|
Cancer
|
|
Deguelin, a naturally occurring rotenoid, acts as a chemopreventive agent by blocking multiple pathways like PI3K-Akt, IKK-NF-κB, and MAPK-mTOR-survivin-mediated apoptosis. Deguelin binding to Hsp90 leads to a decreased expression of numerous oncogenic proteins, including MEK1/2, Akt, HIF1α, COX-2, and NF-κB.
|
-
- HY-17504
-
|
Rosuvastatin hemicalcium; ZD 4522 Calcium
|
HMG-CoA Reductase (HMGCR)
Autophagy
Potassium Channel
Bacterial
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
Rosuvastatin Calcium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC50 of 11 nM. Rosuvastatin Calcium potently blocks hERG current with an IC50 of 195 nM . Rosuvastatin Calcium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Calcium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .
|
-
- HY-N6712
-
|
Acetopyrrothin
|
Bacterial
Antibiotic
Endogenous Metabolite
Deubiquitinase
|
Infection
Metabolic Disease
|
|
Thiolutin (Acetopyrrothin) is a disulfide-containing antibiotic and anti-angiogenic compound produced by Streptomyces. Thiolutin inhibits the JAMM metalloproteases Csn5, Associated-molecule-with-the-SH3-Domain-of-STAM (AMSH) and Brcc36 . Thiolutin is a potent and selective inhibitor of endothelial cell adhesion accompanied by rapid induction of Heat-shock protein beta-1 (Hsp27) phosphorylation .
|
-
- HY-13479
-
|
|
HSP
|
Cancer
|
|
EC144 is a potent and selective inhibitor of heat shock protein 90 (Hsp90) with an IC50 of 1.1 nM. EC144 inhibits tumor growth and causes partial tumor regressions. EC144 has the potential for the research of cancer diseases . EC144 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-153881
-
|
|
Ras
|
Cancer
|
|
KRAS G12C degrader-1 (Compound 283) is a potent KRAS G12C degrader (DC50: < 100 nM) for cancer research. KRAS G12C degrader-1 is a chaperone-mediated protein degrader (CHAMPs). Pink: KRAS G12C ligand (HY-112493); Blue: HSP90 ligand (HY-170326). Black: linker .
|
-
- HY-15990
-
|
|
HSP
|
Cancer
|
|
CH5164840 (16) shows high binding affinity for N-terminal Hsp90a (Kd = 0.52 nM) and strong anti-proliferative activity against human cancer cell lines (HCT116 IC50 = 0.15 μM, NCI-N87 IC50 = 0.066 μM). CH5164840 (16) is orally active (t1/2 = 2.64 h) with potent antitumor efficacy .
|
-
- HY-N6769
-
|
Monorden
|
HSP
Bacterial
Antibiotic
Parasite
|
Infection
|
|
Radicicol is an inhibitor of Hsp90 with an IC50 value < 1 μM, and leads to proteasomal degradation . Radicicol exhibits inhibition on PDK with IC50s of 230 μM (PDK1) and 400 μM (PDK3). Radicicol is an antifungal and antimalarial antibiotic, impairs mitochondrial replication by targeting P. falciparum topoisomerase VIB . Radicicol is also an inhibitor of fat mass and obesity-associated protein (FTO), with an IC50 value of 16.04 μM .
|
-
- HY-162567
-
|
|
HSP
|
Cancer
|
|
AP-4-139B is a heat shock protein 70 inhibitor (IC50=180 nM). HSP70 is a protein that is overexpressed in many types of cancer and is closely related to the survival and proliferation of tumor cells. AP-4-139B exhibits significant cytotoxicity to tumor cells, particularly in colorectal cancer cells. AP-4-139B can be used for cancer research .
|
-
- HY-114211
-
|
|
Histone Methyltransferase
HSP
|
Cancer
|
|
SGC8158 is an inhibitor of PRMT7 and can be used to study the cellular function of PRMT7. SGC8158 decreases monomethylarginine levels of Hsp70 (the best characterized PRMT7 substrate). SGC8158 induces growth inhibition in various cancer cells (IC50: 2-9 μM), as well as multidrug-resistant (MDR) cancer cells. SGC8158 also enhances Doxorubicin (HY-15142A) induced DNA damage and Its cytotoxicity .
|
-
- HY-17504A
-
|
ZD 4522
|
HMG-CoA Reductase (HMGCR)
Autophagy
Potassium Channel
Bacterial
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
Rosuvastatin (ZD 4522) is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM. Rosuvastatin potently blocks hERG current with an IC50 of 195 nM, delayed cardiac repolarization, and thereby prolonged action potential durations (APDs) and corrected QT interval (QTc) intervals. Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .
|
-
- HY-145102
-
|
|
HSP
Apoptosis
|
Cancer
|
|
NCT-58 is a potent inhibitor of C-terminal HSP90. NCT-58 does not induce the heat shock response (HSR) due to its targeting of the C-terminal region and elicits anti-tumor activity via the simultaneous downregulation of HER family members as well as inhibition of Akt phosphorylation. NCT-58 kills Trastuzumab-resistant breast cancer stem-like cells. NCT-58 induces apoptosis in HER2-positive breast cancer cells .
|
-
- HY-153202
-
|
|
MDM-2/p53
Apoptosis
|
Cancer
|
|
SLMP53-2 is a mutant p53 reactivator. SLMP53-2 restores wild-type-like conformation and DNA-binding ability of mutp53-Y220C by enhancing its interaction with the Hsp70, leading to the reestablishment of p53 transcriptional activity. SLMP53-2 can induce cell cycle arrest, apoptosis and endoplasmic reticulum (ER) stress. SLMP53-2 exhibits antitumor activity .
|
-
- HY-17504R
-
|
Rosuvastatin hemicalcium (Standard); ZD 4522 Calcium (Standard)
|
HMG-CoA Reductase (HMGCR)
Autophagy
Potassium Channel
Bacterial
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
Rosuvastatin (Calcium) (Standard) is the analytical standard of Rosuvastatin (Calcium). This product is intended for research and analytical applications. Rosuvastatin Calcium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC50 of 11 nM. Rosuvastatin Calcium potently blocks hERG current with an IC50 of 195 nM . Rosuvastatin Calcium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Calcium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .
|
-
- HY-17504BS2
-
|
ZD 4522-13C,d3 sodium; X-Plended-13C,d3 sodium; Crestor-13C,d3 sodium
|
Autophagy
Bacterial
HMG-CoA Reductase (HMGCR)
Potassium Channel
Isotope-Labeled Compounds
|
Cardiovascular Disease
Metabolic Disease
|
|
Rosuvastatin- 13C,d3 sodium is 13C and deuterated labeled Rosuvastatin sodium (HY-17504B). Rosuvastatin Sodium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC50 of 11 nM. Rosuvastatin Sodium potently blocks hERG current with an IC50 of 195 nM . Rosuvastatin Sodium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Sodium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .
|
-
- HY-158204
-
|
|
Lipoxygenase
|
Neurological Disease
|
|
CNB-001 is a potent 5-lipoxygenase (5-LOX) inhibitor, decreases 5-LOX expression, and increases proteasome activity. CNB-001 also increases eIF2α phosphorylation and HSP90 and ATF4 levels in Alzheimer's disease transgenic mice, and limits the accumulation of soluble Aβ and ubiquitinated aggregated proteins. CNB-001 maintains the expression of synapse-associated proteins and improves memory. CNB-001 can be used for the research of Alzheimer's disease .
|
-
- HY-162751
-
|
|
HSP
Apoptosis
|
Cancer
|
|
Anticancer agent 249 (Compound 89) is an inhibitor for Hsp90β with IC50 of 16.5 μM in PC3MM2 cell. Anticancer agent 249 inhibits proliferation of cancer cells MCF-7, T47D, MDA-MB-231, MDA-MB-468 and SKBr3 with IC50 of 1.8-5.3 μM. Anticancer agent 249 induces apoptosis in MDA-MB-231. Anticancer agent 249 exhibits antitumor efficacy in mice .
|
-
- HY-B0510
-
|
|
Antifolate
Bacterial
Antibiotic
Influenza Virus
|
Infection
Cancer
|
|
Trimethoprim is a bacteriostatic antibiotic and an orally active dihydrofolate reductase inhibitor. Trimethoprim is active against a wide range of Gram-positive and Gram-negative aerobic bacteria. Trimethoprim has the potential for the research of urinary tract infections, Shigellosis and Pneumocystis pneumonia. Trimethoprim can inhibit infection of Influenza A virus in chick embryo when combinated with zinc .
|
-
- HY-B0510B
-
|
|
Antifolate
Bacterial
Antibiotic
Influenza Virus
|
Infection
Cancer
|
|
Trimethoprim hydrochloride is a bacteriostatic antibiotic and an orally active dihydrofolate reductase inhibitor. Trimethoprim hydrochloride is active against a wide range of Gram-positive and Gram-negative aerobic bacteria. Trimethoprim hydrochloride has the potential for the research of urinary tract infections, Shigellosis and Pneumocystis pneumonia. Trimethoprim hydrochloride can inhibit infection of Influenza A virus in chick embryo when combinated with zinc .
|
-
- HY-B0510R
-
|
|
Antifolate
Bacterial
Antibiotic
Influenza Virus
|
Infection
|
|
Trimethoprim (Standard) is the analytical standard of Trimethoprim. This product is intended for research and analytical applications. Trimethoprim is a bacteriostatic antibiotic and an orally active dihydrofolate reductase inhibitor. Trimethoprim is active against a wide range of Gram-positive and Gram-negative aerobic bacteria. Trimethoprim has the potential for the research of urinary tract infections, Shigellosis and Pneumocystis pneumonia. Trimethoprim can inhibit infection of Influenza A virus in chick embryo when combinated with zinc .
|
-
- HY-17504D
-
|
|
HMG-CoA Reductase (HMGCR)
Potassium Channel
Autophagy
|
Cardiovascular Disease
Metabolic Disease
|
|
(3S,5R)-Rosuvastatin is the (3S,5R)-enantiomer of Rosuvastatin. Rosuvastatin is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM . Rosuvastatin potently blocks human ether-a-go-go related gene (hERG) current with an IC50 of 195 nM . Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin is very effective in lowering low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .
|
-
- HY-17504C
-
|
|
HMG-CoA Reductase (HMGCR)
Potassium Channel
Autophagy
|
Cardiovascular Disease
Metabolic Disease
|
|
(3R,5R)-Rosuvastatin is the (3R,5R)-enantiomer of Rosuvastatin. Rosuvastatin is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM . Rosuvastatin potently blocks human ether-a-go-go related gene (hERG) current with an IC50 of 195 nM . Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin is very effective in lowering low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .
|
-
- HY-W010649
-
|
|
Antibiotic
HSP
|
Others
Cancer
|
|
Isoxazole possesses broad biological activities with low cytotoxicity (e.g. anti-microbial, antibacterial, antifungal, anti-viral, anti-cancer, anti-inflammatory, immunomodulatory, analgesic, antituberculous or anti-diabetic properties), which is a member of five-membered heterocycles for a agent scaffold. Isoxazole with reversed ring can be used as HSP90 inhibitor. Isoxazole has been explored as BET bromodomain inhibitor and tricyclic Isoxazole is a promising for selective multidrug resistance protein (MRP1) inhibitors. Isoxazole is promising for research of various inhibitors and diseases .
|
-
- HY-155063
-
|
|
HSP
Mitochondrial Metabolism
|
Cancer
|
|
TRAP1-IN-1 (compound 35) is a potent and selective inhibitor of TRAP1，a mitochondrial isoform of Hsp90. TRAP1-IN-1 has >250-fold TRAP1 selectivity over Grp94，and disrupts TRAP1 tetramer stability，induces TRAP1 client protein degradation. TRAP1-IN-1 also inhibits mitochondrial complex I of oxidative phosphorylation OXPHOS，disrupts the mitochondrial membrane potential，and enhances glycolysis metabolism .
|
-
- HY-168577
-
|
|
Ras
|
Cancer
|
|
KRAS G12D inhibitor 25 (Compound 148) is an inhibitor for KRAS G12C and HSP90α with IC50 of < 0.1 μM and 0.1-1 μM, respectively. KRAS G12D inhibitor 25 inhibits the proliferation of MIA PaCa-2 and NCI-H358 with EC50 of < 0.1 μM and 0.1-1 μM, respectively. KRAS G12D inhibitor 25 degrades ERBB2 with a DC50 of 0.1-1 μM .
|
-
- HY-148877
-
|
|
HSP
HSV
HIF/HIF Prolyl-Hydroxylase
VEGFR
NF-κB
ERK
Akt
FAK
|
Infection
Inflammation/Immunology
Cancer
|
|
AT-533 is a potent Hsp90 and HSV inhibitor. AT-533 suppresses tumor growth and angiogenesis by blocking the HIF-1α/VEGF/VEGFR-2 signaling pathway. AT-533 also inhibits the activation of the downstream pathways, including Akt/mTOR/p70S6K, Erk1/2 and FAK. AT-533 inhibits the tube formation, cell migration, and invasion of human umbilical vein endothelial cells (HUVECs) .
|
-
- HY-113916
-
|
AT13387 lactate
|
HSP
|
Cancer
|
|
Onalespib lactate is a potent and cross the blood-brain barrier heat-shock-protein-90 (Hsp90) inhibitor with an Kd value of 0.71 nM. Onalespib lactate inhibits the proliferation, survival and migration. Onalespib lactate decreases the expression of EGFR, p-EGFR, AKT, P-AKT, ERK1/2, P-ERK1/2, S6, P-S6 protein. Onalespib lactate shows antitumor activity. Onalespib lactate has the potential for the research of non-small cell lung cancer (NSCLC) .
|
-
- HY-13644
-
|
15-Deoxyspergualin
|
Others
|
Others
|
|
Gusperimus is a fully synthetic racemate that has a novel mechanism of action by binding to the intracellular heat shock protein hsp70 and interfering with intracellular signal transduction. This mechanism of action can enhance the effect of immunosuppressive therapy. Gusperimus can inhibit the differentiation of T cells into cytotoxic T cells, reduce the expression of IL-2 receptors on CD4 and CD8 cells, and inhibit IFN-γ-induced B cell maturation. In addition, when used with cyclosporine, tacrolimus or mycophenolate mofetil, Gusperimus can enhance the immunosuppressive effect and prevent allogeneic transplant rejection.
|
-
- HY-N1934
-
|
|
Potassium Channel
HSP
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Dihydroberberine is a naturally occurring isoquinoline alkaloid with anti-inflammatory, anti-atherosclerotic, hypolipidemic and anti-tumor activities. Dihydroberberine inhibits the human ether-related gene (hERG) channel and significantly reduces the expression of heat shock protein 90 (Hsp90) and its interaction with hERG. Dihydroberberine also blocks the TLR4/MyD88/NF-κB signaling pathway to reduce pro-inflammatory cytokines and immunoglobulins, and has inhibitory effects on DSS (HY-116282C)-induced experimental colitis. Dihydroberberine also increases the sensitivity of lung cancer to sunitinib (HY-10255A), with synergistic efficacy .
|
-
- HY-121744
-
PS10
2 Publications Verification
|
PDHK
|
Inflammation/Immunology
|
|
PS10 is a novel, potent and ATP-competitive pan-PDK inhibitor, inhibits all PDK isoforms with IC50 of 0.8 μM, 0.76 μM, 2.1 μM and 21.3 μM for PDK2, PDK4, PDK1, and PDK3, respectively. PS10 shows high affinity for PDK2 (Kd= 239 nM) than for Hsp90 (Kd= 47 μM) . PS10 improves glucose tolerance, stimulates myocardial carbohydrate oxidation in diet-induced obesity. PS10 has the potential for the investigation of diabetic cardiomyopathy .PDK: pyruvate dehydrogenase kinase
|
-
- HY-118783
-
|
(±)-2-Hexyl-4-pentynoic acid
|
HDAC
HSP
|
Neurological Disease
|
|
2-Hexyl-4-pentynoic acid ((±)-2-Hexyl-4-pentynoic acid), valproic acid (VPA) derivative, exhibits potential roles of HDAC inhibition (IC50=13 μM) and HSP70 induction. Potent neuroprotective effects. 2-Hexyl-4-pentynoic acid causes histone hyperacetylation and protect against glutamate-induced excitotoxicity in cultured neurons . 2-Hexyl-4-pentynoic acid is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-161826
-
|
|
β-catenin
HSP
CDK
c-Myc
|
Cancer
|
|
Antitumor agent-174 (Compound 10) directly engages the N-terminal site of Hsp90 and promotes the degradation of β-catenin, thereby suppressing the Wnt/β-catenin signaling. Antitumor agent-174 effectively inhibits proliferation, induce S and G2/M phases arrest and block the clonogenic ability in CRC cells. Antitumor agent-174 down-regulates CDK1, Cyclin D1, c-Myc, Cyclin B1, and Cyclin A2, and upregulaties P21 proteins. Antitumor agent-174 has significant anti-tumor efficacy against colorectal cancer (CRC) with excellent pharmacokinetics and low toxicity .
|
-
- HY-N1934R
-
|
|
Potassium Channel
HSP
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Dihydroberberine (Standard) is the analytical standard of Dihydroberberine. This product is intended for research and analytical applications. Dihydroberberine is a naturally occurring isoquinoline alkaloid with anti-inflammatory, anti-atherosclerotic, hypolipidemic and anti-tumor activities. Dihydroberberine inhibits the human ether-related gene (hERG) channel and significantly reduces the expression of heat shock protein 90 (Hsp90) and its interaction with hERG. Dihydroberberine also blocks the TLR4/MyD88/NF-κB signaling pathway to reduce pro-inflammatory cytokines and immunoglobulins, and has inhibitory effects on DSS (HY-116282C)-induced experimental colitis. Dihydroberberine also increases the sensitivity of lung cancer to sunitinib (HY-10255A), with synergistic efficacy .
|
-
- HY-152263
-
|
|
PROTACs
CDK
Apoptosis
|
Cancer
|
|
HEMTAC CDK4/6 degrader 1 is a PROTAC connected by ligands for HSP90 and CDK4/6 with a Kd value of 35.7 μM. HEMTAC CDK4/6 degrader 1 induces CDK4/6 degradation in B16F10 melanoma cells. HEMTAC CDK4/6 degrader 1 arrests cell cycle at G0/G1 phase and induces apoptosis. HEMTAC CDK4/6 degrader 1 can be used in research of cancer . HEMTAC CDK4/6 degrader 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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-
- HY-121708
-
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Others
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Cancer
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KI-328 is a novel inhibitor targeting KIT kinase that has selective activity against some KIT mutant kinases commonly found in acute myeloid leukemia (AML). KI-328 showed specificity for KIT kinase in in vitro kinase assays and inhibited the growth of wild-type (Wt) and mutant KIT-expressing cells, but had lower activity against D816V-KIT. Comparative analysis of the inhibitory effects of several potent KIT inhibitors on the growth of multiple mutant KIT-expressing cells showed that the multi-kinase inhibitors had comparable activity against D816V-KIT as against other mutant KITs; however, heat shock protein 90 (HSP90) inhibitors showed significant activity against D816V-KIT, inhibiting the growth of D816V-KIT-expressing cells at concentrations that did not affect the growth of other mutant KIT-expressing cells. These results suggest that potent KIT inhibitors have different activities against different types of KIT mutant kinases. Therefore, in clinical development, KIT inhibitors need to validate their activity against multiple types of KIT mutant kinases.
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| Cat. No. |
Product Name |
Type |
-
- HY-133705
-
|
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Fluorescent Dyes/Probes
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Geldanamycin-FITC, a Geldanamycin fluorescent probe, can be used in a fluorescence polarization assay for HSP90 inhibitors. Geldanamycin-FITC also can be used for detection of cell surface HSP90 .
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- HY-D2360
-
|
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Fluorescent Dyes/Probes
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O-Carboranylphenoxyacetanilide is a HIF-1α inhibitor and inhibits HIF-1α activation. O-Carboranylphenoxyacetanilide inhibits transcriptional activity of HIF in HeLa cells (IC50: 0.74 μM). O-Carboranylphenoxyacetanilide inhibits HSP60 chaperone activity and HSP60 ATPase activity .
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- HY-122878
-
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Fluorescent Dyes/Probes
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HS-131, a near infrared dye tethered Hsp90 inhibitor, is able to detect oncogene-driven breast cancers, including multiple different molecular subtypes of human breast cancers .
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| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-W014102
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-
- HY-P1896
-
|
|
HSP
|
Infection
Neurological Disease
Cancer
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Hsp70-derived octapeptide is a conserved octapeptide of the C-terminal end of Hsp70, which physically interacts with tetratricopeptide repeat (TPR) motifs .
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- HY-P10072A
-
|
Hsp25 kinase inhibitor acetate; Mk2 pseudosubstrate acetate
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JNK
HSP
MAPKAPK2 (MK2)
p38 MAPK
ERK
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Others
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|
MK2-IN-5 (Hsp25 kinase inhibitor) acetate is a Mk2 pseudosubstrate (Ki= 8 μM). MK2-IN-5 acetate targets the protein interaction domain in the MAPK pathway. MK2-IN-5 acetate inhibits HSP25 and HSP27 phosphorylation .
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- HY-P1750A
-
|
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HSP
Survivin
|
Cancer
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Shepherdin (79-87) TFA is amino acids 79 to 87 fragment of Shepherdin. Shepherdin is a peptidomimetic antagonist of the complex between Hsp90 and Survivin. Anticancer activity .
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- HY-105063
-
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Peptides
|
Metabolic Disease
Inflammation/Immunology
|
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DiaPep277 is a 24 amino acid peptide derived from positions 437-460 in HSP60. DiaPep277 arrests the progression of β-cell destruction in NOD mice. DiaPep277 has an immune modulatory effect on diabetogenic T cells in animal models of diabetes .
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- HY-W014102R
-
|
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Endogenous Metabolite
|
Metabolic Disease
Inflammation/Immunology
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L-Alanyl-L-glutamine (Standard) is the analytical standard of L-Alanyl-L-glutamine. This product is intended for research and analytical applications. L-Alanyl-L-glutamine, a glutamine dipeptide, is benefit for the antioxidant system, attenuating inflammation, and may modulate the heat shock protein (HSP) response in catabolic situations .
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-
- HY-P10541
-
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Peptides
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Others
|
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HSP70/DnaK substrate peptide is a short peptide that the HSP70/DnaK molecular chaperone can bind and act on. HSP70/DnaK substrate peptide can be used to study the mechanism of action of HSP70/DnaK in molecular chaperone function .
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-
- HY-P10072
-
|
Hsp25 kinase inhibitor; Mk2 pseudosubstrate
|
ERK
JNK
p38 MAPK
HSP
MAPKAPK2 (MK2)
|
Others
|
|
MK2-IN-5 is a Mk2 pseudosubstrate (Ki= 8 μM). MK2-IN-5 targets the protein interaction domain in the MAPK pathway. MK2-IN-5 inhibits HSP25 and HSP27 phosphorylation .
|
-
- HY-P1750
-
|
|
HSP
Survivin
|
Cancer
|
|
Shepherdin (79-87) is amino acids 79 to 87 fragment of Shepherdin. Shepherdin is a peptidomimetic antagonist of the complex between Hsp90 and Survivin. Anticancer activity .
|
-
- HY-P10635
-
|
|
Peptides
|
Inflammation/Immunology
|
|
TKD (450-463) is a 14-mer peptide (TKDNNLLGRFELSG). TKD (450-463) is able to stimulate the cytolytic and proliferative activity of NK cells at concentrations equivalent to full-length Hsp70 protein .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P9962
-
|
|
Fungal
|
Infection
|
|
Efungumab is a monoclonal antibody with antifungal activity. Efungumab binds to HSP 90, preventing a conformational change needed for fungal viability. Efungumab can be used for research on invasive candidiasis (IC) .
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-13757AS
-
|
|
|
Tamoxifen-d5 is a deuterium labeled Tamoxifen. Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM). Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity[1][2].
|
-
-
- HY-13757S
-
|
|
|
Tamoxifen-d3 hydrochloride is deuterated labeled Tamoxifen (Citrate) (HY-13757). Tamoxifen Citrate (ICI 46474) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells .Tamoxifen Citrate is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen Citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively . Tamoxifen Citrate activates autophagy and induces apoptosis .Tamoxifen Citrate also can induce gene knockout of CreER(T2) transgenic mouse .
|
-
-
- HY-13757AS1
-
|
|
|
Tamoxifen-d3 is the deuterium labeled Tamoxifen[1]. Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells[2][3][4]. Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively[6]. Tamoxifen activates autophagy and induces apoptosis[5]. Tamoxifen also can induce gene knockout of CreER(T2) transgenic mouse[7].
|
-
-
- HY-17504BS2
-
|
|
|
Rosuvastatin- 13C,d3 sodium is 13C and deuterated labeled Rosuvastatin sodium (HY-17504B). Rosuvastatin Sodium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC50 of 11 nM. Rosuvastatin Sodium potently blocks hERG current with an IC50 of 195 nM . Rosuvastatin Sodium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Sodium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .
|
-
| Cat. No. |
Product Name |
|
Classification |
-
- HY-117395
-
|
|
|
Alkynes
|
|
PU-H54, a Grp94-selective inhibitor, can be used for the research of breast cancer. Hsp90 chaperone family, comprised in humans of four paralogs, Hsp90α, Hsp90β, Grp94 and Trap-1, has important roles in malignancy . PU-H54 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-118783
-
|
(±)-2-Hexyl-4-pentynoic acid
|
|
Alkynes
|
|
2-Hexyl-4-pentynoic acid ((±)-2-Hexyl-4-pentynoic acid), valproic acid (VPA) derivative, exhibits potential roles of HDAC inhibition (IC50=13 μM) and HSP70 induction. Potent neuroprotective effects. 2-Hexyl-4-pentynoic acid causes histone hyperacetylation and protect against glutamate-induced excitotoxicity in cultured neurons . 2-Hexyl-4-pentynoic acid is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-169098
-
|
|
|
Alkynes
|
|
HSP90/LSD1-IN-1 (compound 6) is a HSP90/LSD1 dual inhibitor. HSP90/LSD1-IN-1 inhibits the proliferation of prostate cancer cell lines PC-3 and DU145, with GI50 values of 0.24 and 0.30 μM, respectively .
|
| Cat. No. |
Product Name |
|
Classification |
-
- HY-145722
-
|
OGX-427 sodium
|
|
Antisense Oligonucleotides
|
|
Apatorsen (sodium) is an antisense oligonucleotide designed to bind to Hsp27 mRNA, resulting in the inhibition of the production of Hsp27 protein.
|
-
- HY-145722A
-
|
OGX-427
|
|
Antisense Oligonucleotides
|
|
Apatorsen is an antisense oligonucleotide designed to bind to Hsp27 mRNA, resulting in the inhibition of the production of Hsp27 protein.
|
-
- HY-RS06415
-
|
|
|
siRNAs
Pre-designed siRNA Sets
|
|
HSP90AA1 Human Pre-designed siRNA Set A contains three designed siRNAs for HSP90AA1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
- HY-RS06416
-
|
|
|
siRNAs
Pre-designed siRNA Sets
|
|
Hsp90aa1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Hsp90aa1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
- HY-RS06417
-
|
|
|
siRNAs
Pre-designed siRNA Sets
|
|
Hsp90aa1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Hsp90aa1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
- HY-RS06418
-
|
|
|
siRNAs
Pre-designed siRNA Sets
|
|
HSP90AB1 Human Pre-designed siRNA Set A contains three designed siRNAs for HSP90AB1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
- HY-RS06419
-
|
|
|
siRNAs
Pre-designed siRNA Sets
|
|
HSP90B1 Human Pre-designed siRNA Set A contains three designed siRNAs for HSP90B1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
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