Search Result
Results for "
Hsps
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
8
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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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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-
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- HY-W014102
-
-
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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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-
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- HY-100110
-
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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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-
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- HY-18669
-
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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-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 nM.
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-
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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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-
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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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-
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- HY-13469
-
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CUDC-305
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HSP
|
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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-
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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-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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-
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- HY-148215A
-
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HSP
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Neurological Disease
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-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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-
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- HY-W107935
-
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HSP
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Cancer
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Hsp90-IN-37 (Z-2) is a heat shock protein 90 (Hsp90) inhibitor that inhibits Hsp90 enzymatic activity by 69%. Hsp90-IN-37 has antitumor activity .
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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-170944
-
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HSP
Apoptosis
Caspase
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Cancer
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BAG3/HSP70-IN-1 (compound 16) is the first-in-class BAG3 and HSP70 dual inhibitor. BAG3/HSP70-IN-1 binds to BAG3 full-length, BAG3-BD, and HSP70 proteins with Kds of 33.10 μM, 27.90 μM, and 33.80 μM, respectively. BAG3/HSP70-IN-1 inhibits HeLa cells with an IC50 of 49.46 μM. BAG3/HSP70-IN-1 induces apoptosis by activating caspase 3 and caspase 9 levels in HeLa cells. BAG3/HSP70-IN-1 elevates p21 levels while reduces FOXM1 expression in HeLa cells. BAG3/HSP70-IN-1 decreases ATPase activity .
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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-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-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-175865
-
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HSP
Apoptosis
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Cancer
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HSP70-IN-7 is a nonselective HSP70 inhibitor with Kds of 4.71, 2.16 and 2.93μM against HSP70, GRP75, and GRP78. HSP70-IN-7 exhibits selective toxicity against breast cancer cells, induces cell apoptosis and effectively suppresses the properties of breast cancer stem cells (BCSCs). HSP70-IN-7 can be used for the study of breast cancer .
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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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-
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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-176279
-
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HSP
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Cancer
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Hsp90-IN-42 (Compound 13l) is a potent heat shock protein 90 (Hsp90) inhibitor (IC50=15.65 nM). Hsp90-IN-42 reduces the stability of the epidermal growth factor receptor (EGFR), suppressing the activation of the EGFR-Akt signaling pathway, inducing G0/G1 phase arrest in colorectal cancer cells (such as HT-29 cells), and slightly triggering apoptosis. Hsp90-IN-42 also inhibits cell proliferation and migration by down-regulating the expression of CDK12, CDK13, and Bcl-2 proteins, and up-regulating the expression of Bax protein. Hsp90-IN-42 is promising for research of colorectal cancer .
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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-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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- HY-178462
-
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HSP
DNA/RNA Synthesis
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Cancer
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Hsp70/FoxM1-IN-1 (Compound 7d) is a potent heat shock protein 70 (Hsp70) and Forkhead box M1 (FoxM1) dual inhibitor. Hsp70/FoxM1-IN-1 demonstrates significant antiproliferative and pro-apoptotic effects in multiple solid tumor models (e.g., breast, colorectal cancer), particularly for tumors co-overexpressing Hsp70/FoxM1 .
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- HY-174476
-
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HSP
Drug Intermediate
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Cancer
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HSP90i is a HSP90 inhibitor. HSP90i can be used as a drug intermediate to synthesize LYTACs, such as dPDL1-4 (HY-174468) .
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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-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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-
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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-170326
-
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Ligands for Target Protein for PROTAC
HSP
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Cancer
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Hsp90-in-35 (Compound 379) is an inhibitor of Hsp90. The IC50 of HSP90-IN-35 for Her2 is between 0.05 and 0.5 μM. HSP90-IN-35 has antitumor activity. HSP90-IN-35 can be used to synthesize PROTAC (HY-153881) .
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- HY-P10541
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HSP
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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-P10541A
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HSP
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Others
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HSP70/DnaK substrate peptide TFA is a short peptide that the HSP70/DnaK molecular chaperone can bind and act on. HSP70/DnaK substrate peptide TFA can be used to study the mechanism of action of HSP70/DnaK in molecular chaperone function .
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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-171755
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HSP
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Cancer
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Hsp90-IN-40 (Compound 15b) is a heat shock protein 90 (Hsp90) C-terminal inhibitor. Hsp90-IN-40 exhibits antiproliferative activity against SKBr3 and MCF-7 breast cancer cells (IC50 of 2.57 µM and 2.43 µM, respectively). Hsp90-IN-40 inhibits cancer cell growth by inhibiting the Hsp90 C-terminal function, leading to Hsp90-dependent protein degradation. Hsp90-IN-40 can be used in breast cancer research .
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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-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-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-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-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-170895
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HSP
Na+/K+ ATPase
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Cancer
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Hsp90-IN-38 (compound 20m) is a HSP90 (heat shock protein) inhibitor. Hsp90-IN-38 exhibits strong HSP90 binding affinity with a Kd of 87 nM. Hsp90-IN-38 inhibits ATPase with an IC50 of 0.13 μM. Hsp90-IN-38 inhibits HCT116, MCF-7, SKBr3, K562 and A549 cells with IC50s of 0.187, 0.072, 0.105, 0.403 and 031 μM, respectively .
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- HY-170910
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HSP
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Cancer
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Hsp90-IN-39 (Compound 16t) is a HSP90 inhibitor with notable selectivity for the HSP90α isoform. Hsp90-IN-39 demonstrates significant antiproliferative activity in various cancer cell lines, including MCF-7, HCT116, SKBr3, K562, and A549. Hsp90-IN-39 holds potential for cancer research .
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- HY-179377
-
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HSP
Tau Protein
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Neurological Disease
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Aha1/Hsp90-IN-2 is a selective inhibitor of the Hsp90/Aha1 interaction, with its IC50 being 1.46 μM. Aha1/Hsp90-IN-2 inhibits the activation of Hsp90 ATPase activity mediated by Aha1 by specifically blocking the binding of Hsp90 to Aha1, thereby reducing tau protein aggregation. Aha1/Hsp90-IN-2 can be used for the study of neurodegenerative diseases, such as Alzheimer's disease .
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- HY-177042
-
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HSP
Fungal
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Infection
Cancer
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Hsp90-IN-41 (Compound C1) is an inhibitor of Hsp90 (IC50 = 0.044 μM). Hsp90-IN-41 exhibits antifungal and antitumor (IC50 = 0.049 μM) activities in vitro .
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- HY-173337
-
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HSP
Interleukin Related
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Cancer
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HSP90α-IN-1 is a HSP90α inhibitor (IC50 = 111 nM) that exhibits senolytic activity across various cellular senescence models. HSP90α-IN-1 is related to the xanthinic family. HSP90α-IN-1 is involved in research on combating age-related inflammaging and diseases, including cancer, and possibly extend a healthy lifespan .
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- HY-179012
-
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APC
CDK
Raf
Akt
HSP
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Cancer
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CDC20/HSP90-IN-1 (Compound 2b) is a Cdc20/Hsp90 inhibitor with a Kd of 16.2 μM for Cdc20 and a Kd of 0.241 μM for Hsp90α. CDC20/HSP90-IN-1 exerts potent antitumor activity through reducing p53-mediated Cdc20, upregulating Bim, downregulating Cyclin B1 expression, and disturbing B-Raf and AKT pathways via destroying Hsp90 chaperone function. CDC20/HSP90-IN-1 overcomes Vemurafenib (HY-12057)-induced resistant melanoma .
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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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-
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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-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-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-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-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-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-175008
-
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HSP
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Others
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Hsp90β-IN-1 (Compound 7b) is a selective biotinylated inhibitor of heat shock protein 90β (HSP90β) with an IC50 = 0.33 μM .
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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-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-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-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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Reference Standards
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
-
-
- 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-152027
-
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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-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-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-170816
-
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HSP
Cytochrome P450
Fungal
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Infection
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CYP51/Hsp90-IN-1 (Compound MM4) is a dual CYP51/Hsp90 inhibitor. CYP51/Hsp90-IN-1 shows antifungal activity against Candida albicans and effectively inhibits important fungal virulence factors. CYP51/Hsp90-IN-1 is promising for research of invasive candidiasis .
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- HY-168178
-
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HSP
STAT
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Cardiovascular Disease
|
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Hsp110-STAT3 PPI-IN-2 (compound 10b) is a Hsp110-STAT3 interaction disruptor. Hsp110-STAT3 PPI-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
|
Cancer
|
|
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 .
|
-
- HY-174347
-
|
|
HSP
Casein Kinase
Apoptosis
|
Cancer
|
|
Hsp90-Cdc37-IN-4, a Celastrol (HY-13067) derivative, inhibits the Hsp90-Cdc37 protein-protein interaction (PPI). Hsp90-Cdc37-IN-4 selectively inhibits casein kinase 2 (CK2), reducing phosphorylation of its substrate Cdc37 at Serine 13. Hsp90-Cdc37-IN-4 induces G0/G1 cell cycle arrest and triggers apoptosis via the mitochondrial pathway. Hsp90-Cdc37-IN-4 demonstrates potent anti-breast cancer activity .
|
-
- HY-163288
-
|
|
Histone Methyltransferase
HSP
Apoptosis
|
Cancer
|
|
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) .
|
-
- HY-150774
-
|
|
HDAC
HSP
Apoptosis
|
Cancer
|
|
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 .
|
-
- HY-169098
-
|
|
HSP
Histone Demethylase
|
Cancer
|
|
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 .
|
-
- HY-146212
-
|
|
HDAC
HSP
|
Cancer
|
|
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.
|
-
- HY-P1896
-
|
|
HSP
|
Infection
Neurological Disease
Cancer
|
|
Hsp70-derived octapeptide is a conserved octapeptide of the C-terminal end of Hsp70, which physically interacts with tetratricopeptide repeat (TPR) motifs .
|
-
- HY-170328
-
|
|
HSP
|
Cancer
|
|
Hsp90-IN-36 (compound 5) is a Hsp90 inhibitor with anticancer activity (MCF-7, IC50=14.74 μM) .
|
-
- HY-175467
-
|
|
HSP
HDAC
|
Cancer
|
|
HDAC6/HSP90-IN-3 (Compound 17) is an orally active dual histone deacetylase 6 (HDAC6) and heat shock protein 90 (HSP90) inhibitor with IC50 values of 28 nM and 0.88 μM, respectively. HDAC6/HSP90-IN-3 is promising for research of malignant tumors such as prostate cancer .
|
-
- HY-162900
-
|
|
HSP
|
Cancer
|
|
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 .
|
-
- HY-161833
-
|
|
Interleukin Related
TNF Receptor
|
Inflammation/Immunology
|
|
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 .
|
-
- HY-130624
-
|
|
HSP
Apoptosis
|
Cancer
|
|
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 .
|
-
- HY-178957
-
|
|
HSP
|
Cancer
|
|
Hsp90β-IN-2 (Compound 16B) is a selective Hsp90β inhibitor with KDs of 225 nM and 73.32 μM against Hsp90β and Hsp90α. KUNB106 exhibits antiproliferative activity against MDA-MB-231 cells, A549 and SKOV-3 cells. KUNB106 can be used for the study of triple negative breast cancer .
|
-
- HY-160145
-
|
|
HSP
|
Others
|
|
HSP70-IN-5 is a HSP70 inhibitor. HSP70-IN-5 exhibits IC₅₀ value for HSP70/DnaJ-mediated luciferase reconstitution of 0.6 μM. HSP70-IN-5 can be used as a biochemical probe to study the role of HSP70/DnaJ in various biological processes .
|
-
- HY-181478
-
|
|
HSP
|
Cancer
|
|
Hsp90-IN-45 is a Hsp90 inhibitor. Hsp90-IN-45 competitively binds to the ATP-binding site of purified Hsp90α with a Kd of 70 nM, blocks ATP hydrolysis, and disrupts Hsp90 client signaling. Hsp90-IN-45 inhibits ATPase activity of purified Hsp90α. Hsp90-IN-45 will be radiolabeled with 76/ 77Br for use as a radiotheragnostic agent for PET imaging and Meitner-Auger electron therapy. Hsp90-IN-45 can be used for the research of cancer .
|
-
- HY-184106
-
|
|
HSP
Caspase
|
Cancer
|
|
HSP70-IN-9 (Compound 27g) is a Hsp70 inhibitor. HSP70-IN-9 activates Caspase-3 and -7. HSP70-IN-9 exerts anticancer effects against acute myeloid leukemia. HSP70-IN-9 can be used for the research of acute myeloid leukemia .
|
-
- HY-179343
-
|
|
HSP
|
Cancer
|
|
Hsp90-IN-43 (Compound 12) is a Hsp90-TPR2A interaction inhibitor with an IC50 of 360 nM and a Kd of 928 nM. Hsp90-IN-43 effectively inhibits the proliferation of BT474 cells. Hsp90-IN-43 can be used for the study of breast cancer .
|
-
- HY-180163
-
|
|
HSP
Drug Derivative
|
Cancer
|
|
HSP70-IN-8 (Compound 1b) is a HSP70 inhibitor and Alpinetin (HY-N0625A) derivative. HSP70-IN-8 inhibits the expression of HSP70 protein.HSP70-IN-8 exhibits excellent anti-liver cancer activity .
|
-
- HY-160430
-
|
|
HSP
|
Cancer
|
|
HSP90-IN-28 (compound 12 h) is a potent and selective Hsp90 inhibitor with an IC50 of 0.46 μM for Hsp90α. HSP90-IN-28 exhibits ~48 fold selectivity versus other Hsp90β (IC50 = 22.28 μM) .
|
-
- HY-177875
-
|
|
HSP
|
Cancer
|
|
Hsp90-IN-44 (compound 16) is a Hsp90 inhibitor with an IC50 of 9.8 µM. Hsp90-IN-44 can be used for cancer research .
|
-
- HY-181687
-
|
|
HSP
CDK
|
Cancer
|
|
Hsp90-IN-46 is a Hsp90 inhibitor. Hsp90-IN-46 exhibits broad-spectrum antiproliferative activity against tumor cell lines. Hsp90-IN-46 inhibits breast cancer cell proliferation by reducing colony formation and downregulating the proliferation marker Ki-67. Hsp90-IN-46 inhibits Hsp90 and its ATPase activity, downregulates the downstream substrate oncoproteins HER2 and CDK4, and moderately induces the heat shock response. Hsp90-IN-46 shows significant antitumor activity in a mouse model of triple-negative breast cancer tumor xenografts. Hsp90-IN-46 can be used for research on various cancers including triple-negative breast cancer, leukemia, non-small cell lung cancer, colon cancer, ovarian cancer, renal cancer, prostate cancer .
|
-
- HY-186076
-
|
|
HSP
Fungal
|
Infection
Cancer
|
|
Hsp90-IN-47 (Compound C15) is a Hsp90 inhibitor and antifungal agent, with an IC50 of 0.014 μM against Hsp90α. When combined with Fluconazole (HY-B0101), Hsp90-IN-47 exerts significant synergistic antifungal effects against fluconazole-resistant Candida albicans 0304103. Hsp90-IN-47 exhibits antitumor activity against acute myeloid leukemia and non-small cell lung cancer .
|
-
- HY-116053
-
|
|
HSP
|
Neurological Disease
|
|
PU-11 is a Hsp90α/Hsp90β inhibitor with IC50 values of 18.6 μM and 89.8 μM and Kd values of 2 and 4.2 μM. PU-11 binds to the ATP-binding pocket of Hsp90α and Hsp90β and displays selective binding preference for Hsp90α over Hsp90β, mediated by the nonconserved Hsp90α Ser52 residue. PU-11 can be used for the research of neurodegenerative disorders .
|
-
- HY-100110R
-
|
Heat Shock Protein Inhibitor I (Standard)
|
HSP
Reference Standards
|
Cancer
|
|
KNK437 (Standard) is the analytical standard of KNK437 (HY-100110). This product is intended for research and analytical applications. KNK437 is a HSP inhibitor, and inhibits the induction of HSP105, HSP70, and HSP40.
|
-
- HY-181148
-
-
- HY-182979
-
|
|
HSP
|
Cancer
|
|
HSP70 ligand 2 is an HSP70 ligand and serves as a ligand for PROTAC target proteins. HSP70 ligand 2 can be used to synthesize Hsp70TAC BRD4 Degrader-1 (HY-182958) and Hsp70TAC PD-1 Degrader-2 (HY-182959) .
|
-
- HY-130273
-
|
|
HDAC
HSP
Microtubule/Tubulin
PD-1/PD-L1
|
Cancer
|
|
HDAC/HSP90-IN-1 (compound 20) is a potent dual inhibitor of HDAC (IC50 = 194 nM) and HSP90 (HSP90α IC50 = 153 nM). HDAC/HSP90-IN-1 induces HSP70 expression, downregulates HSP90 client proteins, and promotes acetylation of α-tubulin and histone H3 in cancer cells. HDAC/HSP90-IN-1 reduces PD-L1 expression in IFN-γ treated H1975 cells. HDAC/HSP90-IN-1 can be used for cancer research, such as lung and colon cancer .
|
-
- HY-130274
-
|
|
HDAC
HSP
Microtubule/Tubulin
PD-1/PD-L1
|
Cancer
|
|
HDAC/HSP90-IN-2 (compound 26) is a potent dual inhibitor of HDAC (IC50 = 360 nM) and HSP90 (HSP90α IC50 = 77 nM). HDAC/HSP90-IN-2 induces HSP70 expression, downregulates HSP90 client proteins, and promotes acetylation of α-tubulin and histone H3 in cancer cells. HDAC/HSP90-IN-2 reduces PD-L1 expression in IFN-γ treated H1975 cells. HDAC/HSP90-IN-2 can be used for cancer research, such as lung and colon cancer .
|
-
- HY-10214R
-
|
PF-04928473 (Standard)
|
Reference Standards
HSP
Autophagy
|
Cancer
|
|
SNX-2112 (Standard) is the analytical standard of SNX-2112 (HY-10214). This product is intended for research and analytical applications. 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 .
|
-
- HY-182959
-
|
|
Hsp-targeting Chimeras
LYTACs
PD-1/PD-L1
HSP
|
Cancer
|
|
Hsp70TAC PD-1 Degrader-2 is a PD-L1 Hsp70TAC (Hsp70-targeting Chimeras) degrader with Kd values of 0.36 μM. Hsp70TAC PD-1 Degrader-2 forms a ternary complex with Hsp70 and PD-L1 to drive PD-L1 degradation. Hsp70TAC PD-1 Degrader-2 induces degradation of mature membrane-bound PD-L1 in an Hsp70-dependent manner and via caveolin-mediated endocytosis and lysosomal trafficking. Hsp70TAC PD-1 Degrader-2 accumulates preferentially in tumor cells with elevated Hsp70 expression for tumor-selective PD-L1 degradation. Hsp70TAC PD-1 Degrader-2 can be used for the research of cancer, such as breast invasive carcinoma, glioblastoma multiforme, diffuse large b-cell lymphoma . (Pink: PD-1/PD-L1 ligand (HY-19745A); Blue: Hsp70 ligand (HY-182979); Black: linker (HY-182982)).
|
-
- HY-181147
-
|
|
PROTACs
HSP
|
Cancer
|
|
PROTAC HSP70 Degrader-1 (compound C4) is a cytosolic HSP70 PROTAC degrader that can engage CRBN to form a ternary complex. PROTAC HSP70 Degrader-1 mediates ubiquitination and proteasomal degradation of cytosolic HSP70. PROTAC HSP70 Degrader-1 exhibits cytotoxic activity against cancer cells, suppressing tumor cell proliferation and inducing apoptosis in combination with DTHIB. PROTAC HSP70 Degrader-1 can be used for the research of colon cancer and leukemia .
|
-
- HY-147974
-
|
|
HSP
Influenza Virus
|
Infection
|
|
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 .
|
-
- HY-15785
-
|
TAS-116
|
HSP
|
Cancer
|
|
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 .
|
-
- HY-10210
-
|
IPI-504
|
HSP
|
Cancer
|
|
Retaspimycin Hydrochloride is a potent inhibitor of Hsp90 with EC50s of 119 nM for both Hsp90 and Grp9.
|
-
- HY-15263
-
|
|
HSP
|
Cancer
|
|
Retaspimycin is a potent inhibitor of Hsp90, with EC50s of 119 nM for both Hsp90 and Grp9.
|
-
- HY-115997
-
|
|
PROTACs
HSP
|
Cancer
|
|
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.
|
-
- HY-117282
-
|
|
HSP
Apoptosis
|
Cancer
|
|
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 .
|
-
- HY-10389A
-
|
17-DMAG TFA; KOS-1022 TFA; NSC 707545 TFA
|
HSP
|
Cancer
|
|
Alvespimycin (17-DMAG) TFA is a potent inhibitor of Hsp90, binding to Hsp90 with an EC50 of 62 nM .
|
-
- HY-10941
-
|
|
HSP
Autophagy
|
Neurological Disease
Cancer
|
|
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.
|
-
- HY-P11185
-
|
|
HSP
|
Cancer
|
|
Hsp90β decapeptide is a C-terminal peptide of Hsp90β, which contains conserved TPR-domain MEEVD. Hsp90β decapeptide is able to bind tightly the Tah1 protein with a Kd of 1.0 μM .
|
-
- HY-174799
-
|
|
HSP
|
Cancer
|
|
HSP90i-COCH2CH2-PEG4-NHBoc is a conjugate of the HSP90 Ligand (HY-174476) and the linker (HY-W021787). HSP90i-COCH2CH2-PEG4-NHBoc can be used for synthesis of LYTACs, such as dPDL1-4 (HY-174468) .
|
-
- HY-10215R
-
|
VER-52296 (Standard); AUY922 (Standard); NVP-AUY922 (Standard)
|
Reference Standards
HSP
Autophagy
Apoptosis
|
Cancer
|
|
Luminespib (Standard) is the analytical standard of Luminespib. This product is intended for research and analytical applications. Luminespib (VER-52296) is a potent HSP90 inhibitor with IC50s of 7.8 and 21 nM for HSP90α and HSP90β, respectively .
|
-
- HY-153588
-
|
|
HSP
|
Cancer
|
|
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.
|
-
- HY-107599R
-
|
|
Reference Standards
JNK
Apoptosis
|
Neurological Disease
|
|
AEG3482 (Standard) is the analytical standard of AEG3482 (HY-107599). This product is intended for research and analytical applications. 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 .
|
-
- HY-12619
-
|
|
HSP
|
Cancer
|
|
DMT003096 is a HSP70 inhibitor. HSP70 has been reported to be upregulated in various cancers including breast, lung, colon, and cervix .
|
-
- HY-12024
-
|
17-DMAG hydrochloride; KOS-1022 hydrochloride; BMS 826476
|
HSP
Apoptosis
|
Cancer
|
|
Alvespimycin hydrochloride (17-DMAG hydrochloride; KOS-1022; BMS 826476) is a potent inhibitor of Hsp90, binding to Hsp90 with EC50 of 62±29 nM.
|
-
- HY-12933
-
|
|
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-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-182958
-
|
|
Hsp-targeting Chimeras
Epigenetic Reader Domain
HSP
|
Cancer
|
|
Hsp70TAC BRD4 Degrader-1 is a degrader targeting BRD4, with a KD value of 0.22 μM. Hsp70TAC BRD4 Degrader-1 forms a ternary complex with Hsp70 (KD: 5.13 μM), and specifically and efficiently degrades intracellular BRD4 via the ubiquitin-proteasome pathway. Hsp70TAC BRD4 Degrader-1 exhibits potent anti-tumor proliferative activity. Hsp70TAC BRD4 Degrader-1 can be used in studies related to triple-negative breast cancer and glioblastoma multiforme. (Pink: BRD4 ligand (HY-78695); Blue: HSP70 ligand (HY-182979); Black: linker (HY-B0236)) .
|
-
- 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-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-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-170453
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
iHAC is an inhibitor HSP90-anchoring chimera, that covalently binds BRD4 ligand (+)-JQ-1 to HSP90, and inhibits the proliferation of cancer cells. iHAC activates the anti-tumor immune response, inhibits the recurrence and metastasis of 4T1 breast cancer in mouse models .
|
-
- HY-124817
-
|
|
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-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-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-123303
-
|
NZ-28
|
HSP
|
Cancer
|
|
NSC-134754 is a dehydroemetine derivative and heat shock protein induction inhibitor. NSC-134754 acts at the post-transcriptional level, targets Hsp72 and Hsp27, and does not alter general protein synthesis, HSF-1 transcriptional activity, or Hsp mRNA levels. NSC-134754 shows no significant toxicity in preclinical models and sensitizes cancer cells to proteasome and Hsp90 inhibitors. NSC-134754 can be used for the research of multiple myeloma, prostate carcinoma, colon carcinoma .
|
-
- 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-178956
-
|
|
HSP
|
Cancer
|
|
KUNB106 is a selective Hsp90β inhibitor with KDs of 91 nM and 38 μM against Hsp90β and Hsp90α. KUNB106 exhibits antiproliferative activity against MDA-MB-231 cells, A549 and SKOV-3 cells. KUNB106 can be used for the study of triple negative breast cancer .
|
-
- 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-168566
-
|
|
HSP
|
Cancer
|
|
EV206 is a Hsp70 binder and apoptosis inducer that binds to the N-terminal domain of Hsp70, promotes Hsp70 degradation via the ubiquitin-proteasome system, and reduces Hsp70 protein stability. EV206 induces apoptotic cell death, inhibits colony formation, and downregulates the expression of cancer stem cell-related markers in non-small cell lung cancer cells. EV206 inhibits the growth of H460 xenograft tumors in nude mice and can be used for the research of non-small cell lung cancer .
|
-
- 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-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-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] sup >.
|
-
- HY-P11052
-
|
|
HSP
|
Cancer
|
|
A8 peptide is a Hsp72 antagonist. A8 peptide inhibits tumor progression and metastasis as well as enhances the cancer cells' sensitivity to apoptosis induced by chemotherapeutic agents (such as Cisplatin (HY-17394)) by blocking the Hsp72-TLR2 interaction and the subsequent activation of MDSCs. A8 peptide can be used for cancers research .
|
-
- HY-110042
-
|
|
HSP
Apoptosis
CDK
PERK
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
CCT018159 is an ATP-competitive HSP90β inhibitor, with an IC50 of 3.2 μM against human HSP90β ATPase and 6.6 μM against yeast HSP90β ATPase. CCT018159 induces cell cycle arrest and apoptosis in tumor cells, and inhibits invasion and angiogenesis. CCT018159 is applicable to cancer-related research .
|
-
- HY-124611
-
|
|
HSP
Apoptosis
|
Cancer
|
|
JG-231 is an allosteric inhibitor of heat shock protein 70 (Hsp70). JG - 231 inhibits the binding of Hsp70 and BAG family proteins, including inhibition of Hsp70 and BAG1 with a Ki of 0.11 μM. JG-231 inhibits proliferation of tumor cells and induces apoptosis. JG-231 has antitumor activity .
|
-
- HY-10389R
-
|
17-DMAG (Standard); KOS-1022 (Standard); NSC 707545 (Standard)
|
Reference Standards
HSP
|
Cancer
|
|
Alvespimycin (Standard) is the analytical standard of Alvespimycin (HY-10389). This product is intended for research and analytical applications. Alvespimycin (17-DMAG) is a potent inhibitor of Hsp90, binding to Hsp90 with an EC50 of 62 nM.
|
-
- HY-Q43097
-
|
|
HSP
STAT
|
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-174438
-
|
|
HSP
|
Metabolic Disease
|
|
PSEC13 is an activator of HSF-1/DAF-16 axis. PSEC13 can upregulate heat shock proteins. PSEC13 can form hydrogen bonds with key residues in the HSP-16.2 active site. PSEC13 can be used to enhance proteostasis and extend lifespan through the modulation of HSP-16.2. PSEC13 could promote the nuclear translocation of daf-16, upgrading the proportion of intermediate. PSEC13 can be studied in research for aging and age-related diseases .
|
-
- 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-P11053
-
|
|
HSP
|
Cancer
|
|
A17 peptide is a Hsp70-targeting peptide. A17 peptide binds to the ATP-binding domains of Hsp70. A17 peptide specifically inhibits the chaperone activity, thereby increasing the cells' sensitivity to apoptosis induced by chemotherapeutic agents, such as Cisplatin (HY-17394). A17 peptide can be used for anticancer chemotherapy research, such multiple myeloma .
|
-
- 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-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-RS18017
-
|
|
Small Interfering RNA (siRNA)
|
Others
|
|
Hsp90ab1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Hsp90ab1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
Hsp90ab1 Mouse Pre-designed siRNA Set A
Hsp90ab1 Mouse 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-RS27757
-
|
|
Small Interfering RNA (siRNA)
|
Others
|
|
Hsp90b1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Hsp90b1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
Hsp90b1 Rat Pre-designed siRNA Set A
Hsp90b1 Rat Pre-designed siRNA Set A
- 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-RS24490
-
|
|
Small Interfering RNA (siRNA)
|
Others
|
|
Hsp90ab1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Hsp90ab1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
Hsp90ab1 Rat Pre-designed siRNA Set A
Hsp90ab1 Rat Pre-designed siRNA Set A
- HY-RS21240
-
|
|
Small Interfering RNA (siRNA)
|
Others
|
|
Hsp90b1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Hsp90b1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
Hsp90b1 Mouse Pre-designed siRNA Set A
Hsp90b1 Mouse 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-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-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-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-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 (Ex/Em = 488/515 nm) .
|
-
- HY-13757AS
-
|
ICI 47699-d5; (Z)-Tamoxifen-d5; trans-Tamoxifen-d5
|
Isotope-Labeled Compounds
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 .
|
-
- HY-181626
-
|
|
HSP
Aurora Kinase
Apoptosis
|
Cancer
|
|
NN-01-195 is a HSP90 and AURKA inhibitor. NN-01-195 binds tightly to and inhibits AURKA and HSP90, with an IC50 of 3.1 nM against AURKA and an IC50 of 8.7 nM against HSP90α. NN-01-195 induces mitotic arrest and spindle abnormality in tumor cells, and triggers cell apoptosis. NN-01-195 can be used in the research of solid tumors .
|
-
- HY-13752
-
|
|
HSP
|
Cancer
|
|
STA-1474 is an orally active and highly selective HSP90 inhibitor. STA-1474 can trigger tumor cell apoptosis. STA-1474 demonstrates significant antitumor efficacy in spontaneous canine cancer models (e.g., osteosarcoma, thyroid carcinoma). STA-1474 is promising for research of solid tumors (e.g., osteosarcoma, breast cancer) and HSP90-driven cancers .
|
-
- 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-15986
-
|
CCT 129397
|
HSP
|
Cancer
|
|
VER-49009 is a Hsp90 inhibitor, with an IC50 of 25 nM and a Kd of 78 nM.
|
-
- 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-182809
-
|
|
Hsp-targeting Chimeras
Androgen Receptor
HSP
|
Neurological Disease
Cancer
|
|
Androgen receptor degrader-6 is a blood-brain barrier-permeable AR degrader. Androgen receptor degrader-6 inhibits the chaperone activity of HSP27 and disrupts the HSP27-AR complex. Androgen receptor degrader-6 promotes the degradation of wild-type and mutant AR, reduces AR protein levels, and inhibits the growth of glioblastoma cells. Androgen receptor degrader-6 can be used in glioblastoma research .
|
-
- 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-U00398
-
|
|
HSP
|
Cardiovascular Disease
|
|
Bimoclomol is a heat shock protein (HSP) coinducer, used for treatment of cardiovascular diseases.
|
-
- HY-B0779
-
-
- 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-148745
-
|
|
HSP
|
Cancer
|
|
JG-258 is an inactive negative control for Hsp70 inhibitors .
|
-
- HY-183633
-
|
|
HSP
|
Others
|
|
GR-25 is an orally active, selective Hsp90p inhibitor.
|
-
- HY-10940
-
-
- 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-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-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-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-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-10211R
-
|
17-AAG (Standard); NSC 330507 (Standard); CP 127374 (Standard)
|
Reference Standards
HSP
Autophagy
Mitophagy
Bacterial
Apoptosis
Antibiotic
|
Infection
Cancer
|
|
Tanespimycin (Standard) is the analytical standard of Tanespimycin. This product is intended for research and analytical applications. 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-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-181062
-
|
|
HSP
Apoptosis
Autophagy
ULK
RIP kinase
CDK
|
Cancer
|
|
VWK147 is a second-generation HSP90 C-terminal domain (CTD) inhibitor. VWK147 targets the CTD dimerization interface, prevents HSP90 CTD dimerization, disrupts co-chaperone PPID binding to HSP90 CTD, and inhibits HSP90 chaperone function dependent on dimerization. VWK147 reduces protein levels of HSP90 client proteins ULK1, RIPK1, and CDK4 without inducing a heat shock response. VWK147 induces cell death, including apoptosis, in Cisplatin (HY-17394)-sensitive and -resistant urothelial carcinoma cells. VWK147 induces LC3-II accumulation, inhibits autophagosome-lysosome fusion to block canonical autophagy, and induces non-canonical LC3 lipidation independent of ULK1 and PIK3C3 complexes. VWK147 can be used for the research of urothelial carcinoma .
|
-
- HY-173320
-
|
|
Hsp-targeting Chimeras
Wee1
HSP
|
Cancer
|
|
HEMTAC WEE1 degrader-1 is a HSP90-mediated targeting chimera (HEMTAC) degrader of WEE1 (HSP90 enzyme inhibitory activity is IC50: 16.76 nM). HEMTAC WEE1 degrader-1 promotes the ubiquitination and degradation of WEE1. HEMTAC WEE1 degrader-1 blocks the G2/M cell cycle. HEMTAC WEE1 degrader-1 has anticancer activity in acute myeloid leukemia (AML) patient-derived xenograft (PDX) models. HEMTAC WEE1 degrader-1 can be used in AML research. (Pink: HSP90 binder; Blue: WEE1 ligand; Black: linker) .
|
-
- 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 (HSP90)-mediated protein degrader (CHAMPs) .
|
-
- HY-117192
-
|
|
HSP
Fungal
|
Infection
|
|
NSC145366 monohydrochloride is a Hsp90 C-terminal inhibitor. NSC145366 monohydrochloride directly interacts with the C-terminus of Hsp90 and inhibits its chaperone activity. NSC145366 monohydrochloride strongly inhibits the growth of Saccharomyces cerevisiae cog7Δ and cog8Δ strains .
|
-
- 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-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-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-152184
-
|
SEW04784
|
HSP
|
Metabolic Disease
|
|
SEW84 is an inhibitor of Aha1-stimulated Hsp90 (ASH) ATPase activity. SEW84 inhibits Aha1-stimulated Hsp90 (ASH) activity with an IC50 value of 0.3 μM. SEW84 can be used in the study of protein deposition diseases .
|
-
- 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-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-163329
-
|
|
Biochemical Assay Reagents
|
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-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-169947
-
|
|
CDK
|
Cancer
|
|
DDO-6079 is a potent CDC37 inhibitor. DDO-6079 inhibits HSP90-CDC37 and CDC37-CDK4/6 chaperone complex by binding to an allosteric site on CDC37. DDO-6079 decreases the thermostability of CDK6 .
|
-
- HY-116279
-
-
- 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-171616
-
|
|
HSP
β-catenin
|
Cancer
|
|
DCEM1 binds to heat shock protein 60 (HSP60) and inhibits the interaction of HSP60 with ClpP, thereby blocking the mitochondrial unfolded protein response. DCEM1 inhibits β-catenin expression and ATP production in PC-3 and TKO cells. DCEM1 can be used in prostate cancer research .
|
-
- HY-N9722
-
|
|
HSP
|
Cancer
|
|
Dehydroherbarin is a selective inhibitor targeting HSP90α with blood-brain barrier penetration. Dehydroherbarin interferes with key pathways of tumor cell survival by binding to HSP90α, while exerting moderate antibacterial and anti-hepatitis A virus activities and inhibiting tumor cell migration. Dehydroherbarin can be used in research on tumors such as breast cancer .
|
-
- HY-106443A
-
|
BRX-220
|
HSP
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
Arimoclomol maleate (BRX-220) is an orally active 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 .Arimoclomol maleate can be used for the study of Niemann–Pick disease type C.
|
-
- 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-N7627
-
-
- HY-133571A
-
|
AHGDM hydrochloride
|
HSP
ADC Payload
|
Cancer
|
|
Aminohexylgeldanamycin (AHGDM) hydrochloride, a Geldanamycin derivative, is a potent HSP90 inhibitor. Aminohexylgeldanamycin hydrochloride shows antiangiogenic and antitumor activities .
|
-
- HY-133571
-
|
AHGDM
|
HSP
ADC Payload
|
Cancer
|
|
Aminohexylgeldanamycin (AHGDM), a Geldanamycin derivative, is a potent HSP90 inhibitor. Aminohexylgeldanamycin shows antiangiogenic and antitumor activities .
|
-
- HY-167731
-
|
|
HSP
|
Infection
|
|
Monorden diacetate serves as a promising lead compound in the development of novel fungicides due to its potential as an Hsp90 inhibitor.
|
-
- HY-127183
-
|
|
HSP
|
Infection
|
|
ML229 is an HSP90 inhibitor. ML229 can be used in the research of infectious diseases such as candidiasis .
|
-
- HY-N6249
-
-
- 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. SST0116CL1 can be used for the study of leukemia, gastric and ovarian carcinoma .
|
-
- 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-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-127179
-
|
|
HSP
|
Infection
|
|
ML189 is an HSP90 inhibitor. ML189 can be used in the research of infectious diseases such as candidiasis .
|
-
- HY-108248
-
-
- HY-106443B
-
|
BRX-220 citrate
|
HSP
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
Arimoclomol citrate (BRX-220 citrate) is an orally active 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 . Arimoclomol citrate can be used for the study of Niemann–Pick disease type C.
|
-
- 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-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-116683
-
116-9e
2 Publications Verification
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-13301
-
|
|
HSP
|
Cancer
|
|
MPC-3100 is an orally bioavailable, synthetic, second-generation small-molecule inhibitor of Hsp90 with potential antineoplastic activity .
|
-
- HY-10212
-
BIIB021
4 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-10211S
-
|
17-AAG-d5; NSC 330507-d5; CP 127374-d5
|
Isotope-Labeled Compounds
Apoptosis
Bacterial
Autophagy
HSP
Mitophagy
Antibiotic
|
Cancer
|
|
Tanespimycin-d5 (17-AAG-d5; NSC 330507-d5; CP 127374-d5) is the deuterium labeled Tanespimycin (HY-10211). 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-133570
-
|
|
HSP
ADC Payload
|
Cancer
|
|
17-AEP-GA, an HSP90 antagonist, is a potent inhibitor of glioblastoma cell proliferation, survival, migration and invasion. ADCs Toxin .
|
-
- HY-B1425
-
-
- 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-145722A
-
|
OGX-427
|
HSP
|
Cancer
|
|
Apatorsen is a 2'-methoxyethyl-modified antisense oligonucleotide and also a Hsp27 inhibitor. Apatorsen reduces Hsp27 mRNA and protein levels, impairs stress-induced cytoprotective functions, induces cell apoptosis, inhibits tumor growth and prevents metastasis. Apatorsen is applicable to research related to non-small cell lung cancer, castration-resistant prostate cancer, breast cancer, ovarian cancer and bladder cancer .
|
-
- 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-164399A
-
|
|
HSP
ERK
CDK
Akt
|
Cancer
|
|
SST0116CL1 free base is a HSP90 inhibitor (IC50: 0.21 μM). SST0116CL1 free base 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 free base induces degradation of Her2 in BT-474 cell (IC50: 0.2 μM). SST0116CL1 free base has antiproliferative activity and inhibits tumor growth. SST0116CL1 free base has antiproliferative activity and inhibits tumor growth. SST0116CL1 free base can be used for the study of leukemia, gastric and ovarian carcinoma .
|
-
- HY-161781
-
-
- HY-145722
-
|
OGX-427 sodium
|
HSP
|
Cancer
|
|
Apatorsen (OGX-427) sodium is a 2'-methoxyethyl-modified antisense oligonucleotide and also a Hsp27 inhibitor. Apatorsen sodium reduces Hsp27 mRNA and protein levels, impairs stress-induced cytoprotective functions, induces cell apoptosis, inhibits tumor growth and prevents metastasis. Apatorsen sodium is applicable to research related to non-small cell lung cancer, castration-resistant prostate cancer, breast cancer, ovarian cancer and bladder cancer .
|
-
- HY-119732
-
|
|
HSP
|
Neurological Disease
Cancer
|
|
KUNG94 is a selective Grp94/HSP90B inhibitor (IC50=8 nM). By inhibiting the chaperone function of Grp94, KUNG94 reduces the maturation and cell surface trafficking of its specific client proteins. KUNG94 can be used for studies on Grp94-related biological mechanisms, as well as diseases including cancer and primary open-angle glaucoma .
|
-
- 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
-
|
Geranylgeranylacetone (Standard)
|
Reference Standards
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-106443
-
|
BRX-220 free base
|
HSP
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
Arimoclomol (BRX-220 free base) is an orally active 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.Arimoclomol can be used for the study of Niemann–Pick disease type C. Arimoclomol can cross the blood-brain barrier and can be used in research on Niemann-Pick disease type C .
|
-
- HY-106443AR
-
|
BRX-220 (Standard)
|
Reference Standards
HSP
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
Arimoclomol maleate (Standard) is the analytical standard of Arimoclomol maleate (HY-106443A). This product is intended for research and analytical applications. Arimoclomol maleate (BRX-220) is an orally active 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 .Arimoclomol maleate can be used for the study of Niemann–Pick disease type C.
|
-
- 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-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-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-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-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-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-B0510CR
-
|
|
Reference Standards
Antifolate
Bacterial
Antibiotic
|
Infection
Cancer
|
|
Actein (Standard) is the analytical standard of Actein. This product is intended for research and analytical applications. Actein, a triterpene glycoside, shows an inhibitory effect on cancer cells, which is isolated from the rhizomes of Cimicifuga foetida. Actein suppresses cell proliferation, induces autophagy and apoptosis through promoting ROS/JNK activation, and blunting AKT pathway in bladder cancer. Actein has little toxicity in vivo .
|
-
- 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-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-10940R
-
|
PFTμ (Standard); 2-Phenylethynesulfonamide (Standard)
|
MDM-2/p53
HSP
Autophagy
Reference Standards
|
Neurological Disease
Cancer
|
|
Pifithrin-μ (Standard) is the analytical standard of Pifithrin-μ. This product is intended for research and analytical applications. Pifithrin-μ is an inhibitor of p53 and HSP70, with antitumor and neuroprotective activity.
|
-
- 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-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-162567
-
|
|
HSP
Beclin1
Autophagy
|
Cancer
|
|
AP-4-139B is a blood-brain barrier-permeable HSP70 inhibitor with a IC50 of 180 nM against hHSP70. AP-4-139B binds directly to HSP70 and inhibits its ATPase activity. AP-4-139B promotes Autophagy by increasing the phosphorylation of Beclin-1. AP-4-139B exerts antitumor effects in preclinical models of colorectal cancer and pancreatic ductal adenocarcinoma .
|
-
- HY-N14780
-
|
(+)-Pochonin D
|
HSP
Interleukin Related
Enterovirus
|
Infection
Inflammation/Immunology
Cancer
|
|
Pochonin D ((+)-Pochonin D) is an inhibitor of heat shock protein 90 (Hsp90) with antiviral and anti-inflammatory activities. Pochonin D inhibits Hsp90, affects the homeostasis, folding and assembly processes of viral proteins, and reduces the replication capacity of viruses. Pochonin D reduces the infiltration of inflammatory cells, decreases the secretion of inflammatory cytokines such as TNF-α and IL-1β, and alleviates inflammatory responses. Pochonin D is a promising candidate for research on human rhinovirus (HRV) infection and cancer .
|
-
- HY-B1817
-
|
|
Environmental Pollutants
Apoptosis
Biochemical Assay Reagents
HSP
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Zinc acetate acts as an immune response modulator. Zinc acetate enhances the expression of HSP-70 mRNA. Zinc acetate restores the proliferation and cytokine production capacities of splenocytes. Zinc acetate reduces the Apoptosis level of splenocytes in endotoxemic mice. Zinc acetate increases plasma zinc levels and improves survival rates in mice with LPS-induced lethal endotoxemia. Zinc acetate induces rapid death of prostate cancer cell lines in vitro. Zinc acetate inhibits the growth of prostate cancer xenografts in SCID mice. Zinc acetate can be used in endotoxemia research .
|
-
- 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-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-176407
-
-
- HY-130997
-
|
|
ADC Payload
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-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-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-15230
-
-
- 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-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-121706
-
|
|
HSP
|
Cancer
|
|
PU-20F (compound 59) is a Hsp90 inhibitor with an EC50 of 6.8 μM. PU-20F competes with Geldanamycin (HY-15230) for binding to Hsp90 and regulates the function of this molecular chaperone. PU-20F induces the degradation of oncogenic Her2 tyrosine kinase. PU-20F blocks the growth of breast cancer cells. PU-20F can be used in breast cancer-related research .
|
-
- 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-N1073
-
|
6-Isopentenylgenistein; Erythrinin B
|
Apoptosis
EGFR
HSP
ERK
Akt
|
Infection
Cancer
|
Wighteone (6-Isopentenylgenistein; Erythrinin B) is a prenylated isoflavone that acts as a HSP90/EGFR L858R/T790M inhibitor and antifungal agent. Wighteone reduces the expression level of HSP90, blocks EGF-induced phosphorylation of EGFR, and thereby inhibits the downstream ERK and AKT signaling pathways. Wighteone induces cell cycle redistribution, inhibits proliferation and triggers apoptosis in cancer cells. Wighteone can be isolated from Erythrina suberosa, and can also be induced to synthesize in Lotus japonicus under specific conditions. Wighteone can be used to study HER2-positive breast cancer, leukemia, non-small cell lung cancer with EGFR L858R/T790M mutation, and fungal infections .
|
-
- HY-175273
-
|
|
PROTACs
FLT3
HSP
ERK
STAT
Akt
Apoptosis
|
Cancer
|
|
MA191 is a FLT3 PROTAC degrader. MA191 abrogates FLT3 inhibitor resistance from rebound activation of mitogen-activated kinases. MA191 mediates rapid FLT3-ITD degradation through a mechanism requiring VHL, neddylation, and BIM. MA191 reduces FLT3-ITD levels before inducing apoptosis. MA191 halts AML cell proliferation in Danio rerio. MA191 can be used for the study of acute myeloid leukemia (AML) (Pink: FLT3 ligand: (HY-175311), Blue: E3 ligase CRBN Ligand (HY-112078), Black: Linker, E3 ligase ligand-linker conjugate (HY-175312)) .
|
-
- HY-W015445R
-
|
|
Reference Standards
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-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-P10635
-
|
|
Biochemical Assay Reagents
|
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 .
|
-
- HY-133961
-
|
Cholesteryl glucoside
|
HSP
|
Metabolic Disease
|
|
Cholesterol β-D-glucoside (Cholesteryl glucoside) is a heat shock transcription factor 1 (HSF1) activator. Cholesterol β-D-glucoside induces HSP70 in fibroblast cells .
|
-
- 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-13313
-
XL888
5 Publications Verification
|
HSP
Apoptosis
|
Cancer
|
|
XL888 is a potent and orally active HSP90 inhibitor with an IC50 value of 24 nM. XL888 shows anti-proliferation activity and induces Apoptosis. XL888 shows anti-tumor activity .
|
-
- 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
-
DN401
1 Publications Verification
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-170667
-
|
|
Autophagy
HSP
|
Cancer
|
|
Autophagy activator-1 (Compound B2) is an autophagy activator Autophagy. Activator-1 ultimately leads to the activation of autophagy by downregulating key members of the HSP70 family and activating the unfolded protein response .
|
-
- HY-B1425R
-
|
|
Reference Standards
HSP
Reactive Oxygen Species (ROS)
|
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-137441
-
|
PU-HZ151
|
HSP
|
Neurological Disease
Cancer
|
|
Icapamespib (PU-HZ151; PU-AD) is a selective, orally active inhibitor of Epichaperomes assembled by HSP90 with slow dissociation kinetics. Icapamespib can cross the blood-brain barrier (BBB) ??and induce epichaperome disassembly by non-covalently binding to HSP90, restoring the normal protein-protein interaction network. Icapamespib can specifically disrupt disease-related abnormal protein interaction networks, reduce neurotoxic protein aggregation and tumor cell survival signals. Icapamespib can be used in the research of neurodegenerative diseases such as Alzheimer's disease, as well as cancers such as glioblastoma and metastatic breast cancer .
|
-
- HY-137441A
-
|
PU-HZ151 hydrochloride
|
HSP
|
Neurological Disease
Cancer
|
|
Icapamespib (PU-HZ151; PU-AD) hydrochloride is a selective, orally active inhibitor of Epichaperomes assembled by HSP90 with slow dissociation kinetics. Icapamespib hydrochloride can cross the blood-brain barrier (BBB) ??and induce epichaperome disassembly by non-covalently binding to HSP90, restoring the normal protein-protein interaction network. Icapamespib hydrochloride can specifically disrupt disease-related abnormal protein interaction networks, reduce neurotoxic protein aggregation and tumor cell survival signals. Icapamespib hydrochloride can be used in the research of neurodegenerative diseases such as Alzheimer's disease, as well as cancers such as glioblastoma and metastatic breast cancer .
|
-
- 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-178496
-
|
|
Hsp-targeting Chimeras
PARP
HSP
|
Cancer
|
|
DDO3602 is a PARP1 HEMTAC degradation agent mediated by HSP90. DDO3602 has good anti-tumor activity and tumor selectivity. DDO3602 induces G2/M phase arrest, DNA damage, and inhibits cell migration by degrading PARP1 in MCF-7 cells (IC50 = 187 nM). DDO3602 can be used for research on cancer such as breast cancer. (Pink: PARP1 Ligand (HY-75706); Blue: HSP90 Ligand (HY-179203); Black: Linker (HY-W015300))
|
-
- HY-10212R
-
|
CNF2024 (Standard)
|
Reference Standards
HSP
Autophagy
|
Cancer
|
|
BIIB021 (Standard) is the analytical standard of BIIB021. This product is intended for research and analytical applications. 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-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-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-176951
-
|
|
Ligands for Target Protein for PROTAC
HSP
|
Cancer
|
|
Chaperone complex ligand 1 is a chaperone ligand for HSP90. Chaperone complex ligand 1 can be connected to the MET ligand (HY-50878) by a linker to synthesis of MET degrader OZD-MET 01 (HY-177893) .
|
-
- 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-164184
-
|
|
Apoptosis
Caspase
HSP
Early 2 Factor (E2F)
DNA/RNA Synthesis
|
Cancer
|
|
Ly101-4B is an apoptosis inducer and multi-target inhibitor with antiproliferative, antitumor and cycytotoxic effects. Ly101-4B reduces HSF1 expression, inhibits microRNA-214 synthesis, downregulates HSP27, HSP70 and HSP90 expression, while suppressing E2F-dependent transcriptional activity and downregulating its target genes. Ly101-4B induces caspase 3/7-mediated apoptosis by reducing DNA synthesis, inhibiting the cell cycle and G1/S phase transition, without affecting RNA synthesis or inducing necrosis. Ly101-4B is selective for pancreatic ductal adenocarcinoma cells with different genotypes and varying degrees of E2F dependence. Ly101-4B can be used in research related to epithelial ovarian cancer and pancreatic ductal adenocarcinoma .
|
-
- HY-147125
-
|
|
HSP
Akt
CDK
Raf
Apoptosis
|
Cancer
|
|
DDO-6600 is a covalent Hsp90 inhibitor. DDO-6600 disrupts the interaction between Hsp90 and its co-chaperone protein Cdc37, thereby inducing the degradation of kinase client proteins (such as AKT, CDK4, c-Raf). DDO-6600 has inhibitory activity against various cancer cells. DDO-6600 inhibits the migration and invasion of HCT-116 cells, and induces cell cycle arrest and apoptosis. DDO-6600 significantly inhibits tumor growth in the HCT-116 xenograft tumor model. DDO-6600 can be used for research on colorectal cancer .
|
-
- 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-P10757
-
-
- 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-13757
-
|
ICI 46474; (Z)-Tamoxifen Citrate; trans-Tamoxifen Citrate
|
Estrogen Receptor/ERR
HSP
Autophagy
Apoptosis
|
Infection
Neurological Disease
Inflammation/Immunology
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 can also be used to induce gene knockout in CreER transgenic mice .
|
-
- 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-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-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-15230R
-
-
- 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-18406
-
|
|
HSP
|
Cancer
|
|
YM-1 tosylate is a stable MKT-077 (HY-15096) analog and an orally active Hsp70 inhibitor. YM-1 tosylate induces cell death of HeLa cells and up-regulates the level of p53 and p21 proteins .
|
-
- HY-18399
-
YM-1
1 Publications Verification
|
HSP
NO Synthase
|
Cancer
|
|
YM-1 is a stable 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-182302
-
|
|
Drug Derivative
HSP
|
Cancer
|
|
SMTIN-P01 is a TRAP1 inhibitor that is selective for cytosolic Hsp90 and accumulates in mitochondria. SMTIN-P01 binds to the ATP-binding site of TRAP1 as an ATP mimic, thereby inhibiting ATPase and foldase activities. SMTIN-P01 induces mitochondrial membrane depolarization and proteolytic degradation in cancer cells. SMTIN-P01 exhibits significant cytotoxicity, but shows extremely low toxicity to primary mouse hepatocytes, and does not interfere with SIRT3-related functions or the levels of cytosolic Hsp90 substrates. SMTIN-P01 has important application value in cancer-related research .
|
-
- HY-13757AS1
-
|
ICI 47699-d3; (Z)-Tamoxifen-d3; trans-Tamoxifen-d3
|
Isotope-Labeled Compounds
Estrogen Receptor/ERR
Apoptosis
Autophagy
HSP
|
Cancer
|
|
Tamoxifen-d3 is the deuterium labeled Tamoxifen . 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-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-105063
-
|
|
HSP
|
Metabolic Disease
Inflammation/Immunology
|
|
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 .
|
-
- HY-124946
-
|
|
HDAC
Sirtuin
Apoptosis
|
Cancer
|
|
C1A is a class I/II HDACs and sirtuin inhibitor with an IC50 of 479 nM for HDAC6. C1A induces sustained acetylation of HDAC6 substrates, α-tubulin and HSP90. C1A shows srtong anticancer effcts, and induces apoptosis in cancer cells .
|
-
- HY-N15154
-
|
|
Cathepsin
HSP
|
Cancer
|
|
Tasiamide B is a Cathepsin D inhibitor, which is a linear peptide found in the marine cyanobacteria Symploca sp.. Tasiamide B is proved as a good template for the development of aspartic proteases inhibitors. Tasiamide B is effective against skin cancer by strongly interacting with the target protein HSP90 .
|
-
- HY-102007AR
-
|
|
Reference Standards
HSP
|
Cancer
|
|
Gamitrinib TPP hexafluorophosphate (Standard) is the analytical standard of Gamitrinib TPP hexafluorophosphate (HY-102007A). This product is intended for research and analytical applications. Gamitrinib TPP hexafluorophosphate is a Gamitrinib (GA) mitochondrial matrix inhibitor. Gamitrinib TPP hexafluorophosphate is a mitochondrial targeted HSP90 inhibitor with anti-cancer activity.
|
-
- 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 .
|
-
- HY-W778408
-
|
ICI 47699-13C6; (Z)-Tamoxifen-13C6; trans-Tamoxifen-13C6
|
Isotope-Labeled Compounds
Apoptosis
Autophagy
HSP
Estrogen Receptor/ERR
|
Endocrinology
|
|
Tamoxifen- 13C6 (ICI 47699- 13C6) is the 13C-labeled Tamoxifen (HY-13757A). 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 transgenic mouse .
|
-
- HY-N2468R
-
|
1,4-β-D-Xylobiose (Standard); 1,4-D-Xylobiose (Standard)
|
Reference Standards
TNF Receptor
Claudin
HSP
|
Metabolic Disease
Inflammation/Immunology
|
|
Xylobiose (1,4-β-D-Xylobiose; 1,4-D-Xylobiose) is an orally active Claudin 2/CLDN2 inhibitor and HSP27 inducer. Xylobiose works by regulating intestinal barrier function and glucose and lipid metabolism-related signaling pathways. Xylobiose inhibits CLDN2 expression to reduce intestinal permeability, induces HSP27 to enhance cell protection, and regulates the miR-122a/miR-33a axis to inhibit liver lipid synthesis and improve insulin resistance. Xylobiose can strengthen intestinal barrier integrity, reduce blood sugar and blood lipid levels, and reduce oxidative stress and inflammatory response. Xylobiose can be used in the study of type 2 diabetes and metabolic syndrome .
|
-
- HY-P10371
-
|
txCD47
|
Reactive Oxygen Species (ROS)
Thrombopoietin Receptor
Mitochondrial Metabolism
HSP
HSV
CD47
|
Infection
Inflammation/Immunology
Cancer
|
|
PKHB1 (txCD47) is a CD47 agonist and Thrombospondin-1 peptide mimetic. PKHB1 activates CD47 and triggers Caspase-independent, calcium-dependent cell death via mitochondrial alterations, ROS production, endoplasmic reticulum morphological changes, and dissipation of mitochondrial membrane potential. PKHB1 induces the exposure of Calreticulin, HSP70, and HSP90, thereby driving immunogenic cell death. PKHB1 promotes intratumoral CD8 + T cell infiltration and inhibits breast tumorigenesis. PKHB1 reduces HSV-1 levels and alleviates the severity of herpes simplex keratitis. PKHB1 can be used in research related to breast cancer, herpes simplex keratitis, and T-cell acute lymphoblastic leukemia .
|
-
- HY-13757AR
-
|
ICI 47699(Standard); (Z)-Tamoxifen(Standard); trans-Tamoxifen (Standard)
|
Reference Standards
Estrogen Receptor/ERR
HSP
Autophagy
Apoptosis
|
Endocrinology
Cancer
|
|
Tamoxifen (Standard) is the analytical standard of Tamoxifen (HY-13757A). 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-N2468
-
|
1,4-β-D-Xylobiose; 1,4-D-Xylobiose
|
TNF Receptor
Claudin
HSP
|
Metabolic Disease
Inflammation/Immunology
|
|
Xylobiose (1,4-β-D-Xylobiose; 1,4-D-Xylobiose) is an orally active Claudin 2/CLDN2 inhibitor and HSP27 inducer. Xylobiose works by regulating intestinal barrier function and glucose and lipid metabolism-related signaling pathways. Xylobiose inhibits CLDN2 expression to reduce intestinal permeability, induces HSP27 to enhance cell protection, and regulates the miR-122a/miR-33a axis to inhibit liver lipid synthesis and improve insulin resistance. Xylobiose can strengthen intestinal barrier integrity, reduce blood sugar and blood lipid levels, and reduce oxidative stress and inflammatory response. Xylobiose can be used in the study of type 2 diabetes and metabolic syndrome .
|
-
- 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-W013675
-
|
|
HSP
|
Inflammation/Immunology
|
|
2-Methoxyhydroquinone is a phenolic compound that reduces TNF-α-induced production of chemokine (C-C motif) ligand 2 (CCL2) with an IC50 value of 64.3 µM. 2-Methoxyhydroquinone is also a precursor in the synthesis of the Hsp90 inhibitor Geldanamycin (HY-15230) .
|
-
- 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-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-179211
-
|
|
HSP
MHC
|
Cancer
|
|
CliMB-325 is an HSP90 inhibitor that can induce MHC-I (EC50 = 498 nM) expression on the surface of CT26 murine colorectal cancer cells. CliMB-325 enhances T cell activation and exhibits lower toxicity. CliMB-325 can be used for the study of colorectal cancer .
|
-
- 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-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-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-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-B1434R
-
|
7-ACA (Standard)
|
Beta-lactamase
Reference Standards
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
-
|
ICI 46474 (Standard); (Z)-Tamoxifen Citrate (Standard); trans-Tamoxifen Citrate (Standard)
|
Reference Standards
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-13757A
-
|
ICI 47699; (Z)-Tamoxifen; trans-Tamoxifen
|
Estrogen Receptor/ERR
HSP
Autophagy
Apoptosis
|
Infection
Neurological Disease
Metabolic Disease
Inflammation/Immunology
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 can also be dissolved in corn oil (HY-Y1888) for use in inducing gene knockout in CreER transgenic mice. Tamoxifen has better solubility in corn oil compared to Tamoxifen Citrate (HY-13757) .
|
-
- 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-176538
-
|
|
HSP
|
Cancer
|
|
Antiproliferative agent-72 (Compound 10) is a Hsp90 inhibitor with a Kd of 11 nM. Antiproliferative agent-72 has antiproliferative activity with IC50s of 1.5 μM and 1.1 μM for HCT116 and NCI-N87 cells, respectively. Antiproliferative agent-72 can be used for cancers research .
|
-
- HY-101026R
-
|
|
HSP
Reference Standards
|
Cancer
|
|
CCT251236 (Standard) is the analytical standard of CCT251236 (HY-101026). This product is intended for research and analytical applications. 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-125037
-
|
|
Estrogen Receptor/ERR
HSP
|
Cancer
|
|
Diptoindonesin G is a 2-arylbenzofuran derivative and a modulator of estrogen receptor and HSP90 middle domain. Diptoindonesin G exhibits strong cytotoxicity against mouse leukemia P-388 cells with an IC50 of 13.2 μM. Diptoindonesin G has antitumor activity and can be used in the research of tumors such as breast cancer .
|
-
- HY-109113
-
|
GPX-150
|
Topoisomerase
|
Cancer
|
|
Camsirubicin (GPX-150) is a non-cardiotoxic Doxorubicin (HY-15142) analog that selectively targets topoisomerase IIβ. Camsirubicin reduces cell viability and clone formation of MDA-MB-468 breast cancer cells. Camsirubicin increases the exposure of CALR and HSP90 on the cell surface. Camsirubicin can be used for the study of breast cancer .
|
-
- HY-101712R
-
|
|
Reference Standards
HSP
|
Neurological Disease
|
|
TRC051384 (Standard) is the analytical standard of TRC051384 (HY-101712). This product is intended for research and analytical applications. 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-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-N12717
-
|
|
PAK
FASTK
HSP
p38 MAPK
NF-κB
NO Synthase
COX
HSV
Caspase
TNF Receptor
Fungal
Apoptosis
|
Infection
Inflammation/Immunology
Cancer
|
|
Casuarinin is an orally active antiproliferative, anti-inflammatory, antifungal, virucidal and gastroprotective agent. Casuarinin upregulates the expression of p21/WAF1, Fas/APO‑1, mFasL, sFasL and HSP‑70, arrests cell cycle, induces apoptosis and inhibits cancer cell proliferation. Casuarinin inhibits TNF‑α-induced phosphorylation of MAPK and activation of NF‑κB, downregulates the expression of iNOS, NF‑κB, COX‑2 and ICAM‑1, and reduces the production of proinflammatory mediators. Casuarinin attenuates ethanol-induced activation of caspase‑3 and elevation of TNF‑α, inhibits the growth of Candida albicans, and inhibits HSV‑2. Casuarinin can be used in research related to mammary adenocarcinoma, inflammatory skin diseases, gastric ulcers, candidiasis and herpes simplex virus infections .
|
-
- HY-131831A
-
|
N6-benzyl ADP sodium
|
ATP Synthase
|
Cancer
|
|
6-Bn-ADP (N6-benzyl ADP) sodium is a derivative of Adenosine 5'-diphosphate (ADP) (HY-W010918) that inhibits ATP hydrolysis. 6-Bn-ADP sodium inhibits the ATPase activities of Mortalin, Hsc70, and Hsp70 protein with Kis of 86.51 μM, 294.5 μM, and 1612 μM, respectively .
|
-
- 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-176404
-
|
|
HSP
|
Cancer
|
|
DDO-6691 is a heat shock protein 90 (HSP90) inhibitor. DDO-6691 has antiproliferative effects on a variety of tumor cells, with HCT-116 colon cancer cells being the most sensitive (IC50: 1.08 μM). DDO-6691 exhibits potent tumor growth inhibition in the HCT-116 xenograft mouse model .
|
-
- HY-179056
-
|
|
PROTACs
PSMA
Androgen Receptor
HSP
Apoptosis
|
Cancer
|
|
Psa-AR is a PROTAC degrader targeting PSMA, with a Kd of 7.2 nM. Psa-AR exhibits strong degradation capabilities for AR, AR-V7, and HSP90, and induces cell apoptosis. Psa-AR demonstrates potent tumor suppressive activity in the 22Rv1 xenograft tumor model. Psa-AR can be used in the research of castration-resistant prostate cancer .
|
-
- HY-B0510R
-
|
|
Reference Standards
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-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-B0425R
-
|
Albamycin (Standard); Cathomycin (Standard)
|
Antibiotic
DNA/RNA Synthesis
HSP
Apoptosis
Bacterial
Orthopoxvirus
Reference Standards
|
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 .
|
-
- HY-19090
-
|
|
NO Synthase
HSP
|
Cardiovascular Disease
Inflammation/Immunology
|
|
FK 409 is a NO donor that can penetrate cell membranes. FK 409 has a vasodilatory effect on bovine retinal arteries. FK 409 alleviates acute-phase inflammation, induces HSP, and mitigates liver transplantation injury in a rat model of orthotopic liver transplantation. FK 409 can be used in research on cardiovascular diseases and liver transplant rejection and inflammatory immune system disorders .
|
-
- 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-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-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-19796R
-
|
Aramchol (Standard); C20-FABAC (Standard)
|
Reference Standards
Stearoyl-CoA Desaturase (SCD)
|
Metabolic Disease
|
|
Cucurbitacin D (Standard) is the analytical standard of Cucurbitacin D. This product is intended for research and analytical applications. 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-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-N1986R
-
|
|
Reference Standards
HSP
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Cucurbitacin D (Standard) is the analytical standard of Cucurbitacin D. This product is intended for research and analytical applications. 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-182596
-
|
|
MAPKAPK2 (MK2)
|
Inflammation/Immunology
Cancer
|
|
INHIB1X is a tetracyclic MAPKAP-K2 (MK2) inhibitor with an IC50 of 0.02 μM. INHIB1X inhibits LPS-induced TNFα release in human peripheral blood mononuclear cells (hPBMCs). INHIB1X suppresses the phosphorylation of hsp27 in Anisomycin-stimulated THP-1 cells. INHIB1X can be used for the research of inflammatory and tumor diseases .
|
-
- HY-15205R
-
|
STA-9090 (Standard)
|
HSP
Apoptosis
Reference Standards
|
Cancer
|
|
Ganetespib (Standard) is the analytical standard of Ganetespib. This product is intended for research and analytical applications. 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-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-17504BS1
-
|
|
HMG-CoA Reductase (HMGCR)
Autophagy
|
Cardiovascular Disease
Metabolic Disease
|
|
Rosuvastatin-d6 sodium is deuterium 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-117051
-
|
|
HSP
|
Cancer
|
|
STA-2842 is an inhibitor of heat shock protein HSP90 with potential to inhibit autosomal dominant polycystic kidney disease (ADPKD). ADPKD is caused by inherited mutations in the PKD1 or PKD2 genes that abnormally activate multiple signaling proteins and pathways that regulate cell proliferation. STA-2842 can significantly reduce initial renal cyst formation and kidney growth in mice, and slow disease progression in mice with existing cysts.
|
-
- HY-120923
-
|
|
HSP
NF-κB
HIV
Apoptosis
Caspase
|
Infection
Cancer
|
|
GUT-70, a tricyclic coumarin, is a Hsp90 inhibitor. GUT-70 activates the caspase 2, 3, 8 and 9, and induces the apoptosis in leukemic cells. GUT-70 inhibits HIV-1 replication in chronically infected cells via suppression of the NF-κB pathway. GUT-70 can be used for the study of leukemic, mantle cell lymphoma (MCL) and HIV-1 infection .
|
-
- HY-111007
-
|
|
HSP
|
Cancer
|
|
CH5015765 is an orally available Hsp90 inhibitor bound to the N-terminal ATP binding site, with a dissociation constant of 3.4 nM, CH5015765 exerts antiproliferative activity against human cancer cell lines, with IC50 values of 0.46 μM for HCT116 colorectal cancer cells and 0.57 μM for NCI-N87 gastric cancer cells. CH5015765 can be used for the study of cancer .
|
-
- HY-Z15805
-
|
|
Drug Isomer
HSP
TrxR
|
Cancer
|
|
Teprenone Impurity 5 (5Z-GGA) is the cis-isomer of Teprenone (HY-B0779). Teprenone Impurity 5 has inhibitory activity on the proliferation of human ovarian cancer cells Caov-3, and can block the invasion process of cancer cells. Teprenone Impurity 5 can induce the expression of heat shock protein 70 (HSP70) and thioredoxin (Trx). Teprenone Impurity 5 can be used for the research of ovarian cancer .
|
-
- HY-17504BR
-
|
ZD 4522 Sodium (Standard); X-Plended Sodium (Standard); Crestor Sodium (Standard)
|
HMG-CoA Reductase (HMGCR)
Potassium Channel
Autophagy
Bacterial
Reference Standards
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
Rosuvastatin (Sodium) (Standard) is the analytical standard of Rosuvastatin (Sodium). This product is intended for research and analytical applications. 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-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-17504R
-
|
Rosuvastatin hemicalcium (Standard); ZD 4522 Calcium (Standard)
|
Reference Standards
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-N15449
-
|
|
HSP
Caspase
Apoptosis
Reactive Oxygen Species (ROS)
Bcl-2 Family
|
Cancer
|
|
Vicanicin is a depsidone compound found in lichens. Vicanicin inhibits the expression of Hsp70, regulates the redox-sensitive mechanisms within cells, promotes the increase of reactive oxygen species (ROS) in cancer cells, changes the Bax/Bcl-2 ratio, activates caspase-3, and triggers apoptosis. Vicanicin inhibits cell growth and induces apoptosis in androgen-sensitive (LNCaP) and androgen-insensitive (DU-145) human prostate cancer cells. Vicanicin is promising for research of prostate cancer .
|
-
- HY-13425R
-
|
(-)-Deguelin (Standard); (-)-cis-Deguelin (Standard)
|
Akt
Autophagy
Apoptosis
Reference Standards
|
Cancer
|
|
Deguelin (Standard) is the analytical standard of Deguelin. This product is intended for research and analytical applications. 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-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-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-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-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-14463
-
|
AT13387
|
HSP
|
Cancer
|
|
Onalespib (AT13387) is a potent and cross the blood-brain barrier heat-shock-protein-90 (Hsp90) inhibitor. Onalespib inhibits the proliferation, survival and migration. Onalespib decreases the expression of EGFR, p-EGFR, AKT, P-AKT, ERK1/2, P-ERK1/2, S6, P-S6 protein. Onalespib shows antitumor activity. Onalespib has the potential for the research of non-small cell lung cancer (NSCLC) .
|
-
- 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-13468
-
KW-2478
4 Publications Verification
|
HSP
Apoptosis
Bcr-Abl
p38 MAPK
CDK
STAT
|
Cancer
|
|
KW-2478 is an HSP90 inhibitor (IC50 = 3.8 nM). KW-2478 inhibits the growth and induces apoptosis in chronic myeloid leukemia (CML) cells and liver cancer cells. KW-2478 weakens the BCR/ABL and MAPK signaling pathways, leading to increased p27 and p21 expression and decreased cyclin B1 expression. KW-2478 downregulates STAT3 expression. KW-2478 may be used in research on cancers such as CML and liver cancer .
|
-
- 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-168577
-
|
|
Ras
EGFR
|
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-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-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-N0576
-
-
- HY-N10379
-
|
|
Akt
mTOR
Apoptosis
Reactive Oxygen Species (ROS)
CDK
Ras
HSP
VEGFR
TNF Receptor
Interleukin Related
|
Inflammation/Immunology
|
|
19-epi-Scholaricine is an orally active indole alkaloid. 19-epi-Scholaricine downregulates the expression of profibrotic/apoptotic proteins (HRAS, HSP90AA1, KDR) and upregulates the expression of cell cycle-related protein (CDK2). 19-epi-Scholaricine suppresses ROS production and reduces the release of inflammatory mediators, thereby attenuating podocyte apoptosis, renal inflammation and oxidative stress by inhibiting AKT/mTOR. 19-epi-Scholaricine can be used in the research of chronic glomerulonephritis and membranous nephropathy .
|
-
- HY-13468A
-
|
|
HSP
Apoptosis
Bcr-Abl
p38 MAPK
CDK
STAT
|
Cancer
|
|
KW-2478 hydrochloride is an HSP90 inhibitor (IC50 = 3.8 nM). KW-2478 hydrochloride inhibits the growth and induces apoptosis in chronic myeloid leukemia (CML) cells and liver cancer cells. KW-2478 hydrochloride weakens the BCR/ABL and MAPK signaling pathways, leading to increased p27 and p21 expression and decreased cyclin B1 expression. KW-2478 hydrochloride downregulates STAT3 expression. KW-2478 hydrochloride may be used in research on cancers such as CML and liver cancer .
|
-
- HY-W010649
-
|
|
HSP
Epigenetic Reader Domain
ATP-binding cassette (ABC) transporters
Bacterial
Fungal
Antibiotic
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Isoxazole is a member of the five-membered heterocycle drug scaffold. Isoxazole has been used as a BET bromodomain inhibitor and can improve β-cell function in a diabetic mouse model. Isoxazole and its derivatives exhibit broad biological activities (such as antimicrobial, antibacterial, antifungal, antiviral, anticancer, anti-inflammatory, immunomodulatory, analgesic, anti-tuberculosis, and anti-diabetic effects). For example, the bicyclic Isoxazole can act as an HSP90 inhibitor, and the tricyclic Isoxazole is promising as a selective multidrug resistance protein (MRP1) inhibitor .
|
-
- 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-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-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-121744
-
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PDHK
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Inflammation/Immunology
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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
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- HY-180195
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HSP
Integrin
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Neurological Disease
Cancer
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Grp94-IN-3 (Compound 47) is a selective ATP competitive inhibitor of Grp94, with a Kd value of 76 nM. Grp94-IN-3 has a much lower affinity for Hsp90α, with a Kd value of 9.17 μM. Grp94-IN-3 induces the degradation of integrin α2 (Integrin α2) in MDA-MB-231 cells and reduces the intracellular accumulation of mutant cardiac proteins in human trabecular meshwork cells. Grp94-IN-3 can be used for the study of metastatic cancer and open-angle glaucoma .
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- HY-17504AS1
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ZD 4522-d6
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Isotope-Labeled Compounds
Autophagy
Bacterial
HMG-CoA Reductase (HMGCR)
Potassium Channel
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Cardiovascular Disease
Metabolic Disease
Cancer
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Rosuvastatin-d6 (ZD 4522-d6) is deuterium labeled Rosuvastatin. 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 .
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- HY-182399
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Aminoacyl-tRNA Synthetase
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Cancer
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BC-DXI-495 is a AIMP2-DX2 inhibitor. BC-DXI-495 disrupts the interaction of HSP70 and destabilizes DX2. BC-DXI-495 induces DX2 degradation via Siah1-mediated ubiquitination. BC-DXI-495 exerts tumor suppressive activity in cancer cells. BC-DXI-495 serves as a chemical probe to elucidate the mechanism of action of arylsulfonamide-based DX2 inhibitors. BC-DXI-495 can be used in lung cancer research .
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- HY-N6606
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Glycosidase
Tyrosinase
Heme Oxygenase (HO)
HSP
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Metabolic Disease
Inflammation/Immunology
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Delphinidin-3-O-galactoside chloride is an anthocyanin found in abbiteye blueberry. Delphinidin-3-O-galactoside chloride show inhibitory activitiesagainst α-glucosidase with an IC50 of 68.33 μM, and tyrosinase with an IC50 of 34.14 μM. Delphinidin-3-O-galactoside chloride attenuates HO-1 and HSP70 messenger RNA down-regulation, suppresses cytotoxicity, reduces endoplasmic reticulum stress responses, scavenges free radicals, reduces intracellular triglyceride levels and lipid droplet accumulation. Delphinidin-3-O-galactoside chloride can be used for the researches of diabesity, melanoma and inflammation .
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- HY-W470101
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Hsp-targeting Chimeras
HIF/HIF Prolyl-Hydroxylase
Apoptosis
HSP
Caspase
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Cancer
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HIF-2α-IN-17 is a selective hypoxia-inducible factor 2α (HIF2α) inhibitor that binds to the PAS-B domain of HIF2α. HIF-2α-IN-17 disrupts the interaction between HIF2α and the molecular chaperone Hsp70, leading to proteasomal degradation of HIF2α. HIF-2α-IN-17 exhibits antitumor activity and induces apoptosis in cancer cells. HIF-2α-IN-17 is applicable for research on cancers such as clear cell renal cell carcinoma .
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- HY-111165
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HSP
NF-κB
ERK
JNK
PDGFR
c-Myc
DNA/RNA Synthesis
Apoptosis
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Inflammation/Immunology
Cancer
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SNX-7081 is an Hsp90 inhibitor with Ki and IC50 values of 26 nM and 44 nM, respectively. SNX-7081 blocks the nuclear translocation of NF-κB, inhibits the production of pro-inflammatory cytokines, attenuates the ERK/JNK and PDGF signaling pathways, and suppresses LPS (HY-D1056)-induced nitric oxide production. SNX-7081 inhibits DNA repair, induces G2/M cell cycle arrest, and triggers apoptosis via downregulation of MYC/nucleolin and activation of Fas. SNX-7081 can be used in research related to rheumatoid arthritis and cancer .
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- HY-N1934
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Potassium Channel
HSP
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Cardiovascular Disease
Inflammation/Immunology
Cancer
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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 .
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- HY-158976
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Lactated ringer's solution (LRS)
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Biochemical Assay Reagents
Collagen
HSP
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Inflammation/Immunology
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Sodium lactate ringer's solution (Lactated ringer's solution (LRS)) is an isotonic crystal intravenous injection and arthroscopic irrigation solution containing racemic sodium lactate and electrolytes such as sodium, potassium, calcium and chloride (130 mEq sodium/L, 274 mOsm/L), which can be used as a cell integrity protectant. Sodium lactate ringer's solution maintains the integrity of human meniscus cells, ensures that they retain normal cell morphology, membrane regularity, size and density, and does not alter the mRNA expression levels of α1 (I) procollagen, α1 (II) procollagen, aggrecan or HSP70. Sodium lactate ringer's solution can be applied to studies related to extracellular fluid deficiency and meniscus tears .
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- HY-120825
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Apoptosis
DNA/RNA Synthesis
Reactive Oxygen Species (ROS)
Keap1-Nrf2
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Cancer
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QD 232 is a quinazolinedione-based ROS inducer and an apoptosis inducer with cytotoxicity and redox regulatory activity. QD 232 promotes ROS accumulation, activates the NRF2-mediated oxidative stress response and unfolded protein response pathways, and upregulates downstream antioxidant and stress response genes. QD 232 inhibits mtDNA transcription driven by HSP2 and LSP promoters, and impairs mitochondrial oxidative phosphorylation function. QD 232 induces apoptosis of pancreatic ductal adenocarcinoma cells and exerts cytotoxicity against gemcitabine (HY-17026)-resistant pancreatic ductal adenocarcinoma cells. QD 232 delays tumor growth in a mouse pancreatic cancer xenograft model .
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- HY-N0754
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YAP
HSP
Reactive Oxygen Species (ROS)
ERK
Autophagy
Apoptosis
Tyrosinase
DNA/RNA Synthesis
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Neurological Disease
Inflammation/Immunology
Cancer
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Eupalinolide A is a Yes-associated protein (YAP) degrader and HSP70 inducer. Eupalinolide A inhibits osteogenic differentiation of tendon-derived stem cells (TDSCs). Eupalinolide A induces autophagy in hepatocellular carcinoma cells via activating the ROS/ERK signaling pathway. Eupalinolide A protects PAM212 cells from UVB-, Menadione (HY-B0332)-, or heat shock-induced apoptosis. Eupalinolide A alleviates trauma-induced heterotopic ossification (HO) of Achilles tendon and inhibits growth of MHCC97-L and HCCLM3 hepatocellular carcinoma xenograft tumors in mice. Eupalinolide A can be used for the study of traumatic heterotopic ossification of tendons and hepatocellular carcinoma .
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- HY-W143216
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Monomethylthionine
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Amyloid-β
Tau Protein
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Neurological Disease
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Azure C acts as a tau oligomer modulator and Aβ42 oligomerization inhibitor. It regulates hsp70 ATPase activity, thereby mediating the clearance of tau protein. Azure C reduces the levels of toxic tau oligomers by promoting the formation of non-toxic tau aggregates, rescues neuroblastoma cells from tau oligomer-induced toxicity, and binds to and inhibits Aβ42 oligomerization without suppressing its fibrillization. Azure C is generated via sequential oxidation of methylene blue or Azure B through a horseradish peroxidase-mediated reaction, and accumulates in HRP reaction media. Azure C can be used in studies related to tauopathies, including Alzheimer's disease .
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- HY-10256
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Adezmapimod
Maximum Cited Publications
601 Publications Verification
SB 203580; RWJ 64809
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Organoid
p38 MAPK
Autophagy
Mitophagy
HSP
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Inflammation/Immunology
Cancer
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Adezmapimod (SB 203580) is a selective and ATP-competitive p38 MAPK inhibitor with IC50s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. Adezmapimod inhibits LCK, GSK3β and PKBα with IC50s of 100-500-fold higher than that for SAPK2a/p38. Adezmapimod can inhibit p38 MAPK and lead to the inhibition of downstream HSP27 phosphorylation. Adezmapimod does not disrupt JNK activity and is an autophagy and mitophagy activator .
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- HY-178955
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EGFR
HSP
PI3K
Caspase
Apoptosis
CDK
ERK
Akt
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Cancer
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EGFR-IN-182 (Compound 4) is an EGFR inhibitor with an IC50 value of 199 nM. EGFR-IN-182 inhibits HSP90 and PI3K, with IC50 values of 5.007 and 13.596 μM respectively. EGFR-IN-182 exhibits strong anti-proliferative activity against MCF-7 and MDA-MB-231 cells. EGFR-IN-182 downregulates Cyclin D1, inducing cell cycle arrest; it enhances the activity of caspase-9, inducing cell apoptosis. EGFR-IN-182 downregulates the expressions of ERK and AKT. EGFR-IN-182 can be used for research on breast cancer .
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- HY-N0576R
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Reference Standards
Endogenous Metabolite
Heme Oxygenase (HO)
HSP
p38 MAPK
Akt
Apoptosis
Caspase
PARP
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Neurological Disease
Metabolic Disease
Inflammation/Immunology
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Solanesol (Standard) is the analytical standard of Solanesol (HY-N0576). This product is intended for research and analytical applications. Solanesol is an orally active aliphatic terpene alcohol. Solanesol is mainly found in tobacco and other Solanaceae plants. Solanesol induces HO-1 and Hsp70 expression, activates p38 and Akt signaling pathways, and inhibits Apoptosis (reduces caspase-3 and PARP cleavage). Solanesol has antioxidant, anti-inflammatory, and neuroprotective activities. Solanesol can be used in the research of Huntington's disease, alcoholic liver disease, chronic inflammatory pain, anxiety, Alzheimer's disease, and bipolar disorder .
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- HY-124792
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HDAC
Apoptosis
Bcr-Abl
HSP
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Cancer
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MRLB-223 is a preferential HDAC1 and HDAC2 inhibitor with activity against tumor cells.MRLB-223 induces histone hyperacetylation, intrinsic apoptotic pathway activation, tumor cell apoptosis, Hsp90 hyperacetylation, and caspase-dependent Bcr-Abl degradation.MRLB-223 mediates p53-independent tumor cell death, with activity suppressed by Bcl-2 overexpression, and kills Bcr-Abl-expressing myeloid cells.MRLB-223 exerts effects in mice bearing Eμ-myc lymphomas.MRLB-223 can be used for the research of Eμ-myc lymphoma .
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- HY-118783
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(±)-2-Hexyl-4-pentynoic acid
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HDAC
HSP
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Neurological Disease
Cancer
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2-Hexyl-4-pentynoic acid ((±)-2-Hexyl-4-pentynoic acid), a Valproic acid (HY-10585) derivative, exhibits potential roles of HDAC inhibition (IC50 = 13 μM) and HSP70 induction. 2-Hexyl-4-pentynoic acid causes histone hyperacetylation and protect against glutamate-induced excitotoxicity in cultured neurons. 2-Hexyl-4-pentynoic acid can be used for the study of breast carcinoma. 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 .
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- HY-161826
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Wnt
β-catenin
HSP
CDK
c-Myc
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Cancer
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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 .
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- HY-179457
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PI3K
mTOR
Akt
HSP
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Cancer
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CC-11 is an orally active small molecule drug conjugate (SMDC) that links the PI3K/mTOR inhibitor with the extracellular heat shock protein 90 (EHSP90) targeting ligand through a cleavable linker. CC-11 exhibits strong HSP90 binding activity (IC50 = 15 nM) and inhibits PI3Kα kinase activity (IC50 = 0.54 nM). CC-11 has anti-proliferative activity against colon cancer cells. CC-11 shows significant efficacy in the HCT-116 xenograft tumor model. CC-11 can be used for research on colon cancer .
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- HY-10212A
-
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CNF2024 mesylate
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HSP
β-catenin
c-Myc
Autophagy
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Cancer
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BIIB021 (CNF2024) mesylate is the mesylate of BIIB021 (HY-10212). BIIB021 is an orally active Hsp90 inhibitor. BIIB021 inhibits the proliferation of chronic myeloid leukemia (CML) cells, with IC50 values of K562, K562/G, 32Dp210, and 32Dp210-T315I cells are 513.99, 603.53, 110.08, and 148.07 nM, respectively. BIIB021 degrades BCR-ABL protein and inhibits the β-catenin/c-Myc pathway. BIIB021 can also induce autophagy in CML cells. BIIB021 can be used for the research of CML .
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- HY-168376
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9(10)-Nitrated oleic acid
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PPAR
ERK
Akt
NO Synthase
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Metabolic Disease
Inflammation/Immunology
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9 (10)-Nitrooleate (9(10)-Nitrated oleic acid) is an endogenous lipid signaling mediator with vasoprotective effects. 9 (10)-Nitrooleate enhances enzymatic activity and improves nitric oxide bioavailability by inducing phosphorylation of Akt and ERK1/2, regulating the multi-site phosphorylation status of eNOS and optimizing its interaction with Hsp90. 9 (10)-Nitrooleate also activates PPARα, PPARδ and PPARγ receptors, thereby regulating adipogenesis, glucose uptake and inflammation-related gene expression, and exhibits immunosuppressive effects by inhibiting neutrophil migration and cytokine secretion. 9 (10)-Nitrooleate is widely used in studies of sepsis and related inflammatory diseases .
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- HY-156566
-
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PROTACs
Epigenetic Reader Domain
HSP
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Cancer
|
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PROTAC BRD4 Degrader-21 is a BRD4-targeting PROTAC degrader with an IC50 value of 59 nM. PROTAC BRD4 Degrader-21 induces ubiquitination of BRD4, leading to its degradation via the proteasome. PROTAC BRD4 Degrader-21 binds to recombinant HSP90α protein with moderate affinity, having an IC50 of 100-1000 nM. PROTAC BRD4 Degrader-21 induces cancer cell death. PROTAC BRD4 Degrader-21 inhibits tumor growth in xenograft mouse models. PROTAC BRD4 Degrader-21 can be used for the research of acute myeloid leukemia, diffuse large B-cell lymphoma .
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- HY-10256R
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SB 203580 (Standard); RWJ 64809 (Standard)
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Organoid
Reference Standards
p38 MAPK
Autophagy
Mitophagy
HSP
|
Inflammation/Immunology
Cancer
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Adezmapimod (Standard) is the analytical standard of Adezmapimod. This product is intended for research and analytical applications. Adezmapimod (SB 203580) is a selective and ATP-competitive p38 MAPK inhibitor with IC50s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. Adezmapimod inhibits LCK, GSK3β and PKBα with IC50s of 100-500-fold higher than that for SAPK2a/p38. Adezmapimod can inhibit p38 MAPK and lead to the inhibition of downstream HSP27 phosphorylation. Adezmapimod does not disrupt JNK activity and is an autophagy and mitophagy activator .
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- HY-183760
-
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Cholinesterase (ChE)
HSP
GSK-3
Amyloid-β
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Neurological Disease
Inflammation/Immunology
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AChE/BChE-IN-37 is a blood-brain barrier-permeable AChE/BChE inhibitor, with an IC50 of 73.65 μM against electric eel-derived AChE and an IC50 of 82.93 μM against horse-derived BChE. AChE/BChE-IN-37 exhibits chelating activity towards Cu 2+, Ca 2+, Mg 2+, Fe 2+ and Zn 2+. AChE/BChE-IN-37 interacts with HSP90AA1 and GSK-3β. AChE/BChE-IN-37 inhibits the self-induced aggregation of Aβ1-42. AChE/BChE-IN-37 suppresses LPS-induced NO production in cells. AChE/BChE-IN-37 can be used in research related to Alzheimer's disease and inflammatory diseases .
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- HY-N1934R
-
|
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Reference Standards
Potassium Channel
HSP
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
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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 .
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- HY-174468
-
|
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LYTACs
PD-1/PD-L1
HSP
|
Cancer
|
|
dPDL1-4 is a potent and selective eHSPTAC eHSP90 PD-L1 degrader with DC50s of 7.77 μM and 6.52 μM in HeLa and B16F10 cells. dPDL1-4 bridges eHSP90 with the target protein, inducing lysosomal degradation. dPDL1-4 can degrade PD-L1 significantly and inhibits tumor growth. dPDL1-4 can be used for the study of cervical cancer and melanoma. ((Pink: eHSP90 ligand (HY-174476); Blue: PD-L1 ligand (HY-116274); Black: Linker (HY-W021787); HSP ligand + linker: HY-174799)) .
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- HY-152263
-
|
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Hsp-targeting Chimeras
CDK
Apoptosis
|
Cancer
|
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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-N6606R
-
|
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Reference Standards
Glycosidase
Tyrosinase
Heme Oxygenase (HO)
HSP
|
Metabolic Disease
Inflammation/Immunology
|
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Delphinidin-3-O-galactoside chloride (Standard) is the analytical standard of Delphinidin-3-O-galactoside chloride (HY-N6606). This product is intended for research and analytical applications. Delphinidin-3-O-galactoside chloride is an anthocyanin found in abbiteye blueberry. Delphinidin-3-O-galactoside chloride show inhibitory activitiesagainst α-glucosidase with an IC50 of 68.33 μM, and tyrosinase with an IC50 of 34.14 μM. Delphinidin-3-O-galactoside chloride attenuates HO-1 and HSP70 messenger RNA down-regulation, suppresses cytotoxicity, reduces endoplasmic reticulum stress responses, scavenges free radicals, reduces intracellular triglyceride levels and lipid droplet accumulation. Delphinidin-3-O-galactoside chloride can be used for the researches of diabesity, melanoma and inflammation .
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- HY-N11262
-
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Phosphodiesterase (PDE)
Sirtuin
PGC-1α
p38 MAPK
HSP
TNF Receptor
NO Synthase
Apoptosis
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Metabolic Disease
Inflammation/Immunology
|
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Sudachitin is an orally active compound that potently inhibits mouse PDE1C and human PDE4B, with IC50 values of 5.0 μM and 15.0 μM, respectively. Sudachitin upregulates Sirt1 and PGC‑1α expression in skeletal muscle to regulate energy metabolism and promote mitochondrial biogenesis. Sudachitin improves lipid metabolism, glucose tolerance, insulin sensitivity, energy expenditure, and fatty acid β‑oxidation. Sudachitin activates p38MAPK signaling, induces HSP27 phosphorylation and caspase‑dependent apoptosis, and blocks EGF‑driven keratinocyte migration and proliferation. Sudachitin suppresses LPS‑induced TNF‑α, NO, and iNOS expression in macrophages and shows potent anti‑inflammatory activity. Sudachitin can be used for the research of metabolic syndrome, type 2 diabetes, and psoriasis. .
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- HY-175527
-
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HyT
Anaplastic lymphoma kinase (ALK)
Apoptosis
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Cancer
|
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ALK degrader 2 is an orally active ALK degrader that degrades EML4-ALK levels (DC50 = 8 nM) and nucleophosmin (NPM)-ALK protein levels (DC50 = 102 nM). ALK degrader 2 mediates ALK degradation via the Hsp70 chaperone system and ubiquitin-proteasome pathway. ALK degrader 2 induces significant S-phase cell cycle arrest and apoptosis in H3122 cells. ALK degrader 2 shows anti-tumor activity in mice bearing H3122 xenografts. ALK degrader 2 can be used for the study of non-small cell lung cancer (NSCLC). (Pink: ALK ligand (HY-W754809), Blue: Hyt (HY-W013021), Black: Linker (HY-Y1760), ALK ligand-linker conjugate (HY-175528)) .
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- HY-164548
-
|
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HSP
Apoptosis
PI3K
Akt
NF-κB
|
Inflammation/Immunology
Cancer
|
|
WK88-1 is an apoptosis inducer and Hsp90 client protein inhibitor with antiproliferative and immunomodulatory activities. WK88-1 inhibits signaling pathways such as PI3K/Akt and NF-κB, and induces mitochondrial dysfunction and cell cycle arrest. WK88-1 effectively suppresses cancer cell migration and invasion, and reverses various EGFR mutations and resistance to Gefitinib (HY-50895). WK88-1 also regulates the differentiation of monocytes and dendritic cells, blocks the expression of multiple chemokines, inhibits immune cell migration and M1 marker transcription, and restores impaired endocytic activity. WK88-1 has been used in studies of breast cancer, non-small cell lung cancer with various EGFR mutations or Met amplification, and atherosclerosis and other related diseases .
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- HY-D1063
-
|
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Fluorescent Dye
Apoptosis
Reactive Oxygen Species (ROS)
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Cancer
|
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IR-780 is a near-infrared fluorescent probe for in vivo imaging of tumor cells. IR-780 is transported into tumor cells via OATPs and ABCB10, with uptake dependent on glycolytic activity and plasma membrane potential. IR-780 preferentially accumulates in tumor cell mitochondria, including those of drug-resistant cancer cells, without chemical conjugation. IR-780 generates reactive oxygen species (ROS), induces hyperthermia and apoptosis, inhibits tumor growth and recurrence, and modulates HSP70 expression upon ultrasound or 808 nm laser exposure. IR-780 acts as a sonosensitizer, photodynamic and photothermal agent, and drug delivery carrier, with low acute imaging-dose toxicity and rapid vital organ clearance. IR-780 can be used for the research of cancer, such as breast cancer, lung cancer, and non-small cell lung cancer (NSCLC) .
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- HY-181907
-
|
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HyT
Keap1-Nrf2
HSP
|
Inflammation/Immunology
|
NBE5 is an orally active hydrophobic tag-targeting (Hyt) degrader (HyTTD) that targets Keap1. NBE5 mimics protein misfolding and recruits the molecular chaperone Hsp90, while achieving targeted degradation of Keap1 through both the ubiquitin-proteasome system and the autophagy-lysosome system. Consequently, NBE5 relieves the inhibition of the transcription factor Nrf2 by Keap1, potently activates the Nrf2-mediated endogenous antioxidant pathway, and upregulates the expression of downstream antioxidant proteins such as HO-1 and GCLM. NBE5 effectively alleviates oxidative stress and inflammatory damage, and exhibits excellent in vivo activity in a mouse model of acute colitis induced by DSS (HY-116282C) .
NBE5 consists of a hydrophobic tag (HY-W022007), a Keap1-Nrf2 ligand (HY-14909), and a linker (HY-W014831).
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- HY-182044
-
|
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Ras
Apoptosis
PARP
Caspase
CDK
|
Cancer
|
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MRTX849-amide-C4-(o)-carborane is a KRAS G12C inhibitor with mutation selectivity for cells expressing KRAS G12C. MRTX849-amide-C4-(o)-carborane shows low intrinsic cytotoxicity in cancer cells. MRTX849-amide-C4-(o)-carborane covalently binds to Cys12 of KRAS G12C, recruits Hsp70, promotes ubiquitination, and induces proteasome-dependent degradation of the target protein. MRTX849-amide-C4-(o)-carborane inhibits the activity of the downstream ERK signaling pathway and induces apoptosis signaling in cancer cells. MRTX849-amide-C4-(o)-carborane is applicable for the research of KRAS G12C-positive cancers .
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- HY-181727
-
|
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Androgen Receptor
HSP
CDK
|
Cancer
|
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AR/AR-V7 degrader-1 is an orally active AR and AR-V7 degrader. AR/AR-V7 degrader-1 disrupts the interaction between AR/AR-V7 and HSP90, leading to their ubiquitination and degradation in castration-resistant prostate cancer cells. AR/AR-V7 degrader-1 regulates the expression of cell cycle-related proteins in prostate cancer cells (downregulates CDK4, CDK6, Cyclin D1, Cyclin E1; upregulates P21) and induces G0/G1 phase arrest. AR/AR-V7 degrader-1 inhibits the proliferation and migration of prostate cancer cells. AR/AR-V7 degrader-1 suppresses the growth of castration-resistant prostate cancer tumors in nude mice and induces the degradation of AR and AR-V7 in tumor tissues. AR/AR-V7 degrader-1 is applicable to the research of castration-resistant prostate cancer .
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- HY-121708
-
|
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c-Kit
|
Cancer
|
|
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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- HY-168894
-
|
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Ferroptosis
JAK
STAT
p38 MAPK
AMPK
GSK-3
Apoptosis
HSP
TNF Receptor
|
Cardiovascular Disease
Neurological Disease
Metabolic Disease
Cancer
|
|
CT-1 is a secreted protein belonging to the IL-6 cytokine family. Overexpression of CT-1 enhances cell proliferation, migration and angiogenesis via the ADMA/DDAH pathway. CT-1 inhibits the growth of triple-negative breast cancer cells by simultaneously inducing Ferroptosis in N2-type tumor-associated neutrophils and cancer cells. CT-1 activates the Jak/STAT-3, p42/p44 MAPK and AMPK pathways, and inhibits GSK-3β activity through phosphorylation to induce cardiomyocyte hypertrophy. CT-1 enhances the viability of cardiomyocytes and neurons, reduces cell Apoptosis, induces the expression of heat shock proteins (HSP) and BNP, and inhibits TNF levels. CT-1 exerts anti-tumor activity in mouse models of triple-negative breast cancer. CT-1 improves cognitive impairment in mice. CT-1 is applicable to the research of ischemic heart disease, triple-negative breast cancer, myocardial hypertrophy, Parkinson's disease, hypertensive heart disease, myocardial infarction, acute Chagas cardiomyopathy, high-fat diet-induced cognitive impairment and diabetes-related cognitive impairment .
|
-
- HY-170820
-
|
|
Molecular Glues
Bcl-2 Family
CDK
EGFR
HSP
Androgen Receptor
c-Myc
|
Cancer
|
|
XYD049 is a CRBN-based molecular glue degrader targeting GSPT1, with a DC50 of 19 nM. XYD049 mediates the formation of a ternary complex between CRBN and GSPT1, thereby triggering CRBN- and proteasome-dependent degradation of GSPT1. By degrading GSPT1, XYD049 downregulates castration-resistant prostate cancer (CRPC)-related oncogenes, including BCL2, CDK2, E2F3, EGFR, HSP90B1, TMPRSS2, AR, AR-V7, PSA and c-Myc. XYD049 inhibits cancer cell growth and suppresses tumor growth in mice. XYD049 can be used for research on castration-resistant prostate cancer. XYD049 consists of a linker (black part) NH2-C5-NH-Boc (HY-W004710), a CRBN-based E3 ligase ligand (blue part) Thalidomide 4-fluoride (HY-41547), and a target protein ligand (red part) GSPT1 ligand-1 (HY-170821), among which the E3 ligase ligand plus linker forms the conjugate E3 Ligase Ligand-linker Conjugate 158 (HY-170822) .
|
-
- HY-N2445
-
|
|
Apoptosis
Akt
JNK
PERK
Caspase
PARP
MDM-2/p53
IAP
Reactive Oxygen Species (ROS)
SOD
FABP
Autophagy
AMPK
mTOR
GLUT
EGFR
PI3K
HSP
VEGFR
FAK
|
Cancer
|
|
Flavokawain C is an orally active natural chalcone. Flavokawain C inhibits the proliferation of various cancer cells. Flavokawain C upregulates GADD153 in cancer cells, inhibits the phosphorylation of Akt and JNK, suppresses early ERK phosphorylation, activates late ERK phosphorylation, activates caspase related subtypes, induces PARP-1 cleavage, causes upregulation of p21 and p27, downregulation of mutant p53 and anti-apoptotic IAP proteins, elevates intracellular ROS levels, reduces SOD activity, and induces apoptosis. Flavokawain C downregulates FABP4, induces autophagy in cancer cells, and activates the AMPK/mTOR pathway . Flavokawain C decreases the expression of glycolysis-related proteins GLUT1 and HK2, and inhibits glycolysis in nasopharyngeal carcinoma cells. Flavokawain C inhibits the activation of the EGFR/PI3K/Akt/mTOR signaling pathway and reduces the expression of HSP90B1. Flavokawain C inhibits angiogenesis by decreasing the expression of angiogenic proteins Ang-1 and VEGF in human umbilical vein endothelial cells. Flavokawain C increases γ-H2AX levels in cells, inhibits the phosphorylation of FAK, PI3K and AKT in cells, and induces DNA damage in cells. Flavokawain C exerts anti-tumor activity in multiple tumor xenograft mouse models. Flavokawain C is applicable to research related to colorectal cancer, colon adenocarcinoma, nephroblastoma, nasopharyngeal carcinoma and liver cancer .
|
-
| Cat. No. |
Product Name |
Type |
-
- HY-D1063
-
|
|
Fluorescent Dye
|
|
IR-780 is a near-infrared fluorescent probe for in vivo imaging of tumor cells. IR-780 is transported into tumor cells via OATPs and ABCB10, with uptake dependent on glycolytic activity and plasma membrane potential. IR-780 preferentially accumulates in tumor cell mitochondria, including those of drug-resistant cancer cells, without chemical conjugation. IR-780 generates reactive oxygen species (ROS), induces hyperthermia and apoptosis, inhibits tumor growth and recurrence, and modulates HSP70 expression upon ultrasound or 808 nm laser exposure. IR-780 acts as a sonosensitizer, photodynamic and photothermal agent, and drug delivery carrier, with low acute imaging-dose toxicity and rapid vital organ clearance. IR-780 can be used for the research of cancer, such as breast cancer, lung cancer, and non-small cell lung cancer (NSCLC) .
|
-
- HY-133705
-
|
|
Fluorescent Dye
|
|
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 (Ex/Em = 488/515 nm) .
|
-
- HY-122878
-
|
|
Fluorescent Dye
|
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-D2360
-
|
|
Fluorescent Dye
|
|
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 .
|
| Cat. No. |
Product Name |
Type |
-
- HY-158976
-
|
Lactated ringer's solution (LRS)
|
Biochemical Assay Reagents
|
|
Sodium lactate ringer's solution (Lactated ringer's solution (LRS)) is an isotonic crystal intravenous injection and arthroscopic irrigation solution containing racemic sodium lactate and electrolytes such as sodium, potassium, calcium and chloride (130 mEq sodium/L, 274 mOsm/L), which can be used as a cell integrity protectant. Sodium lactate ringer's solution maintains the integrity of human meniscus cells, ensures that they retain normal cell morphology, membrane regularity, size and density, and does not alter the mRNA expression levels of α1 (I) procollagen, α1 (II) procollagen, aggrecan or HSP70. Sodium lactate ringer's solution can be applied to studies related to extracellular fluid deficiency and meniscus tears .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-W014102
-
-
- HY-105063
-
|
|
HSP
|
Metabolic Disease
Inflammation/Immunology
|
|
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 .
|
-
- 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-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-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-P11053
-
|
|
HSP
|
Cancer
|
|
A17 peptide is a Hsp70-targeting peptide. A17 peptide binds to the ATP-binding domains of Hsp70. A17 peptide specifically inhibits the chaperone activity, thereby increasing the cells' sensitivity to apoptosis induced by chemotherapeutic agents, such as Cisplatin (HY-17394). A17 peptide can be used for anticancer chemotherapy research, such multiple myeloma .
|
-
- HY-P10541
-
|
|
HSP
|
Others
|
|
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 .
|
-
- HY-P10541A
-
|
|
HSP
|
Others
|
|
HSP70/DnaK substrate peptide TFA is a short peptide that the HSP70/DnaK molecular chaperone can bind and act on. HSP70/DnaK substrate peptide TFA can be used to study the mechanism of action of HSP70/DnaK in molecular chaperone function .
|
-
- HY-P11052
-
|
|
HSP
|
Cancer
|
|
A8 peptide is a Hsp72 antagonist. A8 peptide inhibits tumor progression and metastasis as well as enhances the cancer cells' sensitivity to apoptosis induced by chemotherapeutic agents (such as Cisplatin (HY-17394)) by blocking the Hsp72-TLR2 interaction and the subsequent activation of MDSCs. A8 peptide can be used for cancers research .
|
-
- 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-P10635
-
|
|
Biochemical Assay Reagents
|
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 .
|
-
- HY-P10757
-
-
- HY-P10371
-
|
txCD47
|
Reactive Oxygen Species (ROS)
Thrombopoietin Receptor
Mitochondrial Metabolism
HSP
HSV
CD47
|
Infection
Inflammation/Immunology
Cancer
|
|
PKHB1 (txCD47) is a CD47 agonist and Thrombospondin-1 peptide mimetic. PKHB1 activates CD47 and triggers Caspase-independent, calcium-dependent cell death via mitochondrial alterations, ROS production, endoplasmic reticulum morphological changes, and dissipation of mitochondrial membrane potential. PKHB1 induces the exposure of Calreticulin, HSP70, and HSP90, thereby driving immunogenic cell death. PKHB1 promotes intratumoral CD8 + T cell infiltration and inhibits breast tumorigenesis. PKHB1 reduces HSV-1 levels and alleviates the severity of herpes simplex keratitis. PKHB1 can be used in research related to breast cancer, herpes simplex keratitis, and T-cell acute lymphoblastic leukemia .
|
-
- HY-W014102R
-
|
|
Reference Standards
Endogenous Metabolite
|
Metabolic Disease
Inflammation/Immunology
|
|
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 .
|
-
- HY-P1896
-
|
|
HSP
|
Infection
Neurological Disease
Cancer
|
|
Hsp70-derived octapeptide is a conserved octapeptide of the C-terminal end of Hsp70, which physically interacts with tetratricopeptide repeat (TPR) motifs .
|
-
- HY-P11185
-
|
|
HSP
|
Cancer
|
|
Hsp90β decapeptide is a C-terminal peptide of Hsp90β, which contains conserved TPR-domain MEEVD. Hsp90β decapeptide is able to bind tightly the Tah1 protein with a Kd of 1.0 μM .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-15230
-
-
-
- HY-B0425A
-
-
-
- HY-W014102
-
-
-
- HY-N6769
-
-
-
- HY-N0576
-
-
-
- HY-N1934
-
-
-
- HY-N2468
-
|
1,4-β-D-Xylobiose; 1,4-D-Xylobiose
|
Zea mays L.
Polysaccharides
Classification of Application Fields
Gramineae
Other Diseases
Plants
Disease Research Fields
Saccharides
Source Classification
|
TNF Receptor
Claudin
HSP
|
|
Xylobiose (1,4-β-D-Xylobiose; 1,4-D-Xylobiose) is an orally active Claudin 2/CLDN2 inhibitor and HSP27 inducer. Xylobiose works by regulating intestinal barrier function and glucose and lipid metabolism-related signaling pathways. Xylobiose inhibits CLDN2 expression to reduce intestinal permeability, induces HSP27 to enhance cell protection, and regulates the miR-122a/miR-33a axis to inhibit liver lipid synthesis and improve insulin resistance. Xylobiose can strengthen intestinal barrier integrity, reduce blood sugar and blood lipid levels, and reduce oxidative stress and inflammatory response. Xylobiose can be used in the study of type 2 diabetes and metabolic syndrome .
|
-
-
- HY-13425
-
-
-
- HY-N1073
-
|
6-Isopentenylgenistein; Erythrinin B
|
Leguminosae
Genista ephedroides DC.
Plants
Isoflavones
Source Classification
|
Apoptosis
EGFR
HSP
ERK
Akt
|
Wighteone (6-Isopentenylgenistein; Erythrinin B) is a prenylated isoflavone that acts as a HSP90/EGFR L858R/T790M inhibitor and antifungal agent. Wighteone reduces the expression level of HSP90, blocks EGF-induced phosphorylation of EGFR, and thereby inhibits the downstream ERK and AKT signaling pathways. Wighteone induces cell cycle redistribution, inhibits proliferation and triggers apoptosis in cancer cells. Wighteone can be isolated from Erythrina suberosa, and can also be induced to synthesize in Lotus japonicus under specific conditions. Wighteone can be used to study HER2-positive breast cancer, leukemia, non-small cell lung cancer with EGFR L858R/T790M mutation, and fungal infections .
|
-
-
- HY-N1986
-
-
-
- HY-N6790
-
-
-
- HY-107577
-
-
-
- HY-B1434
-
-
-
- HY-N0754
-
-
-
- HY-N2445
-
|
|
Structural Classification
Classification of Application Fields
Piperaceae
Plants
Chalcones
Flavonoids
other families
Phenols
Polyphenols
Piper methysticum G.Forst.
Disease Research Fields
Source Classification
Cancer
|
Apoptosis
Akt
JNK
PERK
Caspase
PARP
MDM-2/p53
IAP
Reactive Oxygen Species (ROS)
SOD
FABP
Autophagy
AMPK
mTOR
GLUT
EGFR
PI3K
HSP
VEGFR
FAK
|
|
Flavokawain C is an orally active natural chalcone. Flavokawain C inhibits the proliferation of various cancer cells. Flavokawain C upregulates GADD153 in cancer cells, inhibits the phosphorylation of Akt and JNK, suppresses early ERK phosphorylation, activates late ERK phosphorylation, activates caspase related subtypes, induces PARP-1 cleavage, causes upregulation of p21 and p27, downregulation of mutant p53 and anti-apoptotic IAP proteins, elevates intracellular ROS levels, reduces SOD activity, and induces apoptosis. Flavokawain C downregulates FABP4, induces autophagy in cancer cells, and activates the AMPK/mTOR pathway . Flavokawain C decreases the expression of glycolysis-related proteins GLUT1 and HK2, and inhibits glycolysis in nasopharyngeal carcinoma cells. Flavokawain C inhibits the activation of the EGFR/PI3K/Akt/mTOR signaling pathway and reduces the expression of HSP90B1. Flavokawain C inhibits angiogenesis by decreasing the expression of angiogenic proteins Ang-1 and VEGF in human umbilical vein endothelial cells. Flavokawain C increases γ-H2AX levels in cells, inhibits the phosphorylation of FAK, PI3K and AKT in cells, and induces DNA damage in cells. Flavokawain C exerts anti-tumor activity in multiple tumor xenograft mouse models. Flavokawain C is applicable to research related to colorectal cancer, colon adenocarcinoma, nephroblastoma, nasopharyngeal carcinoma and liver cancer .
|
-
-
- HY-N1455
-
-
-
- HY-N7627
-
-
-
- HY-113314
-
-
-
- HY-N6606
-
-
-
- HY-119906
-
-
-
- HY-108486
-
-
-
- HY-N12717
-
|
|
Terminalia arjuna (Roxb. ex DC.) Wight & Arn.
Structural Classification
Combretaceae
Phenols
Polyphenols
Plants
Source Classification
|
PAK
FASTK
HSP
p38 MAPK
NF-κB
NO Synthase
COX
HSV
Caspase
TNF Receptor
Fungal
Apoptosis
|
|
Casuarinin is an orally active antiproliferative, anti-inflammatory, antifungal, virucidal and gastroprotective agent. Casuarinin upregulates the expression of p21/WAF1, Fas/APO‑1, mFasL, sFasL and HSP‑70, arrests cell cycle, induces apoptosis and inhibits cancer cell proliferation. Casuarinin inhibits TNF‑α-induced phosphorylation of MAPK and activation of NF‑κB, downregulates the expression of iNOS, NF‑κB, COX‑2 and ICAM‑1, and reduces the production of proinflammatory mediators. Casuarinin attenuates ethanol-induced activation of caspase‑3 and elevation of TNF‑α, inhibits the growth of Candida albicans, and inhibits HSV‑2. Casuarinin can be used in research related to mammary adenocarcinoma, inflammatory skin diseases, gastric ulcers, candidiasis and herpes simplex virus infections .
|
-
-
- HY-N14780
-
|
(+)-Pochonin D
|
Structural Classification
Natural Products
Microorganisms
Source Classification
|
HSP
Interleukin Related
Enterovirus
|
|
Pochonin D ((+)-Pochonin D) is an inhibitor of heat shock protein 90 (Hsp90) with antiviral and anti-inflammatory activities. Pochonin D inhibits Hsp90, affects the homeostasis, folding and assembly processes of viral proteins, and reduces the replication capacity of viruses. Pochonin D reduces the infiltration of inflammatory cells, decreases the secretion of inflammatory cytokines such as TNF-α and IL-1β, and alleviates inflammatory responses. Pochonin D is a promising candidate for research on human rhinovirus (HRV) infection and cancer .
|
-
-
- HY-N3417
-
-
-
- HY-N11262
-
|
|
Structural Classification
Flavonoids
Flavones
Rutaceae
Citrus sudachi Hort. ex Shirai.
Plants
Source Classification
|
Phosphodiesterase (PDE)
Sirtuin
PGC-1α
p38 MAPK
HSP
TNF Receptor
NO Synthase
Apoptosis
|
|
Sudachitin is an orally active compound that potently inhibits mouse PDE1C and human PDE4B, with IC50 values of 5.0 μM and 15.0 μM, respectively. Sudachitin upregulates Sirt1 and PGC‑1α expression in skeletal muscle to regulate energy metabolism and promote mitochondrial biogenesis. Sudachitin improves lipid metabolism, glucose tolerance, insulin sensitivity, energy expenditure, and fatty acid β‑oxidation. Sudachitin activates p38MAPK signaling, induces HSP27 phosphorylation and caspase‑dependent apoptosis, and blocks EGF‑driven keratinocyte migration and proliferation. Sudachitin suppresses LPS‑induced TNF‑α, NO, and iNOS expression in macrophages and shows potent anti‑inflammatory activity. Sudachitin can be used for the research of metabolic syndrome, type 2 diabetes, and psoriasis. .
|
-
-
- HY-N6249
-
-
-
- HY-15230R
-
-
-
- HY-N15154
-
-
-
- HY-13425R
-
-
-
- HY-N1934R
-
|
|
Alkaloids
Structural Classification
other families
Plants
Isoquinoline Alkaloids
Source Classification
|
Reference Standards
Potassium Channel
HSP
|
|
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-126601
-
-
-
- HY-N2468R
-
|
1,4-β-D-Xylobiose (Standard); 1,4-D-Xylobiose (Standard)
|
Structural Classification
Zea mays L.
Polysaccharides
Gramineae
Plants
Saccharides
Source Classification
|
Reference Standards
TNF Receptor
Claudin
HSP
|
|
Xylobiose (1,4-β-D-Xylobiose; 1,4-D-Xylobiose) is an orally active Claudin 2/CLDN2 inhibitor and HSP27 inducer. Xylobiose works by regulating intestinal barrier function and glucose and lipid metabolism-related signaling pathways. Xylobiose inhibits CLDN2 expression to reduce intestinal permeability, induces HSP27 to enhance cell protection, and regulates the miR-122a/miR-33a axis to inhibit liver lipid synthesis and improve insulin resistance. Xylobiose can strengthen intestinal barrier integrity, reduce blood sugar and blood lipid levels, and reduce oxidative stress and inflammatory response. Xylobiose can be used in the study of type 2 diabetes and metabolic syndrome .
|
-
-
- HY-125037
-
-
-
- HY-N15449
-
|
|
Natural Products
Microorganisms
Source Classification
|
HSP
Caspase
Apoptosis
Reactive Oxygen Species (ROS)
Bcl-2 Family
|
|
Vicanicin is a depsidone compound found in lichens. Vicanicin inhibits the expression of Hsp70, regulates the redox-sensitive mechanisms within cells, promotes the increase of reactive oxygen species (ROS) in cancer cells, changes the Bax/Bcl-2 ratio, activates caspase-3, and triggers apoptosis. Vicanicin inhibits cell growth and induces apoptosis in androgen-sensitive (LNCaP) and androgen-insensitive (DU-145) human prostate cancer cells. Vicanicin is promising for research of prostate cancer .
|
-
-
- HY-N0576R
-
-
-
- HY-W014102R
-
-
-
- HY-119552
-
-
-
- HY-N1986R
-
-
-
- HY-N6606R
-
|
|
Structural Classification
Anthocyans
Flavonoids
Cornaceae
Cornus officinalis Sieb. et Zucc.
Phenols
Polyphenols
Plants
Source Classification
|
Reference Standards
Glycosidase
Tyrosinase
Heme Oxygenase (HO)
HSP
|
|
Delphinidin-3-O-galactoside chloride (Standard) is the analytical standard of Delphinidin-3-O-galactoside chloride (HY-N6606). This product is intended for research and analytical applications. Delphinidin-3-O-galactoside chloride is an anthocyanin found in abbiteye blueberry. Delphinidin-3-O-galactoside chloride show inhibitory activitiesagainst α-glucosidase with an IC50 of 68.33 μM, and tyrosinase with an IC50 of 34.14 μM. Delphinidin-3-O-galactoside chloride attenuates HO-1 and HSP70 messenger RNA down-regulation, suppresses cytotoxicity, reduces endoplasmic reticulum stress responses, scavenges free radicals, reduces intracellular triglyceride levels and lipid droplet accumulation. Delphinidin-3-O-galactoside chloride can be used for the researches of diabesity, melanoma and inflammation .
|
-
-
- HY-N9722
-
|
|
Quinones
Structural Classification
Microorganisms
Naphthalene Quinones
Source Classification
|
HSP
|
|
Dehydroherbarin is a selective inhibitor targeting HSP90α with blood-brain barrier penetration. Dehydroherbarin interferes with key pathways of tumor cell survival by binding to HSP90α, while exerting moderate antibacterial and anti-hepatitis A virus activities and inhibiting tumor cell migration. Dehydroherbarin can be used in research on tumors such as breast cancer .
|
-
| 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 .
|
-
-
- HY-17504AS1
-
|
|
|
Rosuvastatin-d6 (ZD 4522-d6) is deuterium labeled Rosuvastatin. 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-17504BS1
-
|
|
|
Rosuvastatin-d6 sodium is deuterium 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-10211S
-
|
|
|
Tanespimycin-d5 (17-AAG-d5; NSC 330507-d5; CP 127374-d5) is the deuterium labeled Tanespimycin (HY-10211). 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-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-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 .
|
-
-
- HY-13757AS1
-
|
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Tamoxifen-d3 is the deuterium labeled Tamoxifen . 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 .
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- HY-W778408
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Tamoxifen- 13C6 (ICI 47699- 13C6) is the 13C-labeled Tamoxifen (HY-13757A). 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 transgenic mouse .
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Product Name |
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Classification |
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- HY-115997
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PROTAC Synthesis
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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-152263
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PROTAC Synthesis
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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-117395
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Alkynes
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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.
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- HY-118783
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(±)-2-Hexyl-4-pentynoic acid
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Alkynes
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2-Hexyl-4-pentynoic acid ((±)-2-Hexyl-4-pentynoic acid), a Valproic acid (HY-10585) derivative, exhibits potential roles of HDAC inhibition (IC50 = 13 μM) and HSP70 induction. 2-Hexyl-4-pentynoic acid causes histone hyperacetylation and protect against glutamate-induced excitotoxicity in cultured neurons. 2-Hexyl-4-pentynoic acid can be used for the study of breast carcinoma. 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 .
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- HY-169098
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Alkynes
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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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| Cat. No. |
Product Name |
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Classification |
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- HY-145722
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OGX-427 sodium
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Antisense Oligonucleotides
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Apatorsen (OGX-427) sodium is a 2'-methoxyethyl-modified antisense oligonucleotide and also a Hsp27 inhibitor. Apatorsen sodium reduces Hsp27 mRNA and protein levels, impairs stress-induced cytoprotective functions, induces cell apoptosis, inhibits tumor growth and prevents metastasis. Apatorsen sodium is applicable to research related to non-small cell lung cancer, castration-resistant prostate cancer, breast cancer, ovarian cancer and bladder cancer .
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- HY-145722A
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OGX-427
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Antisense Oligonucleotides
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Apatorsen is a 2'-methoxyethyl-modified antisense oligonucleotide and also a Hsp27 inhibitor. Apatorsen reduces Hsp27 mRNA and protein levels, impairs stress-induced cytoprotective functions, induces cell apoptosis, inhibits tumor growth and prevents metastasis. Apatorsen is applicable to research related to non-small cell lung cancer, castration-resistant prostate cancer, breast cancer, ovarian cancer and bladder cancer .
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- HY-RS06415
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siRNAs
Human Pre-designed siRNA Sets
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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.
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- HY-RS18017
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siRNAs
Mouse Pre-designed siRNA Sets
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Hsp90ab1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Hsp90ab1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
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- HY-RS21240
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siRNAs
Mouse Pre-designed siRNA Sets
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Hsp90b1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Hsp90b1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
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- HY-RS06419
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siRNAs
Human Pre-designed siRNA Sets
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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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- HY-RS06416
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siRNAs
Mouse Pre-designed siRNA Sets
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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.
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- HY-RS06418
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siRNAs
Human Pre-designed siRNA Sets
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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.
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- HY-RS06417
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siRNAs
Rat Pre-designed siRNA Sets
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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.
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- HY-RS27757
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siRNAs
Rat Pre-designed siRNA Sets
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Hsp90b1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Hsp90b1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
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- HY-RS24490
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siRNAs
Rat Pre-designed siRNA Sets
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Hsp90ab1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Hsp90ab1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
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