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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
48 Results for "
Hsp90α
" in MedChemExpress (MCE) Product Catalog:
Products (48)
48 Results for "Hsp90α" in MCE Product Catalog:
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Pimitespib (TAS-116) is an oral bioavailable, ATP-competitive, highly specific HSP90α/HSP90β inhibitor (Kis of 34.7 nM and 21.3 nM, respectively) without inhibiting other HSP90 family proteins such as GRP94 . Pimitespib demonstrates less ocular toxicity .
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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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5 Cited Publications
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Research Areas:
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 .
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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.
4
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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2 Cited Publications
Cat. No.: HY-17547
CAS No.: 1253584-84-7
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 .
Cat. No.: HY-155113
CAS No.: 3031078-90-4
PROTAC Hsp90α degrader 1 is a selective PROTAC Hsp90α degrader with a DC50 of 0.295 μM. PROTAC Hsp90α degrader 1 exhibits antitumor activity with low toxic side effects. PROTAC Hsp90α degrader 1 can be used for the research of breast cancer .
Cat. No.: HY-N7627
CAS No.: 117591-85-2
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 .
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.
Research Areas:
Hsp90-IN-17 hydrochloride is a Hsp90 inhibitor. Hsp90-IN-17 hydrochloride binds to the N-terminal ATP-binding pocket of Hsp90, inhibits its chaperone function, and induces the degradation of Hsp90 client proteins. Hsp90-IN-17 hydrochloride inhibits cancer cell proliferation. Hsp90-IN-17 hydrochloride can be used in the research of ovarian cancer .
Cat. No.: HY-173337
CAS No.: 184897-90-3
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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 .
Cat. No.: HY-156566
CAS No.: 2503036-46-0
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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 .
Cat. No.: HY-149431
Target:
Research Areas:
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 .
Cat. No.: HY-169133
CAS No.: 2991588-80-6
Research Areas:
GDCNF-11 is a type of HSP90 interaction-mediated protein degradation chimera (HIM-PROTAC) degrader that targets and degrades GPX4, with a DC50 of 0.08 μM. GDCNF-11 mediates the ubiquitination and proteasome-dependent degradation of GPX4 by recruiting GPX4 to form a ternary complex with HSP90, increases intracellular lipid peroxides and ROS, and ultimately triggers Ferroptosis. GDCNF-11 inhibits tumor growth in mouse models, downregulates GPX4 protein in xenograft tumors, and upregulates the lipid peroxidation marker. GDCNF-11 can be used for the research of fibrosarcoma .
Cat. No.: HY-170910
CAS No.: 3065556-75-1
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 .
Cat. No.: HY-178956
CAS No.: 2393980-27-1
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 .
Cat. No.: HY-168205
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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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
