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HSP70-IN-1

  Cat. No.:  DC10344   Featured
Chemical Structure
1268273-90-0
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More than 5000 active chemicals with high quality for research!
Field of application
HSP70-IN-1 is a heat shock protein (HSP) inhibitor; inhibits the growth of Kasumi-1 cells with an IC50 of 2.3 μM.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1268273-90-0
SMILES: O=C(NC1=CC=CC(SC2=CN=C(N3CCN(C)CC3)N=C2OCC4=CC=CC=C4)=C1)CN
Formula: C24H28N6O2S
M.Wt: 464.58
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: HSP70-IN-1 is a heat shock protein (HSP) inhibitor; inhibits the growth of Kasumi-1 cells with an IC50 of 2.3 μM.
Target: HSP70 Caspase-3/7:1.9 μM (IC50, MOLM13 cells)
In Vitro: The heat shock protein 70 (Hsp70) is a molecular chaperone which plays an important function in protein homeostasis as well as in cell signaling and survival. Hsp70 is frequently overexpressed in cancer, where the elevated expression is furthermore believed to be a cause of or to lead to resistance to chemotherapy and other treatments. HSP70-IN-1 interferes with the formation of functional Hsp70-HOP-Hsp90 machinery by its ability to dose-dependently alter the megacomplex components and to destabilize an Hsp70-Hsp90 machinery client, Raf-1. In cells, the refolding of heat-denatured luciferase by endogenous as well as transfected Hsp70 is inhibited by HSP70-IN-1. HSP70-IN-1 also results in induction of apoptosis in cancer cells. Addition of HSP70-IN-1to cancer cells dose-dependently alters the formation of the Hsp70-HOP complex, a phenomenon associated with their destabilization and reduction in half-life[1].
References: [1]. Taldone T, et al. Heat shock protein 70 inhibitors. 2. 2,5'-thiodipyrimidines, 5-(phenylthio)pyrimidines, 2-(pyridin-3-ylthio)pyrimidines, and 3-(phenylthio)pyridines as reversible binders to an allosteric site on heat shock protein 70. J Med Chem. 2014 Feb 27;57(4):1208-24.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
DC70417 Foldamer 33 Foldamer 33 is a small molecule HSP110 inhibitor, directly binds to the nucleotide-binding domain (NBD) of HSP110, blocks HSP110 chaperone function and colorectal cancer growth.Foldamer 33 significantly inhibit HSP110 anti-aggregating activity with IC50 of 87.8 uM.Foldamer 33 disrupts HSP110-STAT3 interaction with IC50 of 35.9 uM in competitive BLI assays.Foldamer 33 inhibits SW480 colorectal cancer cell proliferation, and (5 mg/kg) Foldamer 33 displays an anti-tumor effect (TGI of 40% and 60%) in mice bearing a colorectal cancer.
DC47938 NCT-58 NCT58(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.
DC46184 YUM70 YUM70 is a potent inhibitor of glucose-regulated protein 78 (GRP78) inhibitor with an IC50 of 1.5 μM. YUM70 induces endoplasmic reticulum (ER) stress-mediated apoptosis in pancreatic cancer.
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DC44512 Conglobatin 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.
DC40344 3-Phenyltoxoflavin 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.
DC5133 SNX-2112 (PF-04928473) SNX-2112 selectively binds to the ATP pocket of HSP90α and HSP90β with Ka of 30 nM and 30 nM, uniformly more potent than 17-AAG.
DC7449 KW-2478 KW-2478 is a nonansamycin HSP90 inhibitor with IC50 of 3.8 nM. Phase 1/2
DC10344 HSP70-IN-1 HSP70-IN-1 is a heat shock protein (HSP) inhibitor; inhibits the growth of Kasumi-1 cells with an IC50 of 2.3 μM.
DC11617 PU-H54 PU-H54 is potent, selective Grp94 inhibitor.
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