NMS-E973 - CAS 1253584-84-7
Catalog number:
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
Molecular Weight:
NMS-E973 shows a widespread antiproliferative activity with an average IC50 of 1.6 μM, and induces the degradation of client protein.
Publictions citing BOC Sciences Products
  • >> More
Brife Description:
NMS-E973 is a potent and selective Hsp90 inhibitor with DC50 of <10 nM for Hsp90 binding, no activiy against a panel of 52 diverse protein kinases.
Solid powder
DMSO: 90 mg/mL warming
3 years -20oC powder, 6 months-80oC in solvent.
Quality Standard:
Canonical SMILES:
1.NMS-E973, a novel synthetic inhibitor of Hsp90 with activity against multiple models of drug resistance to targeted agents, including intracranial metastases.
Fogliatto G1, Gianellini L, Brasca MG, Casale E, Ballinari D, Ciomei M, Degrassi A, De Ponti A, Germani M, Guanci M, Paolucci M, Polucci P, Russo M, Sola F, Valsasina B, Visco C, Zuccotto F, Donati D, Felder E, Pesenti E, Galvani A, Mantegani S, Isacchi A Clin Cancer Res. 2013 Jul 1;19(13):3520-32. doi: 10.1158/1078-0432.CCR-12-3512. Epub 2013 May 14.
PURPOSE: Recent developments of second generation Hsp90 inhibitors suggested a potential for development of this class of molecules also in tumors that have become resistant to molecular targeted agents. Disease progression is often due to brain metastases, sometimes related to insufficient drug concentrations within the brain. Our objective was to identify and characterize a novel inhibitor of Hsp90 able to cross the blood-brain barrier (BBB).
2.Discovery of NMS-E973 as novel, selective and potent inhibitor of heat shock protein 90 (Hsp90).
Brasca MG1, Mantegani S, Amboldi N, Bindi S, Caronni D, Casale E, Ceccarelli W, Colombo N, De Ponti A, Donati D, Ermoli A, Fachin G, Felder ER, Ferguson RD, Fiorelli C, Guanci M, Isacchi A, Pesenti E, Polucci P, Riceputi L, Sola F, Visco C, Zuccotto F, Fo Bioorg Med Chem. 2013 Nov 15;21(22):7047-63. doi: 10.1016/j.bmc.2013.09.018. Epub 2013 Sep 19.
Novel small molecule inhibitors of heat shock protein 90 (Hsp90) were discovered with the help of a fragment based drug discovery approach (FBDD) and subsequent optimization with a combination of structure guided design, parallel synthesis and application of medicinal chemistry principles. These efforts led to the identification of compound 18 (NMS-E973), which displayed significant efficacy in a human ovarian A2780 xenograft tumor model, with a mechanism of action confirmed in vivo by typical modulation of known Hsp90 client proteins, and with a favorable pharmacokinetic and safety profile.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related Hsp90 Products

CAS 4434-05-3 Coumermycin A1

Coumermycin A1
(CAS: 4434-05-3)

Coumemycin A1 is found to bind at a second ATP-binding site in the C-terminal domain of Hsp90, thus disrupting the dimerization of the Hsp90 complex.IC50 70μmol...

CAS 908112-43-6 SNX-2112

(CAS: 908112-43-6)

SNX-2112 is an Hsp90 inhibitor which is currently undergoing multiple phase 1 clinical trials. In all cell lines, SNX-2112 led to degradation of MET, HER-2, EGF...

(CAS: 1260533-36-5)

TAS-116 is a inhibitor of Hsp90. It induces significant cytotoxicity in MM cells even in the presence of BMSCs, associates with downregulation of phospho-Akt an...

CAS 12772-57-5 Radicicol

(CAS: 12772-57-5)

Radiocicol is an antifungal antibiotic. It inhibits heat Hsp90 activity by binding to the ATP-binding pocket, subsequently suppressing cell transformation induc...

Pochonin D
(CAS: 544712-82-5)

Pochocin D is a patent Hsp90 inhibitor. IC50 80.0nM.

PF-04929113 mesylate
(CAS: 1173111-67-5)

The methlate salt form of PF-04929113 that has potential antineoplastic activity targeting Hsp90. It could probably result in the proteasomal degradation of onc...

EC 144
(CAS: 911397-80-3)

EC 114 is a high affinity, potent and selective Hsp90 inhibitor. IC50 1.1 nM. It exhibits selectivity for Hsp90 over Grp94 and TRAP1 (Ki values are 61 and 255 n...

CAS 747413-08-7 VER-50589

(CAS: 747413-08-7)

VER-50589 is a potent Hsp90 inhibitor with IC50 of 21 nM for Hsp90β.

(CAS: 1860793-58-3)

CPUY201112 is an N-terminal Hsp90 inhibitor, which leads to decreased expression of Hsp90 client proteins and may result in increased tumor cell apoptosis.

CAS 1134156-31-2 VER-155008

(CAS: 1134156-31-2)

VER-155008 is an adenosine-derived inhibitor of heat shock protein 70 (Hsp70; IC50 = 0.5 µM) that is selective over Hsp90.It targets the nucleotide-binding doma...

CAS 912999-49-6 Onalespib

(CAS: 912999-49-6)

Onalespib, also known as AT13387, is a synthetic, orally bioavailable, small-molecule inhibitor of heat shock protein 90 (Hsp90) with potential antineoplastic a...

(CAS: 1373761-12-6)

NW-457 is a potent Hsp90 inhibitor with no detectable hepatocytotoxicity in vitro. It synergizes with ionizing irradiation to induce chromatin condensation, nuc...

CAS 467214-21-7 Alvespimycin HCl

Alvespimycin HCl
(CAS: 467214-21-7)

Alvespimycin hydrochloride is the hydrochloride salt of alvespimycin, an analogue of the antineoplastic benzoquinone antibiotic geldanamycin. Alvespimycin binds...

CAS 959763-06-5 CH5138303

(CAS: 959763-06-5)

CH5138303 is a novel and potent Hsp90 inhibitor. CH5138303 showed high binding affinity for N-terminal Hsp90α (Kd=0.52nM) and strong in vitro cell growth inhibi...

(CAS: 1202920-93-1)

SST0116CL1 is a second-generation small molecule inhibitor of Hsp90, which leads to decreased expression of Hsp90 client proteins and reduced tumor cell prolife...

CAS 70563-58-5 Herbimycin A

Herbimycin A
(CAS: 70563-58-5)

Herbimycin A is an ansamycin antibiotic that acts as a Src family kinase inhibitor. Binds to the SH domain and inhibits the activity of p60v-src and p210BCR-ABL...

CAS 303-81-1 Novobiocin

(CAS: 303-81-1)

Novobiocin is found to bind at a second ATP-binding site in the C-terminal domain of Hsp90, thus disrupting the interaction of both p23 and Hsp70 co-chaperones ...

CAS 467214-20-6 Alvespimycin

(CAS: 467214-20-6)

Alvespimycin (17-DMAG; KOS-1022; NSC 707545) is a potent, H2O-soluble Hsp90 inhibitor with IC50 of 62 nM.17-DMAG displays ~2 times potency against human Hsp90 t...

CAS 911710-03-7 17-AAG hydrochloride

17-AAG hydrochloride
(CAS: 911710-03-7)

17-AAG hydrochloride is a potent HSP90 inhibitor with IC50 value of 5 nM, which is a 100-fold higher binding affinity for HSP90 derived from tumour cells than t...

CAS 1149705-71-4 XL888

(CAS: 1149705-71-4)

XL888 is an ATP-competitive inhibitor of Hsp90. Through this action, specific client proteins are degraded, leading to cell cycle arrest or apoptosis. XL888 is ...

Chemical Structure

CAS 1253584-84-7 NMS-E973

Quick Inquiry

Verification code

Featured Items