Cat. No.: HY-111165

SNX-7081

SNX-7081 is an Hsp90 inhibitor with K_i 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.

For research use only. We do not sell to patients.

CAS No.: 908111-22-8
Formula: C₂₄H₃₁N₃O₃
Molecular Weight:409.53

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

SNX-7081 Chemical Structure

CAS No.: 908111-22-8

Size

Price

Stock

Quantity

Amount: USD 0.00

* Please select Quantity before adding items.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

HSP90

26 nM (Ki)

HSP90

44 nM (Ki)

All HSP Isoforms :

All NF-κB Isoforms :

All ERK Isoforms :

All JNK Isoforms :

All PDGFR Isoforms :

All DNA/RNA Synthesis Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A-375	IC₅₀	14 nM Compound: 34	Inhibition of Hsp90 in human A375 cells assessed as Hsp70 induction after 24 hrs by high content screening Inhibition of Hsp90 in human A375 cells assessed as Hsp70 induction after 24 hrs by high content screening	[PMID: 19552433]
A-375	IC₅₀	7 nM Compound: 34	Inhibition of Hsp90 in human A375 cells assessed as pS6 degradation after 24 hrs by high content screening Inhibition of Hsp90 in human A375 cells assessed as pS6 degradation after 24 hrs by high content screening	[PMID: 19552433]
A-375	IC₅₀	9 nM Compound: 34	Antiproliferative activity against human A375 cells after 72 to 144 hrs by cyquant DNA dye method Antiproliferative activity against human A375 cells after 72 to 144 hrs by cyquant DNA dye method	[PMID: 19552433]
AU565	IC₅₀	16 nM Compound: 34	Inhibition of Hsp90 in human AU565 cells assessed as pERK degradation after 24 hrs by high content screening Inhibition of Hsp90 in human AU565 cells assessed as pERK degradation after 24 hrs by high content screening	[PMID: 19552433]
AU565	IC₅₀	7 μM Compound: 34	Inhibition of Hsp90 in human AU565 cells assessed as Her2 degradation after 24 hrs by high content screening Inhibition of Hsp90 in human AU565 cells assessed as Her2 degradation after 24 hrs by high content screening	[PMID: 19552433]
HCT-15	IC₅₀	61 nM Compound: 34	Antiproliferative activity against human HCT15 cells after 72 to 144 hrs by cyquant DNA dye method Antiproliferative activity against human HCT15 cells after 72 to 144 hrs by cyquant DNA dye method	[PMID: 19552433]
HT-29	IC₅₀	7 nM Compound: 34	Antiproliferative activity against human HT-29 cells after 72 to 144 hrs by cyquant DNA dye method Antiproliferative activity against human HT-29 cells after 72 to 144 hrs by cyquant DNA dye method	[PMID: 19552433]
K562	IC₅₀	3 nM Compound: 34	Antiproliferative activity against human K562 cells after 72 to 144 hrs by cyquant DNA dye method Antiproliferative activity against human K562 cells after 72 to 144 hrs by cyquant DNA dye method	[PMID: 19552433]
LNCaP	IC₅₀	4 nM Compound: 34	Antiproliferative activity against human LNCAP cells after 72 to 144 hrs by cyquant DNA dye method Antiproliferative activity against human LNCAP cells after 72 to 144 hrs by cyquant DNA dye method	[PMID: 19552433]
MCF7	IC₅₀	10 nM Compound: 34	Antiproliferative activity against human MCF7 cells after 72 to 144 hrs by cyquant DNA dye method Antiproliferative activity against human MCF7 cells after 72 to 144 hrs by cyquant DNA dye method	[PMID: 19552433]
MDA-MB-231	IC₅₀	10 nM Compound: 34	Antiproliferative activity against human MDA-MB-231 cells after 72 to 144 hrs by cyquant DNA dye method Antiproliferative activity against human MDA-MB-231 cells after 72 to 144 hrs by cyquant DNA dye method	[PMID: 19552433]
MRC5	CC₅₀	24.93 μM Compound: SNX-7081	Cytotoxicity against human MRC5 cells after 48 hrs by MTT assay Cytotoxicity against human MRC5 cells after 48 hrs by MTT assay	[PMID: 22704890]
NCI-H460	IC₅₀	248 nM Compound: 34	Antiproliferative activity against human NCI-H460 cells after 72 to 144 hrs by cyquant DNA dye method Antiproliferative activity against human NCI-H460 cells after 72 to 144 hrs by cyquant DNA dye method	[PMID: 19552433]
PC-3	IC₅₀	14 nM Compound: 34	Antiproliferative activity against human PC3 cells after 72 to 144 hrs by cyquant DNA dye method Antiproliferative activity against human PC3 cells after 72 to 144 hrs by cyquant DNA dye method	[PMID: 19552433]
SK-MEL-5	IC₅₀	7 nM Compound: 34	Antiproliferative activity against human SK-MEL-5 cells after 72 to 144 hrs by cyquant DNA dye method Antiproliferative activity against human SK-MEL-5 cells after 72 to 144 hrs by cyquant DNA dye method	[PMID: 19552433]
SW-620	IC₅₀	6 nM Compound: 34	Antiproliferative activity against human SW620 cells after 72 to 144 hrs by cyquant DNA dye method Antiproliferative activity against human SW620 cells after 72 to 144 hrs by cyquant DNA dye method	[PMID: 19552433]
Vero	CC₅₀	12.94 μM Compound: SNX-7081	Cytotoxicity against african green monkey Vero cells assessed as inhibition of cell viability after 48 hrs by MTT assay Cytotoxicity against african green monkey Vero cells assessed as inhibition of cell viability after 48 hrs by MTT assay	[PMID: 22704890]
Vero	EC₅₀	1 μM Compound: SNX-7081	Antiviral activity against HSV2 strain 333 infected in african green monkey Vero cells assessed as inhibition of cytopathic effect after 48 hrs by plaque reduction assay Antiviral activity against HSV2 strain 333 infected in african green monkey Vero cells assessed as inhibition of cytopathic effect after 48 hrs by plaque reduction assay	[PMID: 22704890]
Vero	EC₅₀	1.03 μM Compound: SNX-7081	Antiviral activity against HSV1 strain F ATCC VR733 infected in african green monkey Vero cells assessed as inhibition of cytopathic effect after 48 hrs by plaque reduction assay Antiviral activity against HSV1 strain F ATCC VR733 infected in african green monkey Vero cells assessed as inhibition of cytopathic effect after 48 hrs by plaque reduction assay	[PMID: 22704890]

In Vitro

SNX-7081 (0.0001-10 μM; 6-24 h) inhibits the nuclear translocation of NF-κB, with an IC₅₀ value of 114 nM in IL-1β-stimulated human umbilical vein endothelial cells, 241 nM in LPS-stimulated J774 mouse macrophages, 44 nM in IL-1β-stimulated rheumatoid arthritis synovial fibroblasts, and 88 nM in TNF-α-stimulated rheumatoid arthritis synovial fibroblasts^[1].
SNX-7081 (6-24 h) potently suppresses the production of multiple proinflammatory cytokines in THP-1 human monocytes, human umbilical vein endothelial cells, and rheumatoid arthritis synovial fibroblasts, with an IC₅₀ value as low as 13 nM; it also inhibits the proliferation of activated human umbilical vein endothelial cells with an IC₅₀ of 3 nM, while exerting minimal effects on the proliferation of rheumatoid arthritis synovial fibroblasts^[1].
SNX-7081 (0.001-10 μM; 24 h) inhibits growth factor-induced ERK-1/2 signaling pathway in human umbilical vein endothelial cells with an IC₅₀ of 11 nM; inhibits IL-1β-induced JNK signaling pathway in human umbilical vein endothelial cells with an IC₅₀ of 94 nM; inhibits PDGF-induced global tyrosine signaling pathway in NIH3T3 mouse fibroblasts with an IC₅₀ of 56 nM; and also inhibits PDGF-induced ERK-1/2 signaling pathway in NIH3T3 mouse fibroblasts with an IC₅₀ of 14 nM^[1].
SNX-7081 (0.001-10 μM; 6 h) inhibits lipopolysaccharide (LPS)-induced nitric oxide production in J774 murine macrophages, with an IC₅₀ of 6 nM^[1].
SNX-7081 (100 nM; 48 h) induces extensive changes in protein expression in MEC1 cells, including significant downregulation of DNA replication and repair proteins, as well as upregulation of proteins related to energy metabolism and protein metabolism^[2].
SNX-7081 (100 nM; 48 h) alters the levels of key regulatory proteins in MEC1 cells, including decreased expression of NFκB2 p52, MYC and BRCA1^[2].
SNX-7081 (100 nM; 48 h) induces a slight increase in the DNA damage marker γH2AX in p53-mutant MEC1, MEC2 and U266 B-lymphoma cells^[2].
SNX-7081 (100 nM; 48 h) induces extensive changes in protein expression in MEC1 cells, including upregulation of proteins related to DNA damage, epigenetic regulation and pro-apoptosis, as well as downregulation of proteins related to DNA replication and repair^[2].
SNX-7081 (100 nM; 48 h) alters the levels of key regulatory proteins in MEC1 cells, including decreased expression of MYC, CCND1 and BRCA1^[2].
SNX-7081 (100 nM; 48 h) synergistically increases the expression level of the DNA damage marker γH2AX in p53-mutated MEC1, MEC2 and U266 B-lymphocyte cancer cells^[2].
SNX-7081 (72 h) potently inhibits the growth of human cancer cell lines including K562, A375, MCF-7, Hep-2, HepG2, A549, SW-620 and HeLa, with a mean IC₅₀ of approximately 1 μM, while exhibits low cytotoxicity against human normal cell lines L-02, HDF and MRC5^[3].
SNX-7081 (1 μM; 48 h) induces G₂/M cell cycle arrest in K562, Hep-2, A549, SW-620 and HeLa human cancer cells, and exhibits stronger activity than SNX-2112 in K562, Hep-2 and A549 cells^[3].
SNX-7081 (1 μM; 48 h) induces apoptosis in K562, A375, Hep-2, A549, SW-620 and HeLa human cancer cells, and exhibits stronger activity against K562, Hep-2 and A549 cells than SNX-2112^[3].
SNX-7081 (1 μM; 0-48 h) reduces the expression of Hsp90 client proteins IKKα, CHK1, GSK3 and Raf-1 in human leukemia K562 cells in a time-dependent manner, and is more potent than SNX-2112^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[2]

Cell Line:

human p53-negative MEC1 chronic lymphocytic leukemia cells
Concentration:

100 nM
Incubation Time:

48 h
Result:

Significantly decreased NFκB2 p52 levels.
Significantly decreased MYC levels.
Significantly decreased BRCA1 levels.
Induced a non-significant increase in cyclin D1 (CCND1) levels.

Western Blot Analysis^[2]

Cell Line:

human p53-negative MEC1 chronic lymphocytic leukemia cells
Concentration:

100 nM (combined with 10 μM 2-FaraA)
Incubation Time:

48 h
Result:

Significantly decreased MYC levels.
Significantly decreased CCND1 levels.
Significantly decreased BRCA1 levels.

Cell Cycle Analysis^[3]

Cell Line:

K562, Hep-2, A549, SW-620, HeLa
Concentration:

1 μM
Incubation Time:

48 h
Result:

Induced G2/M phase cell cycle arrest in all tested cancer cell lines.
Increased the percentage of cells in G2/M phase to 22.6% (K562), 35.0% (Hep-2), 13.6% (A549), 27.0% (SW-620), and 17.6% (HeLa), compared to control levels of 3.1% (K562), 6.8% (Hep-2), 4.3% (A549), 7.4% (SW-620), and 10.7% (HeLa).
Was more effective at inducing G2/M arrest than SNX-2112 in K562, Hep-2, and A549 cells, but less effective in SW-620 and HeLa cells.

Apoptosis Analysis^[3]

Cell Line:

K562, A375, Hep-2, A549, SW-620, HeLa
Concentration:

1 μM
Incubation Time:

48 h
Result:

Induced apoptosis in all 6 tested cancer cell lines.
Increased the percentage of apoptotic cells to 22.3% (K562), 48.7% (A375), 17.9% (Hep-2), 33.2% (A549), 16.7% (SW-620), and 13.8% (HeLa), compared to control levels of 4.0% (K562), 5.5% (A375), 7.5% (Hep-2), 11.8% (A549), 6.5% (SW-620), and 5.6% (HeLa).
Induced more apoptosis than SNX-2112 in K562, Hep-2, and A549 cells, but less apoptosis in SW-620 and HeLa cells.

Western Blot Analysis^[3]

Cell Line:

K562
Concentration:

1 μM
Incubation Time:

0, 6, 12, 24, 48 h
Result:

Reduced the expression of Hsp90 client proteins (IKKα, CHK1, GSK3, Raf-1) in a time-dependent manner.
Decreased protein levels to 11.7% (IKKα), 21.8% (CHK1), 5.8% (GSK3), and 10.4% (Raf-1) of control levels after 48 h of treatment.
Exerted stronger inhibitory effects on these client proteins than SNX-2112.

Chemical Information

CAS No. 908111-22-8
Molecular Weight 409.53
Formula C₂₄H₃₁N₃O₃
SMILES

CC=1C2=C(N(C1)C3=CC(N[C@@H]4CC[C@@H](O)CC4)=C(C(N)=O)C=C3)CC(C)(C)CC2=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Rice JW, et al. Small molecule inhibitors of Hsp90 potently affect inflammatory disease pathways and exhibit activity in models of rheumatoid arthritis. Arthritis Rheum. 2008;58(12):3765-3775. [Content Brief]

[2]. Kaufman KL, et al. The Hsp90 inhibitor SNX-7081 is synergistic with fludarabine nucleoside via DNA damage and repair mechanisms in human, p53-negative chronic lymphocytic leukemia. Oncotarget. 2015;6(38):40981-40997. [Content Brief]

[3]. Wang X, et al. Comparative effects of SNX-7081 and SNX-2112 on cell cycle, apoptosis and Hsp90 client proteins in human cancer cells. Oncol Rep. 2015;33(1):230-238. [Content Brief]

Calculators

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent:

Product Name:
CAS No.:
Species:
Purity:
Quantity:

SNX-7081

All HSP Isoforms

All NF-κB Isoforms

All ERK Isoforms

All JNK Isoforms

All PDGFR Isoforms

All DNA/RNA Synthesis Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

SNX-7081 Related Classifications

HY-111165 Related Classifications