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E1286

Eeyarestatin I

synthetic (organic), ≥98% (HPLC), ERAD inhibitor, powder

Synonym(s):

3-(4-Chlorophenyl)-4-[[[(4-chlorophenyl)amino]carbonyl]hydroxyamino]-5,5-dimethyl-2-oxo-1-imidazolidineacetic acid 2-[3-(5-nitro-2-furanyl)-2-propen-1-ylidene]hydrazide

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Pack SizeSKUAvailabilityPrice
10 mg
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CZK 8,100.00
CZK 6,885.00

About This Item

Empirical Formula (Hill Notation):
C27H25Cl2N7O7
CAS Number:
412960-54-4
Molecular Weight:
630.44
MDL number:
MFCD00319108
UNSPSC Code:
12352204
NACRES:
NA.77

CZK 6,885.00

List PriceCZK 8,100.00Save 15%
Please contact Customer Service for Availability
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Product Name

Eeyarestatin I, ≥98% (HPLC)

biological source

synthetic (organic)

Quality Level

200

assay

≥98% (HPLC)

form

powder

storage condition

desiccated

solubility

DMSO: 5 mg/mL

storage temp.

2-8°C

SMILES string

Clc1ccc(cc1)N2C(C(N(C2=O)CC(=O)NN=CC=Cc4[o]c(cc4)[N+](=O)[O-])(C)C)N(O)C(=O)Nc3ccc(cc3)Cl

InChI

1S/C27H25Cl2N7O7/c1-27(2)24(35(40)25(38)31-19-9-5-17(28)6-10-19)34(20-11-7-18(29)8-12-20)26(39)33(27)16-22(37)32-30-15-3-4-21-13-14-23(43-21)36(41)42/h3-15,24,40H,16H2,1-2H3,(H,31,38)(H,32,37)

InChI key

JTUXTPWYZXWOIB-UHFFFAOYSA-N

Biochem/physiol Actions

Eeyarestatin I is a potent inhibitor of endoplasmic reticulum associated protein degradation (ERAD). Specifically targets the p97-associated deubiquinating process (PAD) and inhibits ataxin-3 (atx3)-dependent deubiquitination.
Eeyarestatin I is a potent inhibitor of endoplasmic reticulum associated protein degradation (ERAD). Specifically targets the p97-associated deubiquinating process (PAD) and inhibits ataxin-3 (atx3)-dependent deubiquitination. Also inhibits Sec61-mediated protein translocation at the ER. Displays cytotoxic activity preferentially against cancer cells; induces cell death via the proapoptotic protein NOXA.
Eeyarestatin I or Eer1 promotes transcriptional activation of the pro-apoptotic protein NOXA by inducing activation of the NOXA transcription factors ATF3 and ATF4 and by inhibiting the degradation of histone H2A by blocking its ubiquitination. [1]

Other Notes

This product is a mixture of E/Z imine isomers

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This Item
SML3644SML2993SML3503
Eeyarestatin I ≥98% (HPLC)

Sigma-Aldrich

E1286

Eeyarestatin I

JR-AB2-011 ≥98% (HPLC)

Sigma-Aldrich

SML3644

JR-AB2-011

JH-RE-06 ≥98% (HPLC)

Sigma-Aldrich

SML2993

JH-RE-06

EN523 ≥98% (HPLC)

Sigma-Aldrich

SML3503

EN523

assay

≥98% (HPLC)

assay

≥98% (HPLC)

assay

≥98% (HPLC)

assay

≥98% (HPLC)

biological source

synthetic (organic)

biological source

-

biological source

-

biological source

-

Quality Level

200

Quality Level

100

Quality Level

100

Quality Level

100

form

powder

form

powder

form

powder

form

powder

solubility

DMSO: 5 mg/mL

solubility

DMSO: 2 mg/mL, clear (Warmed)

solubility

DMSO: 2 mg/mL, clear

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

2-8°C

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Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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Certificates of Analysis (COA)

Lot/Batch Number
0000297727
0000297727
0000292790
0000286717
0000289575

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Qiuyan Wang et al.
Proceedings of the National Academy of Sciences of the United States of America, 106(7), 2200-2205 (2009-01-24)
The ubiquitin-proteasome system has recently emerged as a major target for drug development in cancer therapy. The proteasome inhibitor bortezomib has clinical activity in multiple myeloma and mantle cell lymphoma. Here we report that Eeyarestatin I (EerI), a chemical inhibitor
Jose Lora et al.
The Journal of biological chemistry, 296, 100733-100733 (2021-05-07)
A disintegrin and metalloprotease 17 (ADAM17) is a cell-surface metalloprotease that serves as the principle sheddase for tumor necrosis factor α (TNFα), interleukin-6 receptor (IL-6R), and several ligands of the epidermal growth factor receptor (EGFR), regulating these crucial signaling pathways.
Avantika Gupta et al.
eLife, 9 (2020-06-12)
The transcription factor FoxO has been shown to block proliferation and progression in mTORC1-driven tumorigenesis but the picture of the relevant FoxO target genes remains incomplete. Here, we employed RNA-seq profiling on single clones isolated using laser capture microdissection from
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Global Trade Item Number

SKUGTIN
E1286-10MG04061833234358

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