PYR 41
Synonym(s):4[4-(5-Nitro-furan-2-ylmethylene)-3,5-dioxo-pyrazolidin-1-yl]-benzoic acid ethyl ester
- CAS NO.:418805-02-4
- Empirical Formula: C17H13N3O7
- Molecular Weight: 371.3
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-10-31 18:15:48
What is PYR 41?
Description
Pyr41 (418805-02-4) inhibits ubiquitin activating enzyme E1 (>60% inhibition at 10 μM) with little or no activity against E2 or E3. Cell permeable
The Uses of PYR 41
PYR 41 is an irreversible and cell-permeable UBE1 inhibitor.
What are the applications of Application
Ubiquitin E1 Inhibitor, PYR-41 is a cell-permeable pyrazone that irreversibly inhibits ubiquitin-activating enzyme E1 activity
What are the applications of Application
PYR 41 is an irreversible and cell-permeable ubiquitin-activating enzyme (E1) inhibitor
Definition
ChEBI: PYR-41 is an ethyl ester resulting from the formal condensation of the carboxy group of 4-{4-[(5-nitrofuran-2-yl)methylidene]-3,5-dioxopyrazolidin-1-yl}benzoic acid with ethanol. It is an irreversible and cell-permeable inhibitor of ubiquitin-activating enzyme E1. It has a role as an EC 6.2.1.45 (E1 ubiquitin-activating enzyme) inhibitor and an antineoplastic agent. It is an ethyl ester, a member of furans, a C-nitro compound, a member of pyrazolidines and a benzoate ester.
Biochem/physiol Actions
PYR-41 is a cell permeable inhibitor of Ubiquitin activating enzyme (E1) with little or no activity against E3, E2, or caspase enzymatic activity.
in vitro
in addition to blocking ubiquitylation, pyr-41 was found to increase total sumoylation in cells. pyr-41 could attenuate cytokine-mediated nuclear factor-kbactivation. this correlated with inhibition of nonproteasomal ubiquitylation of traf6, which is important to ikbkinase activation. pyr-41 also prevented the downstream ubiquitylation and proteasomal degradation of ikba. moreover, pyr-41 has demonstrated effective uae e1 inhibition as well as some off-target inhibition of the other ubiquitin regulatory enzymes and signal-transducing proteins, suggesting it is a nonspecific inhibitor [1].
storage
Store at -20°C
References
1) Yang et al. (2007), Inhibitors of Ubiquitin-Activating Enzyme (E1), a New Class of Potential Cancer Therapeutics; Cancer Res., 67 9472 2) Mi et al. (2009), Cancer Preventive isothiocyanates induce selective degradation of cellular alpha- and beta-tubulins by proteasomes; J. Biol. Chem., 284 17039 3) Maehama et al. (2014), Nucleolar Stress Induces Ubiquitination-independent Proteasomal Degradation of PICT1 Protein PYR41; J. Biol. Chem., 289 20802 [Focus Citation]
Properties of PYR 41
Melting point: | 228 - 235°C |
Density | 1.486±0.06 g/cm3(Predicted) |
storage temp. | -20°C |
solubility | Soluble in DMSO at 5mg/ml with warming |
form | powder |
pka | 7.43±0.20(Predicted) |
color | red to brown |
Sensitive | Light Sensitive |
Stability: | Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 1 week. |
Safety information for PYR 41
Signal word | Warning |
Pictogram(s) |
Exclamation Mark Irritant GHS07 |
GHS Hazard Statements |
H302:Acute toxicity,oral H317:Sensitisation, Skin |
Precautionary Statement Codes |
P280:Wear protective gloves/protective clothing/eye protection/face protection. P302+P352:IF ON SKIN: wash with plenty of soap and water. |
Computed Descriptors for PYR 41
InChIKey | ARGIPZKQJGFSGQ-LCYFTJDESA-N |
New Products
Bromine 99.5% AR (4 x 500ml) Fehling's Solution No. B Amino Acid Kit of 23 items set Ammonium Molybdate Reagent Solution Beam's Reagent Solution Ehrlich's Reagent For detection of urobillinogen 4-((2-isopropoxyethoxy)methyl)phenol 4-Hydroxy Carbazole Amino Salicylic Acid. U.S.P. 2 – Methoxy – 5- Sulfamoyl Benzoic acid 1,2,3,4-Tetrahydrocarbazol-4-one Acetone Isobutryl oxime ester Curcuma aromatica Oil Curry leaf Extract Terminalia bellirica Extract Aloe vera extract 200x Withania somnifera (Ashwagandha Extract) Citrus bioflavonoids Extract Ethyl 3-(Pyridin-2-Ylamino)Propanoate Bilastine -IP/BP/ Cypermethric Acid Chloride Methyl Di Chloride (Mdc) 5-Nitrosalicylaldehyde 5-(Difluoromethoxy)-2-Mercapto-1H-Benzimidazole- IP/BP/Related products of tetrahydrofuran
You may like
-
Thermo Scientific Chemicals Ubiquitin E1 Inhibitor CAS 418805-02-4View Details
418805-02-4 -
PYR-41 CAS 418805-02-4View Details
418805-02-4 -
7726-95-6 Bromine 99.5% AR (4 x 500ml) 99%View Details
7726-95-6 -
Formamide 99%View Details
75-12-7 -
2, 4-Pyrimidinediamine 3-Oxide 99%View Details
74638-76-9 -
85-81-4 6-Methoxy-8-Nitroquinoline 99%View Details
85-81-4 -
3-Bromo-4,5-Dihydro-1H-Benzo[B]Azepin-2(3H)-One 99%View Details
86499-96-9 -
(−)-Dip-Chloride 85116-37-6 99%View Details
85116-37-6