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BiochemicalTargets

Ubiquitin/Proteasome

The ubiquitin-proteasome system (UPS) is a major intracellular protein degradation system in eukaryotes. Damaged, misfolded, or superfluous proteins are labeled with multiple ubiquitin molecules (a 76 amino acid peptide) via the sequential action of E1 activating enzyme, E2 conjugating enzyme, and E3 ligase ultimately leading to destruction of the protein by the 26S proteasome. Deubiquitinases cleave the bond between ubiquitin and protein. Dysregulation of the UPS and/or DUBs is implicated in many neurological disorders, cancer, atherosclerosis and other pathological states.

DUBS

OTUDin3 | OTUD3 inhibitor

OTUDin3 (441290-65-9) is a potent inhibitor of the deubiquitinase OTUD3, a member of the ovarian tumor proteases which plays a key role in tumorigenesis, neurodegeneration, metabolism,

iBAP-II | BAP1 inhibitor

CAS:
1013813-81-4
Catalog Number:
10-4038
Activity:
BAP1 inhibitor
Chemical Names:
4-(8-Nitro-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-4-yl)phenol
Molecular Weight:
308.33
Molecular Formula:
C18H16N2O3
Solubility:
Soluble in DMSO (25 mg/ml)
Physical Properties:
Yellow solid
Purity:
>98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

P22077 | Selective USP7 inhibitor

CAS:
1247819-59-5
Catalog Number:
10-4125
Activity:
Selective USP7 inhibitor
Chemical Name:
1-(5-((2,4-Difluorophenyl)thio)-4-nitrothiophen-2-yl)ethanone
Molecular Weight:
315.32
Molecular Formula:
C12H7F2NO3S2
Solubility:
Soluble in DMSO (up to 25 mg/ml)
Physical Properties:
Off-white solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

E3 Ubiquitin ligases

Indisulam | RBM39 Molecular glue

Indisulam (165668-41-7) was originally described as a potent antitumor agent that targeted the G1 phase of cell cycle via suppression of activation of CDK2 and cyclin

Other ligases

TRIM-473 | RING ligase TRIM58 ligand

TRIM-473 is a ligand (EC50 = 5.3 µM) for the PRY-SPRY domain of the RING ligase TRIM58.  An interesting new tool for the development of heterobifunctional

Proteasome

Z-Leu-Leu-Leu-vinylsulfone | Proteasome inhibitor

Z-Leu-Leu-Leu-vinylsulfone (193482-47-2) blocks the trypsin-like, chymotrypsin-like, and peptidylglutamyl peptidase activity in isolated proteasomes and in living cells via covalent modification of active site threonine residues.1,2 References/Citations: Bogyo et al.

Gliotoxin | Immunomodulator

CAS:
67-99-2
Catalog Number:
10-2076
Activity:
Immunomodulator
Chemical Names:

(3R,5aS,6S,10aR)-2,3,5a,6-Tetrahydro-6-hydroxy-3-(hydroxymethyl)-2-methyl-10H-3,10a-epidithiopyrazino
[1,2-a]indole-1,4-dione; Aspergillin

Molecular Weight:
326.39
Molecular Formula:
C13H14N2O4S2
Solubility:
Soluble in DMSO (up to 15 mg/ml)
Physical Properties:
White lyophilized solid
Purity:
98%  HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 yeara as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.
Shipping Code:
RT

ML241 | p97 AAA ATPase inhibitor

CAS:
1346528-06-0
Catalog Number:
10-1555
Activity:
p97 AAA ATPase inhibitor
Chemical Name:
N-Benzyl-2-(2,3-dihydro-1,4-benzoxazin-4-yl)-5,6,7,8-tetrahydroquinazolin-4-amine
Alternate Name:
CID49830260
Molecular Weight:
372.46
Molecular Formula:
C23H24N4O
Solubility:
Soluble in DMSO (up to 50 mg/ml) or in Ethanol (up to 14 mg/ml with warming).
Physical Properties:
Pale yellow solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months.
Shipping Code:
RT

Ubiquitin-like modifiers

NAcM-OPT | NEDD8 ligation inhibitor

CAS:
2089293-61-6
Catalog Number:
10-1636
Activity:
NEDD8 ligation inhibitor
Chemical Name:
1-Benzyl-1-(1-butylpiperidin-4-yl)-3-(3,4-dichlorophenyl)urea
Molecular Weight:
434.40
Molecular Formula:
C23H29Cl2N3O
Solubility:
Soluble in DMSO (up to 30 mg/ml) or in Ethanol (up to 20 mg/ml)
Physical Properties:
White solid
Purity:
98% by HPLC/TLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year as from date of purchase supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
Shipping Code:
RT

MLN4924 | NEDD8 activating enzyme inhibitor

CAS:
905579-51-3
Catalog Number:
10-1311
Activity:
NEDD8 activating enzyme inhibitor
Chemical Name:
((1S,2S,4R)-4-(4-(((S)-2,3-Dihydro-1H-inden-1-yl)amino)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-2-hydroxycyclopentyl)methyl sulfamate; Pevonedistat
Molecular Weight:
443.53
Molecular Formula:
C21H25N5O4S
Solubility:
Soluble in DMSO (up to 10 mg/ml).
Physical Properties:
White solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°C (des.)
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.
Shipping Code:
RT

Ubiquitin activating enzyme

Pyr41 | E1 UAE inhibitor

CAS:
418805-02-4
Catalog Number:
10-1304
Activity:
E1 UAE inhibitor
Chemical Name:
4-[4-(5-Nitro-furan-2-ylmethylene)-3,5-dioxo-pyrazolidin-1-yl]-benzoic acid ethyl ester
Molecular Weight:
371.31
Molecular Formula:
C17H13N3O7
Solubility:
Soluble in DMSO (up to 25 mg/ml).
Physical Properties:
Brown solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°C (des.)
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 1 week.
Shipping Code:
RT

Other

M22 | NEDD8 activating enzyme inhibitor

Protein neddylation is a post-translational modification which transfers the ubiquitin-like protein NEDD8 to a lysine residue of the target substrate through a three-step enzymatic cascade and

NSC697923 | E2 ubiquitin-conjugating enzyme inhibitor

CAS:
343351-67-7
Catalog Number:
10-1418
Activity:
Ubiquitin E2 conjugating enzyme inhibitor
Chemical Name:
2-[(Methylphenyl)sulfonyl]-5-nitrofuran
Molecular Weight:
267.26
Molecular Formula:
C11H9NO5S
Solubility:
Soluble in DMSO (up to 25 mg/ml) or in Ethanol (up to 5 mg/ml with warming)
Physical Properties:
Pink solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 1 month.
Shipping Code:
RT