SML4050
OTUB2-IN-1
≥98% (HPLC)
别名:
(E)-6-(5-(1-(Carboxymethyl)-2-oxoindolin-3-ylidene)-4-oxo-2-thioxothiazolidin-3-yl)hexanoic acid, OTUB2 inhibitor, OTUB2i
InChI key
VQTUGMPRAUNMNP-FOCLMDBBSA-N
SMILES string
O=C(N(C1=C/2C=CC=C1)CC(O)=O)C2=C3C(N(C(S/3)=S)CCCCCC(O)=O)=O
assay
≥98% (HPLC)
form
powder
color
, Light orange to very dark red
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
Quality Level
Biochem/physiol Actions
Inhibits tumor growth by selectively disrupting OTUB2′s activity, thereby reducing PD-L1 levels and enhancing antitumor immunity.
OTUB2-IN-1 selectively targets OTUB2 (OTU deubiquitinase, ubiquitin aldehyde binding 2), a positive regulator of PD-L1, to diminish PD-L1 levels dose-dependently in tumor cells, thereby enhancing antitumor immunity. OTUB2i binds reversibly to OTUB2′s catalytic pocket (KD = 12 µM), selectively impairing its deubiquitinase function without disrupting OTUB2-PD-L1 interactions. OTUB2-IN-1 operates by destabilizing PD-L1 through Lys-48-linked polydeubiquitination leading to a significant reduction in PD-L1-overexpressing tumor growth and enhanced CD8+ CTL-mediated tumor cell elimination, increasing T-cell infiltration in tumors, all achieved without noticeable toxicity. Note: The recommended usage of OTUB2-IN-1 is 10 µM for cellular applications, and for in vivo experiments, it is suggested at 20 mg/kg, administered intraperitoneally (i.p.) in mice. This dosing strategy aims to maximize the inhibitor′s effectiveness in reducing PD-L1 levels in tumor cells while minimizing potential toxicity.
OTUB2-IN-1 selectively targets OTUB2 (OTU deubiquitinase, ubiquitin aldehyde binding 2), a positive regulator of PD-L1, to diminish PD-L1 levels dose-dependently in tumor cells, thereby enhancing antitumor immunity. OTUB2i binds reversibly to OTUB2′s catalytic pocket (KD = 12 µM), selectively impairing its deubiquitinase function without disrupting OTUB2-PD-L1 interactions. OTUB2-IN-1 operates by destabilizing PD-L1 through Lys-48-linked polydeubiquitination leading to a significant reduction in PD-L1-overexpressing tumor growth and enhanced CD8+ CTL-mediated tumor cell elimination, increasing T-cell infiltration in tumors, all achieved without noticeable toxicity. Note: The recommended usage of OTUB2-IN-1 is 10 µM for cellular applications, and for in vivo experiments, it is suggested at 20 mg/kg, administered intraperitoneally (i.p.) in mice. This dosing strategy aims to maximize the inhibitor′s effectiveness in reducing PD-L1 levels in tumor cells while minimizing potential toxicity.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
Pharmaceutical targeting of OTUB2 sensitizes tumors to cytotoxic T cells via degradation of PD-L1
Nature Communications, 15(1), 9-9 (2024)
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