A selective inhibitor of the USP1-UAF1 deubiquitinase complex activity (IC50 = 76 nM); potentiates cisplatin cytotoxicity in NSCLC H596 cells and U2OS osteosarcoma cells by targeting the TLS and FA DNA damage response pathways

ML-323 – 5 mg

Brand:
Cayman
CAS:
1572414-83-5
Storage:
-20
UN-No:
Non-Hazardous - /

The USP1 deubiquitinating enzyme, which regulates the DNA translesion synthesis (TLS) and Fanconi anemia (FA) DNA damage response pathways by deubiquitinating the central players of these pathways, is activated by the WD40-repeat containing UAF1 protein through formation of a stable USP1-UAF1 protein complex.{30972} ML-323 is an inhibitor of the USP1-UAF1 deubiquitinase complex with an IC50 value of 76 nM.{30973} It demonstrates excellent selectivity against other human deubiquitinases, deSUMOylase, deneddylase, and unrelated proteases.{30973} ML-323 has been shown to inhibit the deubiquitination of proliferating cell nuclear antigen and FA complementation group D2 by inhibiting USP1-UAF1 activity in H596 cells.{30973} ML-323 potentiates cisplatin (Item No. 13119) cytotoxicity in NSCLC H596 cells and U2OS osteosarcoma cells by targeting the TLS and FA DNA damage response pathways.{30973}  

 

Available on backorder

Add to quotes
SKU: - Category:

Description

A selective inhibitor of the USP1-UAF1 deubiquitinase complex activity (IC50 = 76 nM); potentiates cisplatin cytotoxicity in NSCLC H596 cells and U2OS osteosarcoma cells by targeting the TLS and FA DNA damage response pathways

Formal name: 5-methyl-2-[2-(1-methylethyl)phenyl]-N-[[4-(1H-1,2,3-triazol-1-yl)phenyl]methyl]-4-pyrimidinamine

Synonyms: 

Molecular weight: 384.5

CAS: 1572414-83-5

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Ubiquitin Ligase System||Research Area|Cancer|Cell Death||Research Area|Cancer|DNA Damage and Repair||Research Area|Cell Biology|Proteolysis|Ubiquitin/Proteasome System

Related products

  • A potent inhibitor of Cdk2/cyclin E with an IC50 value of 0.1 µM; also inhibits Cdk7/cyclin H

    (R)-Roscovitine – 1 mg

    Cyclin-dependent kinases (CDKs) are key regulators of cell cycle progression and are therefore promising targets for cancer therapy. (R)-Roscovitine is a potent inhibitor of Cdk2/cyclin E with an IC50 value of 0.1 µM.{14988} It also inhibits Cdk7/cyclin H, Cdk5/p35, and cell division cycle (cdc)/cyclin B with IC50 values of 0.49, 0.16, and 0.65 µM, respectively.{14987,14988,14991} (R)-Roscovitine inhibits the growth of rapidly proliferating cells with an average IC50 value of 15.2 µM against a panel of 19 human tumor cell lines.{14988} In murine models of polycystic kidney disease, (R)-roscovitine effectively inhibited disease progression at doses of 50-100 mg/kg.{14564}  

     

    Brand:
    Cayman
    SKU:10009569 - 1 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • A small molecule activator of stem cell renewal that allows the propagation of OG2 mES cells for at least 10 passages in an undifferentiated state; activity is mediated by the combined inhibition of RasGAP and ERK1 with Kd values of 98 and 212 nM

    SC-1 – 25 mg

    The maintenance of embryonic stem cells in culture typically requires feeder cells and various exogenous factors found in serum. Murine embryonic stem (mES) cells can be maintained in the absence of feeder cells and serum but require the leukemia inhibitor factor (LIF) and bone morphogenic protein (BMP) to prevent differentiation and promote self-renewal. SC-1 is a small molecule activator of stem cell renewal that allows the propagation of OG2 mES cells for at least 10 passages in an undifferentiated state.{14533} The activity of SC-1 is mediated by the combined inhibition of RasGAP and ERK1 with Kd values of 98 and 212 nM, respectively.{14533} Inhibition of RasGAP increases Ras signaling via the PI3-kinase pathway which promotes self-renewal, whereas inhibition of ERK blocks differentiation.  

     

    Brand:
    Cayman
    SKU:10009557 - 25 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}

    CAY10512 – 100 mg

    The nuclear factor-κB (NF-κB) regulates the expression of numerous genes involved in immunity and inflammation, cellular stress responses, growth, and apoptosis. Resveratrol, a polyphenolic trans-stilbene, is a known inhibitor of the activation of NF-κB and exhibits activity against a wide variety of cancer cells. CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}  

     

    Brand:
    Cayman
    SKU:10009536 - 100 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • A small molecule activator of stem cell renewal that allows the propagation of OG2 mES cells for at least 10 passages in an undifferentiated state; activity is mediated by the combined inhibition of RasGAP and ERK1 with Kd values of 98 and 212 nM

    SC-1 – 5 mg

    The maintenance of embryonic stem cells in culture typically requires feeder cells and various exogenous factors found in serum. Murine embryonic stem (mES) cells can be maintained in the absence of feeder cells and serum but require the leukemia inhibitor factor (LIF) and bone morphogenic protein (BMP) to prevent differentiation and promote self-renewal. SC-1 is a small molecule activator of stem cell renewal that allows the propagation of OG2 mES cells for at least 10 passages in an undifferentiated state.{14533} The activity of SC-1 is mediated by the combined inhibition of RasGAP and ERK1 with Kd values of 98 and 212 nM, respectively.{14533} Inhibition of RasGAP increases Ras signaling via the PI3-kinase pathway which promotes self-renewal, whereas inhibition of ERK blocks differentiation.  

     

    Brand:
    Cayman
    SKU:10009557 - 5 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page