A potent inhibitor of HDAC6 (IC50 = 0.40 nM); selective for HDAC6 over HDAC3 (IC50 = 51.61 nM); induces α-tubulin acetylation

WT161 – 25 mg

Brand:
Cayman
CAS:
1206731-57-8
Storage:
-20
UN-No:
Non-Hazardous - /

WT161 is a potent inhibitor of HDAC6 with an IC50 value of 0.40 nM.{32615} It is selective for HDAC6 over HDAC3 (IC50 = 51.61 nM) and induces α-tubulin acetylation, an HDAC6-dependent process, with minimal effect on global lysine acetylation. WT161 inhibits growth of patient-derived multiple myeloma cell lines with IC50 values ranging from 1.5 to 4.7 μM. WT161 enhances the cytotoxicity of bortezomib (Item No. 10008822) and carfilzomib (Item No. 17554) against patient-derived multiple myeloma cells. It also decreases tumor size in a human MM.1S multiple myeloma mouse xenograft model when administered in combination with bortezomib at doses of 50 and 0.5 mg/kg, respectively.  

 

Out of stock

Add to quotes
SKU: 21099 - Category:

Description

A potent inhibitor of HDAC6 (IC50 = 0.40 nM); selective for HDAC6 over HDAC3 (IC50 = 51.61 nM); induces α-tubulin acetylation, an HDAC6-dependent process, with minimal effect on global lysine acetylation; inhibits growth of patient-derived multiple myeloma cell lines (IC50s = 1.5-4.7 μM); enhances cytotoxicity of bortezomib and carfilzomib against patient-derived multiple myeloma cells; decreases tumor size in a human MM.1S multiple myeloma mouse xenograft model when administered in combination with bortezomib at doses of 50 and 0.5 mg/kg, respectively

Formal name: 8-(hydroxyamino)-8-oxo-octanoic acid, 2-[[4-(diphenylamino)phenyl]methylene]hydrazide

Synonyms: 

Molecular weight: 458.6

CAS: 1206731-57-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Deacetylases||Research Area

Related products

  • A zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers

    1,2-Dipalmitoyl-sn-glycero-3-PC – 50 mg

    1,2-Dipalmitoyl-sn-glycero-3-PC (DPPC) is a zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers, bilayers, and liposomes for use in a variety of applications.{14480,24261,14478,14479} It has been used in the formation of proteoliposomes for implantation of γ-glutamyl transpeptidase into human erythrocyte membranes.{14478} Incorporation of glycosphingolipid antigens into DPPC-containing liposomes increases the immunogenicity of the antigens in mice.{14479}  

     

    Brand:
    Cayman
    SKU:10009473 - 50 mg

    Available on backorder

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

    (R)-Roscovitine – 500 µg

    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 - 500 µg

    Available on backorder

    Add to quotes
    View product page
  • A zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers

    1,2-Dipalmitoyl-sn-glycero-3-PC – 100 mg

    1,2-Dipalmitoyl-sn-glycero-3-PC (DPPC) is a zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers, bilayers, and liposomes for use in a variety of applications.{14480,24261,14478,14479} It has been used in the formation of proteoliposomes for implantation of γ-glutamyl transpeptidase into human erythrocyte membranes.{14478} Incorporation of glycosphingolipid antigens into DPPC-containing liposomes increases the immunogenicity of the antigens in mice.{14479}  

     

    Brand:
    Cayman
    SKU:10009473 - 100 mg

    Available on backorder

    Add to quotes
    View product page