An irreversible

Tranylcypromine (hydrochloride) – 250 mg

Brand:
Cayman
CAS:
1986-47-6
Storage:
-20
UN-No:
Non-Hazardous - /

Tranylcypromine is an irreversible, mechanism-based inhibitor of lysine-specific demethylase 1 (LSD1; IC50 = 20.7 µM in a cell-free assay).{15036} It also irreversibly inhibits monoamine oxidase A (MAO-A) and MAO-B with IC50 values of 2.3 and 0.95 µM, respectively. Tranylcypromine inhibits nucleosomal demethylation of histone H3 lysine 4 (H3K4; IC50 = 13122) to promote the differentiation of keratinocytes into induced pluripotent stem cells (iPSCs) when transduced with the transcription factors Oct4 and Klf4.{49327} It also decreases proliferation of neural progenitors in the hippocampal dentate gyrus in adult mice when administered at a dose of 10 mg/kg for ten days.{49328} Tranylcypromine (0.5-10 mg/kg) decreases the time juvenile rats spend immobile in the forced swim test, indicating antidepressant-liked activity.{49329} Formulations containing tranylcypromine have been used in the treatment of treatment-resistant major depressive disorder.  

 

Available on backorder

Add to quotes
SKU: 10010494 - 250 mg Category:

Description

An irreversible, mechanism-based inhibitor of LSD1 (IC50 = 20.7 µM); irreversibly inhibits MAO-A and MAO-B (IC50s = 2.3 and 0.95 µM, respectively); PCPA inhibits nucleosomal demethylation of H3K4 (IC50 = <2 µM); induces EpiSCs to convert to more undifferentiated state but requires inhibitors of ALK5, MEK, FGFR, and GSK3 for full conversion to pluripotent mESCs; decreases proliferation of neural progenitors in the hippocampal dentate gyrus in adult mice at 10 mg/kg for ten days; decreases the time juvenile rats spend immobile in the forced swim test at 0.4-10 mg/kg

Formal name: (1R,2S)-rel-2-phenyl-cyclopropanamine, monohydrochloride

Synonyms:  trans-2-Phenylcyclopropylamine|2-PCPA

Molecular weight: 169.7

CAS: 1986-47-6

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Demethylases||Research Area|Cell Biology|Stem Cell Research|Differentiation||Research Area|Epigenetics, Transcription, & Translation|Erasers|Histone Demethylation||Research Area|Neuroscience|Behavioral Neuroscience|Depression

Related products

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

    (R)-Roscovitine – 5 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 - 5 mg

    Available on backorder

    Add to quotes
    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 – 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
  • PtdIns-(3

    PtdIns-(3,4,5)-P3-biotin (sodium salt) – 100 µg

    The PtdIn phosphates play an important role in the generation and transduction of intracellular signals.{8344,4096,14518} PtdIns-(3,4,5)-P3-biotin is an affinity probe which allows the PIP3 to be detected through an interaction with the biotin ligand. This design allows PtdIns-(3,4,5)-P3-biotin to serve as a general probe for any protein with a high affinity binding interaction with inositol-(3,4,5)-triphosphate phospholipids, such as phosphatidylinositol 3-kinase, PTEN, or PH-domain-containing proteins.  

     

    Brand:
    Cayman
    SKU:10009531 - 100 µg

    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 – 10 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 - 10 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page