Language:English
Language:

Xcessbio

Place your promotion here

You have no items in your shopping cart.

4SC-202, HDAC/LSD1 Dual Inhibitor

4SC-202, HDAC/LSD1 Dual Inhibitor

$109.00
A potent, selective and orally bioavailable HDAC/LSD1 dual Inhibitor.
Catalog No. Unit Price Qty
M60230-2s 2 mg solid $109.00

Details

Product Information
Molecular Weight: 619.71
Formula: C30H29N5O6S2
Purity: ≥98%
CAS#: 1186222-89-8
Solubility: DMSO up to 50 mM
Chemical Name: (E)-N-(2-aminophenyl)-3-(1-((4-(1-methyl-1H-pyrazol-4-yl)phenyl)sulfonyl)-1H-pyrrol-3-yl)acrylamide tosylic acid
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

Biological Activity:

4SC-202 is a potent, selective and orally bioavailable HDAC/LSD1 dual Inhibitor. It inhibits class I HDAC with IC50 of 1.20 μM, 1.12 μM, and 0.57 μM for HDAC1, HDAC2, and HDAC3, respectively. It also displays inhibitory activity against Lysine specific demethylase 1 (LSD1). 4SC-202 has very high selectivity over ClassIIa/IIb/III HDACs. In HeLa cells, it induces hyperacetylation of histone H3 with EC50 of 1.1 μM. It induces a G2/M cell cycle arrest by interfering with the normal development of the mitotic spindle and causing collapsed spindle apparatus and multiple nucleation centres. In addition, 4SC-202 shows a broad anti-proliferative activity towards human cancer cell lines with a mean IC50 of 0.7 μM. In vivo it shows pronounced and robust anti-tumor activity in both A549 NSCLC xenograft and RKO27 colon carcinoma model. Currently it is in phase I trials for patients with advanced haematological tumours.

How to Use:

In vitro: 4SC-202 was used at 10 µM final concentration in various in vitro assays.
In vivo: 4SC-202 was dosed to A549 NSCLC xenograft model and RKO27 colon carcinoma xenografts model orally at 120 mg/Kg once per day.

Reference:

  • 1. S.W.Henning, et al. Preclinical characterization of 4SC-202, a noval isotype specific HDAC inhibitor.
  • 2. http://www.4sc.de/product-pipeline/clinical/4SC-202


4SC-202_spec.pdf      
4SC-202_MSDS.pdf      

Products are for research use only. Not for human use. 

Description

Details

Product Information
Molecular Weight: 619.71
Formula: C30H29N5O6S2
Purity: ≥98%
CAS#: 1186222-89-8
Solubility: DMSO up to 50 mM
Chemical Name: (E)-N-(2-aminophenyl)-3-(1-((4-(1-methyl-1H-pyrazol-4-yl)phenyl)sulfonyl)-1H-pyrrol-3-yl)acrylamide tosylic acid
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

Biological Activity:

4SC-202 is a potent, selective and orally bioavailable HDAC/LSD1 dual Inhibitor. It inhibits class I HDAC with IC50 of 1.20 μM, 1.12 μM, and 0.57 μM for HDAC1, HDAC2, and HDAC3, respectively. It also displays inhibitory activity against Lysine specific demethylase 1 (LSD1). 4SC-202 has very high selectivity over ClassIIa/IIb/III HDACs. In HeLa cells, it induces hyperacetylation of histone H3 with EC50 of 1.1 μM. It induces a G2/M cell cycle arrest by interfering with the normal development of the mitotic spindle and causing collapsed spindle apparatus and multiple nucleation centres. In addition, 4SC-202 shows a broad anti-proliferative activity towards human cancer cell lines with a mean IC50 of 0.7 μM. In vivo it shows pronounced and robust anti-tumor activity in both A549 NSCLC xenograft and RKO27 colon carcinoma model. Currently it is in phase I trials for patients with advanced haematological tumours.

How to Use:

In vitro: 4SC-202 was used at 10 µM final concentration in various in vitro assays.
In vivo: 4SC-202 was dosed to A549 NSCLC xenograft model and RKO27 colon carcinoma xenografts model orally at 120 mg/Kg once per day.

Reference:

  • 1. S.W.Henning, et al. Preclinical characterization of 4SC-202, a noval isotype specific HDAC inhibitor.
  • 2. http://www.4sc.de/product-pipeline/clinical/4SC-202


4SC-202_spec.pdf      
4SC-202_MSDS.pdf      

Products are for research use only. Not for human use. 

Reviews

Write Your Review

How do you rate this product? *

Price:
Value:
Quality: