[CAS NO. 500579-04-4] GANT61

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PRODUCTS SPECIFICATIONS [500579-04-4]

Catalog

SLK-S8075

Brand

Selleck

CAS

500579-04-4

DESCRIPTION [500579-04-4]

Overview

MDL	MFCD14635408
Molecular Weight	429.6
Molecular Formula	C27H35N5
SMILES	C(N1C(N(CC2=C(N(C)C)C=CC=C2)CCC1)C=3C=CN=CC3)C4=C(N(C)C)C=CC=C4

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Description

GANT61 (NSC 136476) is an inhibitor for as well as GLI2-induced transcription, inhibits with of 5 μM in GLI1 expressing HEK293T cell, displays selectivity over other pathways, such as TNF and glucocorticoid receptor gene transactivation. GANT61 induces and activates protective in LX-2 cells.

Targets

GLI1 ^[1]
(HEK293T cells expressing GLI1)

5 μM

In vitro

GANT61 is an inhibitor for GLI1 as well as GLI2-induced transcription. GANT61 inhibits the DNA binding ability of GLI1. GANT61 inhibits hedgehog signaling with IC50 of 5 μM, displays selectivity over other pathways, such as TNF signaling/NFκB activation, glucocorticoid receptor gene transactivation, and the Ras–Raf–Mek–Mapk cascade. GANT61 efficiently inhibited in vitro tumor cell proliferation in a GLI-dependent manner. GANT61 induces apoptosis in chronic lymphocytic leukemia cells (CLL), but not in normal B lymphocytes. GANT61 induces robust cytotoxicity and abolishs the clonogenicity in human colon carcinoma cell lines. GANT61 induces inhibition of DNA replication in early S-phase in human colon carcinoma cell lines, leading to DNA damage signaling involving an ATM–Chk2 axis and induction of cell death. GANT61 (30 μM) causes growth arrest and apoptosis in acute myeloid leukemia (AML) cells.

In vivo

In nude mice injected with GLI1-positive 22Rv1 prostate cancer cells, GANT61 induces growth regression until no tumor is palpable. In nude mice carrying SK-N-AS neuroblastoma xenografts, GANT61 treatment (oral gavage, 50 mg/kg) significantly inhibits tumor growth at Day 12 , as the tumor volume is reduced to 63% compared with controls.

References

[1] Lauth M, et al. Proc Natl Acad Sci, 2007, 104(20), 8455-8560
[2] Desch P, et al. Oncogene, 2010, 29(35), 4885-4895.
[3] Mazumdar Y, et al. Cancer Res, 2011, 71(3), 1092-1102.
[4] Mazumdar T, et al. Cancer Res, 2011,71(17), 5904-5914.
[5] Pan D, et al. Leuk Res, 2012, 36(6), 742-748.
[6] Wickstorm M, et al. Int J Cancer, 2013, 132(7), 1516-1524.

Synonyms

Benzenamine, 2,2′-[[dihydro-2-(4-pyridinyl)-1,3(2H,4H)-pyrimidinediyl]bis(methylene)]bis[N,N-dimethyl-

2,2′-[[Dihydro-2-(4-pyridinyl)-1,3(2H,4H)-pyrimidinediyl]bis(methylene)]bis[N,N-dimethylbenzenamine]

NSC 136476

GANT 61

2-[[3-[[2-(Dimethylamino)phenyl]methyl]-2-pyridin-4-yl-1,3-diazinan-1-yl]methyl]-N,N-dimethylaniline