GANT61 (Synonyms: NSC 136476)

Name: GANT61
Brand: GlpBio
SKU: GC10359
Availability: InStock
Rating: 5 (18 reviews)

カタログ番号GC10359

GANT61は、GLI1およびGLI2による転写を効率的に阻害することができました。IC50は5µMです。

Products are for research use only. Not for human use. We do not sell to patients.

GANT61 化学構造

Cas No.: 500579-04-4

サイズ

価格

在庫数

個数

10mM (in 1mL EtOH)	$53.00	在庫あり
5mg	$38.00	在庫あり
25mg	$115.00	在庫あり
100mg	$338.00	在庫あり

Tel：(909) 407-4943 Email: sales@glpbio.com

顧客レビュー

カスタマーレビューに基づきます。

Sample solution is provided at 25 µL, 10mM.

評判の良い論文で引用されたGlpBio製品

Nature
610.7931 (2022): 366-372

Nature
618, 1017–1023 (2023)

Cell
183.7 (2020): 1867-1883

Cell Research
31, 1291–1307 (2021)

Cell Research
33, 273–287 (2023)

Cell Research
33, 546–561 (2023)

Molecular Cancer
21.1 (2022): 1-17

Molecular Cancer
21.1 (2022): 1-18

Cancer Cell
39 (2021): 1-16

Cell Host Microbe
30.8 (2022): 1124-1138

Cell Host Microbe
31.5 (2023): 766-780

Cell Host Microbe
31.3 (2023): 418-43

Cell Metabolism
34.2 (2022): 240-255

Ann Rheum Dis
82(4): 533-545 (2023)

Cell Mol Immunol
20, 264–276 (2023)

Adv Funct Mater
33.35 (2023): 2214998

Description Protocol Chemical Properties Product Documents

Product Documents

Quality Control & SDS

View current batch:

Purity: >98.00%

Protocol

Compound Screen [1]:
Preparation Method	HEK293 cells were transfected with GLI1 expression plasmid, together with the reporter plasmids 12xGliBS-Luc and R-Luc on 10-cm plates (day 0). Twenty-four hours later, cells were seeded in white 96-well plates with clear bottom at a density of 15,000 cells per well. Cells were allowed to attach, and compounds (1990 compounds) were added at a final concentration of 10 μM in DMSO (0.5% final DMSO concentration) (day 1.5). Cells were grown for another 24 h, subsequently lysed, and then analyzed by using the Dual Luciferase kit. Plates were read on a Berthold Technologies microplate luminometer.
Applications	GANT61 was able to efficiently block GLI1 as well as GLI2-induced transcription, IC50 is 5 μM.
Cell experiment [1]:
Cell lines	PANC1 and 22Rv1 cells
Preparation Method	PANC1 and 22Rv1 cells were treated with 5 μM GANT61 for 48 h.
Reaction Conditions	5 μM GANT61; 48 h
Applications	Incubation of PANC1 or 22Rv1 cells with 5 μM GANT61 for 48 h led to a reduction in GLI1 and PTCH expression.
Animal experiment [1]:
Animal models	Female BALB/c nude mice (nu/nu).
Preparation Method	22Rv1 cells suspension was injected s.c. at the posterior flank of female BALB/c nude mice (nu/nu). Animals were randomly divided into four groups (n = 4 5) and treated with solvent only (corn oil:ethanol, 4:1) or GANT61 (50 mg/kg) for 16 days. s.c. injections of compounds were performed several centimeters away from the tumor.
Dosage form	50 mg/kg GANT61;16 days . (s.c. injections of compounds were performed several centimeters away from the tumor.)
Applications	GANT61 induced growth regression until no tumor was palpable.
References: [1]. Lauth M, Bergström A, et,al.Inhibition of GLI-mediated transcription and tumor cell growth by small-molecule antagonists. Proc Natl Acad Sci U S A. 2007 May 15;104(20):8455-60. doi: 10.1073/pnas.0609699104. Epub 2007 May 9. PMID: 17494766; PMCID: PMC1866313.

GANT61 was able to efficiently block GLI1 as well as GLI2-induced transcription, IC50 is 5 µM^[1].

Incubated with GANT61 (5 µM ;48 h) in PANC1 or 22Rv1 cells, the expression of GLI1 and PTCH was decreased^[1]. In the Hh-responsive murine cell line C3H/10T1/2cell line, GANT61 (5/10µM ;48 h) dose-dependently suppressed endogenous Glil transcriptional upregulation induced by SHH treatment ^[2]. GANT61 treatment (20µM ;36h) abolished the clonogenicity of all six human colon carcinoma cell lines. Analysis of the molecular mechanisms of GANT61-induced cytotoxicity in HT29 cells showed increased Fas expression and decreased expression of PDGFRα^[3]. GANT61 induced transient cellular accumulation at G(1)-S (24 hours) and in early S-phase (32 hours), with elevated p21(Cip1), cyclin E, and cyclin A in HT29 cells. GANT61 induced DNA damage within 24 hours, with the appearance of p-ATM and p-Chk2^[4]. GANT61 induces cell death of SK-N-LO cells in a caspase-independent manner, by inhibiting DNA replication in the S phase^[7]. GANT61 caused growth arrest and apoptosis in AML cells. Synergism effect between GANT61 and rapamycin was found in Kasumi-1, HL-60 and U937 cell lines^[5].

GANT61(50 mg/kg; s.c.;16 days) induced tumor growth regression until no tumor was palpable in Human prostate cancer xenograft^[1].GANT61(50 mg/kg; i.g. 12 days) enhanced the effects of chemotherapeutic drugs used in the treatment of neuroblastoma in an additive or synergistic manner and reduced the growth of established neuroblastoma xenografts in nude mice^[6].

References:
[1]. Lauth M, BergstrÖm A,et,al. Inhibition of GLI-mediated transcription and tumor cell growth by small-molecule antagonists. Proc Natl Acad Sci U S A. 2007 May 15;104(20):8455-60. doi: 10.1073/pnas.0609699104. Epub 2007 May 9. PMID: 17494766; PMCID: PMC1866313.
[2]. Desch P, Asslaber D et,al.Inhibition of GLI, but not Smoothened, induces apoptosis in chronic lymphocytic leukemia cells. Oncogene. 2010 Sep 2;29(35):4885-95. doi: 10.1038/onc.2010.243. Epub 2010 Jul 5. PMID: 20603613.
[3]. Mazumdar T, DeVecchio J, et,al.Hedgehog signaling drives cellular survival in human colon carcinoma cells. Cancer Res. 2011 Feb 1;71(3):1092-102. doi: 10.1158/0008-5472.CAN-10-2315. Epub 2010 Dec 6. PMID: 21135115; PMCID: PMC3032813.
[4]. Mazumdar T, Devecchio J, et,al. Blocking Hedgehog survival signaling at the level of the GLI genes induces DNA damage and extensive cell death in human colon carcinoma cells. Cancer Res. 2011 Sep 1;71(17):5904-14. doi: 10.1158/0008-5472.CAN-10-4173. Epub 2011 Jul 11. PMID: 21747117; PMCID: PMC3165104.
[5]. Pan D, Li Y et,al. Gli inhibitor GANT61 causes apoptosis in myeloid leukemia cells and acts in synergy with rapamycin. Leuk Res. 2012 Jun;36(6):742-8. doi: 10.1016/j.leukres.2012.02.012. Epub 2012 Mar 6. PMID: 22398221.
[6]. WickstrÖm M, Dyberg C, et,al.Targeting the hedgehog signal transduction pathway at the level of GLI inhibits neuroblastoma cell growth in vitro and in vivo. Int J Cancer. 2013 Apr 1;132(7):1516-24. doi: 10.1002/ijc.27820. Epub 2012 Oct 3. PMID: 22949014.
[7]. Matsumoto T, Tabata K, et,al.The GANT61, a GLI inhibitor, induces caspase-independent apoptosis of SK-N-LO cells. Biol Pharm Bull. 2014;37(4):633-41. doi: 10.1248/bpb.b13-00920. PMID: 24694609.

Cas No.	500579-04-4	SDF
同義語	NSC 136476
Chemical Name	2-[[3-[[2-(dimethylamino)phenyl]methyl]-2-pyridin-4-yl-1,3-diazinan-1-yl]methyl]-N,N-dimethylaniline
Canonical SMILES	CN(C)C1=CC=CC=C1CN2CCCN(C2C3=CC=NC=C3)CC4=CC=CC=C4N(C)C
Formula	C₂₇H₃₅N₅	M.Wt	429.6
溶解度	≥ 9.95mg/mL in Ethanol	Storage	Store at -20°C
General tips	Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition	Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
		1 mg	5 mg	10 mg
	1 mM	2.3277 mL	11.6387 mL	23.2775 mL
	5 mM	0.4655 mL	2.3277 mL	4.6555 mL
	10 mM	0.2328 mL	1.1639 mL	2.3277 mL

モルアリティ計算機
希釈計算機

計算

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

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Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 18 reference(s) in Google Scholar.)

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GANT61 (Synonyms: NSC 136476)

顧客レビュー

GlpBio Citations

Bioactive Compounds Premium Provider

評判の良い論文で引用されたGlpBio製品

Product Documents

Quality Control & SDS

Protocol

Complete Stock Solution Preparation Table

モルアリティ計算機

希釈計算機

In vivo Formulation Calculator (Clear solution)

レビュー

GANT61 (Synonyms: NSC 136476)

顧客レビュー

GlpBio Citations

Bioactive Compounds Premium Provider

評判の良い論文で引用されたGlpBio製品

Product Documents

Quality Control & SDS

Protocol

Complete Stock Solution Preparation Table

モルアリティ計算機

希釈計算機

In vivo Formulation Calculator (Clear solution)

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