R162 | CAS# 64302-87-0 | GDH activity inhibitor

MedKoo Cat#: 561746 | Name: R162

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

R162 is an inhibitor of GDH activity and represses glioma cell growth.

Chemical Structure

R162

CAS#64302-87-0

Theoretical Analysis

MedKoo Cat#: 561746

Name: R162

CAS#: 64302-87-0

Chemical Formula: C17H12O3

Exact Mass: 264.0786

Molecular Weight: 264.28

Elemental Analysis: C, 77.26; H, 4.58; O, 18.16

Price and Availability

Size	Price	Availability
10mg	USD 265.00	2 weeks
25mg	USD 480.00	2 weeks
50mg	USD 850.00	2 Weeks

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Related CAS #

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Synonym

R162; R 162; R-162;

IUPAC/Chemical Name

2-Allyl-1-hydroxy-anthraquinone

InChi Key

IMUBGIOLZQTIGI-UHFFFAOYSA-N

InChi Code

InChI=1S/C17H12O3/c1-2-5-10-8-9-13-14(15(10)18)17(20)12-7-4-3-6-11(12)16(13)19/h2-4,6-9,18H,1,5H2

SMILES Code

O=C(C1=C2C=CC=C1)C3=CC=C(CC=C)C(O)=C3C2=O

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

R162 is an inhibitor of GDH1 (IC50 = 23 µM).1 It decreases intracellular fumarate levels and increases the production of mitochondrial ROS in human H1299 lung and MDA-MB-231 breast cancer cells. R162 inhibits proliferation in several human cancer cell lines, including lung, breast, and leukemia cells.

In vitro activity:

To be determined

In vivo activity:

The successful application of R162 to overcome both acquired resistance and epithelial-mesenchymal transition-induced metastasis in vivo identified GLUD1 as a promising and druggable therapeutic target for malignant progression of non-small-cell lung cancer. Reference: Pharmacol Res. 2022 Nov;185:106490. https://pubmed.ncbi.nlm.nih.gov/36216131/

	Solvent	mg/mL	mM
Solubility
	DMSO	13.2	50.00

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 264.28 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Wang Q, Wu M, Li H, Rao X, Ao L, Wang H, Yao L, Wang X, Hong X, Wang J, Aa J, Sun M, Wang G, Liu J, Zhou F. Therapeutic targeting of glutamate dehydrogenase 1 that links metabolic reprogramming and Snail-mediated epithelial-mesenchymal transition in drug-resistant lung cancer. Pharmacol Res. 2022 Nov;185:106490. doi: 10.1016/j.phrs.2022.106490. Epub 2022 Oct 8. PMID: 36216131. 2. Jin L, Chun J, Pan C, Kumar A, Zhang G, Ha Y, Li D, Alesi GN, Kang Y, Zhou L, Yu WM, Magliocca KR, Khuri FR, Qu CK, Metallo C, Owonikoko TK, Kang S. The PLAG1-GDH1 Axis Promotes Anoikis Resistance and Tumor Metastasis through CamKK2-AMPK Signaling in LKB1-Deficient Lung Cancer. Mol Cell. 2018 Jan 4;69(1):87-99.e7. doi: 10.1016/j.molcel.2017.11.025. Epub 2017 Dec 14. PMID: 29249655; PMCID: PMC5777230. 3. Jin L, Li D, Alesi GN, Fan J, Kang HB, Lu Z, Boggon TJ, Jin P, Yi H, Wright ER, Duong D, Seyfried NT, Egnatchik R, DeBerardinis RJ, Magliocca KR, He C, Arellano ML, Khoury HJ, Shin DM, Khuri FR, Kang S. Glutamate dehydrogenase 1 signals through antioxidant glutathione peroxidase 1 to regulate redox homeostasis and tumor growth. Cancer Cell. 2015 Feb 9;27(2):257-70. doi: 10.1016/j.ccell.2014.12.006. PMID: 25670081; PMCID: PMC4325424.

In vitro protocol:

To be determined

In vivo protocol:

1: Jin L, Chun J, Pan C, Kumar A, Zhang G, Ha Y, Li D, Alesi GN, Kang Y, Zhou L, Yu WM, Magliocca KR, Khuri FR, Qu CK, Metallo C, Owonikoko TK, Kang S. The PLAG1-GDH1 Axis Promotes Anoikis Resistance and Tumor Metastasis through CamKK2-AMPK Signaling in LKB1-Deficient Lung Cancer. Mol Cell. 2017 Dec 12. pii: S1097-2765(17)30884-5. doi: 10.1016/j.molcel.2017.11.025. [Epub ahead of print] PubMed PMID: 29249655. 2: Cima LN, Colita A, Fica S. Perspectives on the co-treatment with GnRHa in female patients undergoing hematopoietic stem cell transplantation. Endocr Connect. 2017 Nov;6(8):R162-R170. doi: 10.1530/EC-17-0246. Epub 2017 Sep 25. Review. PubMed PMID: 28947558; PubMed Central PMCID: PMC5655684. 3: Gronsang D, Bui AN, Trinh DQ, Bui VN, Nguyen KV, Can MX, Omatsu T, Mizutani T, Nagai M, Katayama Y, Thampaisarn R, Ogawa H, Imai K. Characterization of cross-clade monoclonal antibodies against H5N1 highly pathogenic avian influenza virus and their application to the antigenic analysis of diverse H5 subtype viruses. Arch Virol. 2017 Aug;162(8):2257-2269. doi: 10.1007/s00705-017-3350-0. Epub 2017 Apr 12. PubMed PMID: 28405766. 4: Steffen-Munsberg F, Matzel P, Sowa MA, Berglund P, Bornscheuer UT, Höhne M. Bacillus anthracis ω-amino acid:pyruvate transaminase employs a different mechanism for dual substrate recognition than other amine transaminases. Appl Microbiol Biotechnol. 2016 May;100(10):4511-21. doi: 10.1007/s00253-015-7275-9. Epub 2016 Jan 21. PubMed PMID: 26795966. 5: Akhmanova A, Hoogenraad CC. Microtubule minus-end-targeting proteins. Curr Biol. 2015 Feb 16;25(4):R162-71. doi: 10.1016/j.cub.2014.12.027. Review. PubMed PMID: 25689915. 6: Jin L, Li D, Alesi GN, Fan J, Kang HB, Lu Z, Boggon TJ, Jin P, Yi H, Wright ER, Duong D, Seyfried NT, Egnatchik R, DeBerardinis RJ, Magliocca KR, He C, Arellano ML, Khoury HJ, Shin DM, Khuri FR, Kang S. Glutamate dehydrogenase 1 signals through antioxidant glutathione peroxidase 1 to regulate redox homeostasis and tumor growth. Cancer Cell. 2015 Feb 9;27(2):257-70. doi: 10.1016/j.ccell.2014.12.006. PubMed PMID: 25670081; PubMed Central PMCID: PMC4325424. 7: Peat G, Bergknut C, Frobell R, Jöud A, Englund M. Population-wide incidence estimates for soft tissue knee injuries presenting to healthcare in southern Sweden: data from the Skåne Healthcare Register. Arthritis Res Ther. 2014 Jul 31;16(4):R162. doi: 10.1186/ar4678. PubMed PMID: 25082600; PubMed Central PMCID: PMC4262192. 8: Beurskens CJ, Horn J, de Boer AM, Schultz MJ, van Leeuwen EM, Vroom MB, Juffermans NP. Cardiac arrest patients have an impaired immune response, which is not influenced by induced hypothermia. Crit Care. 2014 Jul 30;18(4):R162. doi: 10.1186/cc14002. PubMed PMID: 25078879; PubMed Central PMCID: PMC4261599. 9: Marthiens V, Basto R. Microcephaly: STIL(l) a tale of too many centrosomes. Curr Biol. 2014 Feb 17;24(4):R162-4. doi: 10.1016/j.cub.2013.12.054. PubMed PMID: 24556440. 10: Ten Cate DF, Luime JJ, van der Ven M, Hazes JM, Kooiman K, de Jong N, Bosch JG. Very different performance of the power Doppler modalities of several ultrasound machines ascertained by a microvessel flow phantom. Arthritis Res Ther. 2013 Oct 24;15(5):R162. doi: 10.1186/ar4345. PubMed PMID: 24286540; PubMed Central PMCID: PMC3978434. 11: Xie X, Zhang X, Fu J, Wang H, Jonas JB, Peng X, Tian G, Xian J, Ritch R, Li L, Kang Z, Zhang S, Yang D, Wang N; Beijing iCOP Study Group. Noninvasive intracranial pressure estimation by orbital subarachnoid space measurement: the Beijing Intracranial and Intraocular Pressure (iCOP) study. Crit Care. 2013 Jul 24;17(4):R162. doi: 10.1186/cc12841. PubMed PMID: 23883736; PubMed Central PMCID: PMC4056099. 12: Schultheiß C, Saugel B, Phillip V, Thies P, Noe S, Mayr U, Haller B, Einwächter H, Schmid RM, Huber W. Continuous venovenous hemodialysis with regional citrate anticoagulation in patients with liver failure: a prospective observational study. Crit Care. 2012 Aug 22;16(4):R162. doi: 10.1186/cc11485. PubMed PMID: 22913794; PubMed Central PMCID: PMC3580752. 13: Bjersing JL, Dehlin M, Erlandsson M, Bokarewa MI, Mannerkorpi K. Changes in pain and insulin-like growth factor 1 in fibromyalgia during exercise: the involvement of cerebrospinal inflammatory factors and neuropeptides. Arthritis Res Ther. 2012 Jul 9;14(4):R162. doi: 10.1186/ar3902. PubMed PMID: 22776095; PubMed Central PMCID: PMC3580554. 14: Pinotti M, Caruso P, Canella A, Campioni M, Tagariello G, Castaman G, Giacomelli S, Belvini D, Bernardi F. Ribosome readthrough accounts for secreted full-length factor IX in hemophilia B patients with nonsense mutations. Hum Mutat. 2012 Sep;33(9):1373-6. doi: 10.1002/humu.22120. Epub 2012 Jun 11. PubMed PMID: 22618954. 15: Hsieh AH, Jhou YJ, Liang CT, Chang M, Wang SL. Fragment of tegument protein pp65 of human cytomegalovirus induces autoantibodies in BALB/c mice. Arthritis Res Ther. 2011;13(5):R162. doi: 10.1186/ar3481. Epub 2011 Oct 11. PubMed PMID: 21989080; PubMed Central PMCID: PMC3308095. 16: He JL, Liu JH, Liu F, Tan P, Lin T, Li XL. Mutation screening of BMP4 and Id2 genes in Chinese patients with congenital ureteropelvic junction obstruction. Eur J Pediatr. 2012 Mar;171(3):451-6. doi: 10.1007/s00431-011-1561-z. Epub 2011 Sep 17. PubMed PMID: 21927809. 17: Chantry A. WWP2 ubiquitin ligase and its isoforms: new biological insight and promising disease targets. Cell Cycle. 2011 Aug 1;10(15):2437-9. Epub 2011 Aug 1. PubMed PMID: 21750408; PubMed Central PMCID: PMC4074766. 18: Shahin J, DeVarennes B, Tse CW, Amarica DA, Dial S. The relationship between inotrope exposure, six-hour postoperative physiological variables, hospital mortality and renal dysfunction in patients undergoing cardiac surgery. Crit Care. 2011 Jul 7;15(4):R162. doi: 10.1186/cc10302. PubMed PMID: 21736726; PubMed Central PMCID: PMC3387599. 19: Blumenthal T. Split genes: another surprise from Giardia. Curr Biol. 2011 Feb 22;21(4):R162-3. doi: 10.1016/j.cub.2011.01.032. PubMed PMID: 21334298. 20: Soond SM, Chantry A. Selective targeting of activating and inhibitory Smads by distinct WWP2 ubiquitin ligase isoforms differentially modulates TGFβ signalling and EMT. Oncogene. 2011 May 26;30(21):2451-62. doi: 10.1038/onc.2010.617. Epub 2011 Jan 24. PubMed PMID: 21258410; PubMed Central PMCID: PMC4073228.