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XMD8-92
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WARNING: This product is for research use only, not for human or veterinary use.

Hodoodo CAT#: H407373

CAS#: 1234480-50-2

Description: XMD8-92 is an ERK5/BMK1 inhibitor and also BRD4 inhibitor. XMD8-92 inhibits pancreatic tumor xenograft growth via a DCLK1-dependent mechanism. XMD8-92 blocks cellular BMK1 activation and significantly suppresses tumor growth in lung and cervical tumor models and is well tolerated in animals.

Chemical Structure

XMD8-92

CAS# 1234480-50-2

Instruction

Theoretical Analysis

Hodoodo Cat#: H407373
Name: XMD8-92
CAS#: 1234480-50-2
Chemical Formula: C26H30N6O3
Exact Mass: 474.24
Molecular Weight: 474.565
Elemental Analysis: C, 65.80; H, 6.37; N, 17.71; O, 10.11

Price and Availability

Size	Price	Availability	Quantity
50mg	USD 350
100mg	USD 600
200mg	USD 950
500mg	USD 1950
1g	USD 2950
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. Hodoodo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: XMD8-92; XMD-8-92; XMD 8-92; XMD892; XMD-892; XMD 892.

IUPAC/Chemical Name: 2-[[2-ethoxy-4-(4-hydroxy-1-piperidinyl)phenyl]amino]-5,11-dihydro-5,11-dimethyl-6H-pyrimido[4,5-b][1,4]benzodiazepin-6-one

InChi Key: QAPAJIZPZGWAND-UHFFFAOYSA-N

InChi Code: InChI=1S/C26H30N6O3/c1-4-35-23-15-17(32-13-11-18(33)12-14-32)9-10-20(23)28-26-27-16-22-24(29-26)30(2)21-8-6-5-7-19(21)25(34)31(22)3/h5-10,15-16,18,33H,4,11-14H2,1-3H3,(H,27,28,29)

SMILES Code: O=C1N(C)C2=CN=C(NC3=CC=C(N4CCC(O)CC4)C=C3OCC)N=C2N(C)C5=CC=CC=C15

Appearance: White to beige 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:

Instruction:

View handling instruction

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 474.57 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:
In vitro protocol:
In vivo protocol:

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1: Sun Y, Liang Y, Li Z, Xia N. Liraglutide Promotes Osteoblastic Differentiation in MC3T3-E1 Cells by ERK5 Pathway. Int J Endocrinol. 2020 Dec 9;2020:8821077. doi: 10.1155/2020/8821077. PMID: 33488706; PMCID: PMC7780226.

2: Lee GH, Park JS, Jin SW, Pham TH, Thai TN, Kim JY, Kim CY, Choi JH, Han EH, Jeong HG. Betulinic Acid Induces eNOS Expression via the AMPK-Dependent KLF2 Signaling Pathway. J Agric Food Chem. 2020 Dec 9;68(49):14523-14530. doi: 10.1021/acs.jafc.0c06250. Epub 2020 Nov 24. PMID: 33232606.

3: Zhang T, Zhao L, Zhang T, Wu W, Liu J, Wang X, Wan Y, Geng H, Sun X, Qian W, Yu D. Curcumin Negatively Regulates Cigarette Smoke-Induced Renal Cell Carcinoma Epithelial-Mesenchymal Transition Through the ERK5/AP-1 Pathway. Onco Targets Ther. 2020 Sep 29;13:9689-9700. doi: 10.2147/OTT.S265847. PMID: 33061449; PMCID: PMC7532894.

4: Ma C, Geng B, Zhang X, Li R, Yang X, Xia Y. Fluid Shear Stress Suppresses Osteoclast Differentiation in RAW264.7 Cells through Extracellular Signal- Regulated Kinase 5 (ERK5) Signaling Pathway. Med Sci Monit. 2020 Jan 8;26:e918370. doi: 10.12659/MSM.918370. PMID: 31914120; PMCID: PMC6977602.

5: Wright TD, Raybuck C, Bhatt A, Monlish D, Chakrabarty S, Wendekier K, Gartland N, Gupta M, Burow ME, Flaherty PT, Cavanaugh JE. Pharmacological inhibition of the MEK5/ERK5 and PI3K/Akt signaling pathways synergistically reduces viability in triple-negative breast cancer. J Cell Biochem. 2020 Feb;121(2):1156-1168. doi: 10.1002/jcb.29350. Epub 2019 Aug 28. PMID: 31464004; PMCID: PMC6923606.

6: Yue W, Li Y, Ou D, Yang Q. The GLP-1 receptor agonist liraglutide protects against oxidized LDL-induced endothelial inflammation and dysfunction via KLF2. IUBMB Life. 2019 Sep;71(9):1347-1354. doi: 10.1002/iub.2046. Epub 2019 Apr 10. PMID: 30969479.

7: Morimoto H, Kanastu-Shinohara M, Ogonuki N, Kamimura S, Ogura A, Yabe- Nishimura C, Mori Y, Morimoto T, Watanabe S, Otsu K, Yamamoto T, Shinohara T. ROS amplification drives mouse spermatogonial stem cell self-renewal. Life Sci Alliance. 2019 Apr 2;2(2):e201900374. doi: 10.26508/lsa.201900374. PMID: 30940732; PMCID: PMC6448598.

8: Pereira DM, Gomes SE, Borralho PM, Rodrigues CMP. MEK5/ERK5 activation regulates colon cancer stem-like cell properties. Cell Death Discov. 2019 Feb 11;5:68. doi: 10.1038/s41420-019-0150-1. PMID: 30774996; PMCID: PMC6370793.

9: Kang C, Kim JS, Kim CY, Kim EY, Chung HM. The Pharmacological Inhibition of ERK5 Enhances Apoptosis in Acute Myeloid Leukemia Cells. Int J Stem Cells. 2018 Nov 30;11(2):227-234. doi: 10.15283/ijsc18053. PMID: 30343550; PMCID: PMC6285287.

10: Tusa I, Cheloni G, Poteti M, Gozzini A, DeSouza NH, Shan Y, Deng X, Gray NS, Li S, Rovida E, Dello Sbarba P. Targeting the Extracellular Signal-Regulated Kinase 5 Pathway to Suppress Human Chronic Myeloid Leukemia Stem Cells. Stem Cell Reports. 2018 Oct 9;11(4):929-943. doi: 10.1016/j.stemcr.2018.08.016. Epub 2018 Sep 20. PMID: 30245209; PMCID: PMC6178886.

11: Deng Y, Lei T, Li H, Mo X, Wang Z, Ou H. ERK5/KLF2 activation is involved in the reducing effects of puerarin on monocyte adhesion to endothelial cells and atherosclerotic lesion in apolipoprotein E-deficient mice. Biochim Biophys Acta Mol Basis Dis. 2018 Aug;1864(8):2590-2599. doi: 10.1016/j.bbadis.2018.04.021. Epub 2018 Apr 30. PMID: 29723698.

12: Ding N, Geng B, Li Z, Yang Q, Yan L, Wan L, Zhang B, Wang C, Xia Y. Fluid shear stress promotes osteoblast proliferation through the NFATc1-ERK5 pathway. Connect Tissue Res. 2019 Mar;60(2):107-116. doi: 10.1080/03008207.2018.1459588. Epub 2018 Apr 16. PMID: 29609502.

13: Tusa I, Gagliardi S, Tubita A, Pandolfi S, Urso C, Borgognoni L, Wang J, Deng X, Gray NS, Stecca B, Rovida E. ERK5 is activated by oncogenic BRAF and promotes melanoma growth. Oncogene. 2018 May;37(19):2601-2614. doi: 10.1038/s41388-018-0164-9. Epub 2018 Feb 27. PMID: 29483645; PMCID: PMC5945581.

14: Sun X, Zhang T, Deng Q, Zhou Q, Sun X, Li E, Yu D, Zhong C. Benzidine Induces Epithelial-Mesenchymal Transition of Human Bladder Cancer Cells through Activation of ERK5 Pathway. Mol Cells. 2018 Mar 31;41(3):188-197. doi: 10.14348/molcells.2018.2113. Epub 2018 Feb 21. PMID: 29463068; PMCID: PMC5881092.

15: Thompson JK, Shukla A, Leggett AL, Munson PB, Miller JM, MacPherson MB, Beuschel SL, Pass HI, Shukla A. Extracellular signal regulated kinase 5 and inflammasome in progression of mesothelioma. Oncotarget. 2017 Dec 6;9(1):293-305. doi: 10.18632/oncotarget.22968. PMID: 29416614; PMCID: PMC5787465.

16: Cheng Z, Gao W, Fan X, Chen X, Mei H, Liu J, Luo X, Hu Y. Extracellular signal-regulated kinase 5 associates with casein kinase II to regulate GPIb-IX- mediated platelet activation via the PTEN/PI3K/Akt pathway. J Thromb Haemost. 2017 Aug;15(8):1679-1688. doi: 10.1111/jth.13755. Epub 2017 Jul 14. PMID: 28603902.

17: Wang H, Dai YY, Zhang WQ, Hsu PC, Yang YL, Wang YC, Chan G, Au A, Xu ZD, Jiang SJ, Wang W, Jablons DM, You L. DCLK1 is correlated with MET and ERK5 expression, and associated with prognosis in malignant pleural mesothelioma. Int J Oncol. 2017 Jul;51(1):91-103. doi: 10.3892/ijo.2017.4021. Epub 2017 May 26. PMID: 28560410; PMCID: PMC5467791.

18: Min J, Geng H, Liu Z, Liang Z, Zhang Z, Xie D, Wang Y, Zhang T, Yu D, Zhong C. ERK5 regulates tobacco smoke‑induced urocystic epithelial‑mesenchymal transition in BALB/c mice. Mol Med Rep. 2017 Jun;15(6):3893-3897. doi: 10.3892/mmr.2017.6457. Epub 2017 Apr 11. PMID: 28440402.

19: Song C, Wang L, Xu Q, Wang K, Xie D, Yu Z, Jiang K, Liao L, Yates JR, Lee JD, Yang Q. Targeting BMK1 Impairs the Drug Resistance to Combined Inhibition of BRAF and MEK1/2 in Melanoma. Sci Rep. 2017 Apr 7;7:46244. doi: 10.1038/srep46244. Erratum in: Sci Rep. 2017 May 26;7:46833. PMID: 28387310; PMCID: PMC5384194.

20: Liu Z, Liu J, Zhao L, Geng H, Ma J, Zhang Z, Yu D, Zhong C. Curcumin reverses benzidine-induced epithelial-mesenchymal transition via suppression of ERK5/AP-1 in SV-40 immortalized human urothelial cells. Int J Oncol. 2017 Apr;50(4):1321-1329. doi: 10.3892/ijo.2017.3887. Epub 2017 Feb 21. PMID: 28259934.

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XMD8-92 featured