OTS514 | CAS#1338540-63-8 | TOPK inhibitor

MedKoo Cat#: 471199 | Name: OTS514

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Description:

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

OTS514 is a potent TOPK (T-LAK cell-originated protein kinase) inhibitor. OTS514 exhibits growth suppressive effect on small cell lung cancer. TS514 effectively suppressed growth of SCLC cell lines (IC50 ; 0.4 ~ 42.6 nM) and led to their apoptotic cell death. Treatment with OTS514 suppressed forkhead box protein M1 (FOXM1) activity, which was involved in stemness of CSC. Furthermore, OTS514 treatment reduced CD90-positive SCLC cells and showed higher cytotoxic effect against lung sphere-derived CSC-like SCLC cells.

Chemical Structure

OTS514

CAS#1338540-63-8

Theoretical Analysis

MedKoo Cat#: 471199

Name: OTS514

CAS#: 1338540-63-8

Chemical Formula: C21H20N2O2S

Exact Mass: 364.1250

Molecular Weight: 364.46

Elemental Analysis: C, 69.21; H, 5.53; N, 7.69; O, 8.78; S, 8.80

Price and Availability

Size	Price	Availability
10mg	USD 265.00	2 Weeks
25mg	USD 450.00	2 Weeks
50mg	USD 800.00	2 Weeks

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Related CAS #

1338540-63-8 (free base) 1338544-87-8 (HBr) 1338541-25-5 (s-isomer) 1338545-92-8 (S-isomer HCl) 2319647-76-0 (HCl)

Synonym

OTS514; OTS 514; OTS-514

IUPAC/Chemical Name

9-[4-[(1R)-2-amino-1-methylethyl]phenyl]-8-hydroxy-6-methyl-thieno[2,3-c]quinolin-4(5H)-one

InChi Key

OETLNMOJNONWOY-LBPRGKRZSA-N

InChi Code

InChI=1S/C21H20N2O2S/c1-11-9-16(24)17(14-5-3-13(4-6-14)12(2)10-22)18-15-7-8-26-20(15)21(25)23-19(11)18/h3-9,12,24H,10,22H2,1-2H3,(H,23,25)/t12-/m0/s1

SMILES Code

O=C1NC2=C(C(C3=CC=C([C@@H](C)CN)C=C3)=C(O)C=C2C)C4=C1SC=C4

Appearance

To be determined

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

To be determined

Shelf Life

>2 years if stored properly

Drug Formulation

To be determined

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

Preparing Stock Solutions

The following data is based on the product molecular weight 364.46 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

1: Zeng F, Du S, Wu M, Dai C, Li J, Wang J, Hu G, Cai P, Wang L. The oncogenic kinase TOPK upregulates in psoriatic keratinocytes and contributes to psoriasis progression by regulating neutrophils infiltration. Cell Commun Signal. 2024 Aug 1;22(1):386. doi: 10.1186/s12964-024-01758-9. PMID: 39090602; PMCID: PMC11292866. 2: Zeng F, Lu H, Wu M, Dai C, Li J, Wang J, Hu G. Topical application of TOPK inhibitor OTS514 suppresses psoriatic progression by inducing keratinocytes cell cycle arrest and apoptosis. Exp Dermatol. 2023 Oct;32(10):1823-1833. doi: 10.1111/exd.14909. Epub 2023 Aug 14. PMID: 37578092. 3: Cai C, Yao S, Zou Y, Lu H, Chen X, Wang Y, Zheng K, Zhu F, Wang Y, Xiong H, Zhu J. KRASG12C mutation-induced TOPK overexpression contributes to tumour progression in non-small cell lung cancer. J Cell Mol Med. 2023 Jun;27(12):1637-1652. doi: 10.1111/jcmm.17640. Epub 2023 May 24. PMID: 37226642; PMCID: PMC10273069. 4: Kato M, Ota A, Ono T, Karnan S, Hyodo T, Rahman ML, Hasan MN, Onda M, Kondo S, Ito K, Furuhashi A, Hayashi T, Konishi H, Tsuzuki S, Hosokawa Y, Kazaoka Y. PDZ-binding kinase inhibitor OTS514 suppresses the proliferation of oral squamous carcinoma cells. Oral Dis. 2024 Mar;30(2):223-234. doi: 10.1111/odi.14533. Epub 2023 Mar 13. PMID: 36799330. 5: Zhang H, Dong QQ, Shu HP, Tu YC, Liao QQ, Yao LJ. TOPK Activation Exerts Protective Effects on Cisplatin-induced Acute Kidney Injury. Curr Med Sci. 2022 Aug;42(4):742-753. doi: 10.1007/s11596-022-2545-0. Epub 2022 Jun 9. Erratum in: Curr Med Sci. 2022 Dec;42(6):1334. doi: 10.1007/s11596-022-2660-y. PMID: 35678915. 6: Koshino A, Nagano A, Ota A, Hyodo T, Ueki A, Komura M, Sugimura-Nagata A, Ebi M, Ogasawara N, Kasai K, Hosokawa Y, Kasugai K, Takahashi S, Inaguma S. PBK Enhances Cellular Proliferation With Histone H3 Phosphorylation and Suppresses Migration and Invasion With CDH1 Stabilization in Colorectal Cancer. Front Pharmacol. 2022 Jan 18;12:772926. doi: 10.3389/fphar.2021.772926. PMID: 35115926; PMCID: PMC8804381. 7: Thanindratarn P, Wei R, Dean DC, Singh A, Federman N, Nelson SD, Hornicek FJ, Duan Z. T-LAK cell-originated protein kinase (TOPK): an emerging prognostic biomarker and therapeutic target in osteosarcoma. Mol Oncol. 2021 Dec;15(12):3721-3737. doi: 10.1002/1878-0261.13039. Epub 2021 Jun 29. PMID: 34115928; PMCID: PMC8637563. 8: Nagano-Matsuo A, Inoue S, Koshino A, Ota A, Nakao K, Komura M, Kato H, Naiki- Ito A, Watanabe K, Nagayasu Y, Hosokawa Y, Takiguchi S, Kasugai K, Kasai K, Inaguma S, Takahashi S. PBK expression predicts favorable survival in colorectal cancer patients. Virchows Arch. 2021 Aug;479(2):277-284. doi: 10.1007/s00428-021-03062-0. Epub 2021 Feb 27. PMID: 33638656. 9: Alhawas L, Amin KS, Salla B, Banerjee PP. T-LAK cell-originated protein kinase (TOPK) enhances androgen receptor splice variant (ARv7) and drives androgen-independent growth in prostate cancer. Carcinogenesis. 2021 Apr 17;42(3):423-435. doi: 10.1093/carcin/bgaa120. PMID: 33185682. 10: Ma H, Han F, Yan X, Qi G, Li Y, Li R, Yan S, Yuan C, Song K, Kong B. PBK promotes aggressive phenotypes of cervical cancer through ERK/c-Myc signaling pathway. J Cell Physiol. 2021 Apr;236(4):2767-2781. doi: 10.1002/jcp.30134. Epub 2020 Nov 13. PMID: 33184870. 11: Thanindratarn P, Dean DC, Nelson SD, Hornicek FJ, Duan Z. T-LAK cell- originated protein kinase (TOPK) is a Novel Prognostic and Therapeutic Target in Chordoma. Cell Prolif. 2020 Oct;53(10):e12901. doi: 10.1111/cpr.12901. Epub 2020 Sep 22. Erratum in: Cell Prolif. 2023 Apr;56(4):e13414. doi: 10.1111/cpr.13414. PMID: 32960500; PMCID: PMC7574876. 12: Park JH, Park SA, Lee YJ, Joo NR, Shin J, Oh SM. TOPK inhibition accelerates oxidative stress‑induced granulosa cell apoptosis via the p53/SIRT1 axis. Int J Mol Med. 2020 Nov;46(5):1923-1937. doi: 10.3892/ijmm.2020.4712. Epub 2020 Aug 27. PMID: 32901866. 13: Ota A, Hanamura I, Karnan S, Inaguma S, Takei N, Lam VQ, Mizuno S, Kanasugi J, Wahiduzzaman M, Rahman ML, Hyodo T, Konishi H, Tsuzuki S, Ikeda H, Takami A, Hosokawa Y. Novel Interleukin-6 Inducible Gene PDZ-Binding Kinase Promotes Tumor Growth of Multiple Myeloma Cells. J Interferon Cytokine Res. 2020 Aug;40(8):389-405. doi: 10.1089/jir.2020.0111. Epub 2020 Jul 23. PMID: 32721246; PMCID: PMC7462034. 14: Pirovano G, Roberts S, Reiner T. TOPKi-NBD: a fluorescent small molecule for tumor imaging. Eur J Nucl Med Mol Imaging. 2020 Apr;47(4):1003-1010. doi: 10.1007/s00259-019-04608-w. Epub 2019 Nov 16. PMID: 31734783; PMCID: PMC7080599. 15: Stefka AT, Johnson D, Rosebeck S, Park JH, Nakamura Y, Jakubowiak AJ. Potent anti-myeloma activity of the TOPK inhibitor OTS514 in pre-clinical models. Cancer Med. 2020 Jan;9(1):324-334. doi: 10.1002/cam4.2695. Epub 2019 Nov 12. PMID: 31714026; PMCID: PMC6943155. 16: Cabré A, Romagnoli E, Martínez-Balart P, Verdaguer X, Riera A. Highly Enantioselective Iridium-Catalyzed Hydrogenation of 2-Aryl Allyl Phthalimides. Org Lett. 2019 Dec 6;21(23):9709-9713. doi: 10.1021/acs.orglett.9b03865. Epub 2019 Nov 8. PMID: 31702157. 17: Uchida E, Suwa S, Yoshimoto R, Watanabe K, Kasama T, Miura O, Fukuda T. TOPK is regulated by PP2A and BCR/ABL in leukemia and enhances cell proliferation. Int J Oncol. 2019 May;54(5):1785-1796. doi: 10.3892/ijo.2019.4740. Epub 2019 Mar 5. PMID: 30864683. 18: Ma H, Li Y, Wang X, Wu H, Qi G, Li R, Yang N, Gao M, Yan S, Yuan C, Kong B. PBK, targeted by EVI1, promotes metastasis and confers cisplatin resistance through inducing autophagy in high-grade serous ovarian carcinoma. Cell Death Dis. 2019 Feb 18;10(3):166. doi: 10.1038/s41419-019-1415-6. PMID: 30778048; PMCID: PMC6379381. 19: Herbert KJ, Ashton TM, Prevo R, Pirovano G, Higgins GS. T-LAK cell- originated protein kinase (TOPK): an emerging target for cancer-specific therapeutics. Cell Death Dis. 2018 Oct 24;9(11):1089. doi: 10.1038/s41419-018-1131-7. PMID: 30356039; PMCID: PMC6200809. 20: Park JH, Inoue H, Kato T, Zewde M, Miyamoto T, Matsuo Y, Salgia R, Nakamura Y. TOPK (T-LAK cell-originated protein kinase) inhibitor exhibits growth suppressive effect on small cell lung cancer. Cancer Sci. 2017 Mar;108(3):488-496. doi: 10.1111/cas.13160. PMID: 28075524; PMCID: PMC5378278.