KUS121 | CAS#1357164-52-3 | VCP modulator

MedKoo Cat#: 461979 | Name: KUS121

Featured

Description:

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

KUS121 is a valosin-containing protein (VCP) modulator that inhibits VCP ATPase activity. It inhibits cell death, ATP depletion, and upregulation of C/EBP-homologous protein (CHOP) induced by tunicamycin, an inducer of ER stress, in HeLa cells.

Chemical Structure

KUS121

CAS#1357164-52-3 (sodium)

Theoretical Analysis

MedKoo Cat#: 461979

Name: KUS121

CAS#: 1357164-52-3 (sodium)

Chemical Formula: C22H16FN4NaO3S

Exact Mass: 458.0825

Molecular Weight: 458.44

Elemental Analysis: C, 57.64; H, 3.52; F, 4.14; N, 12.22; Na, 5.01; O, 10.47; S, 6.99

Price and Availability

Size	Price	Availability	Quantity
10mg	USD 350.00	2 Weeks
50mg	USD 1,050.00	2 Weeks

Bulk Inquiry

Buy Now

Add to Cart

Related CAS #

1357245-09-0 (free acid) 1357164-52-3 (sodium)

Synonym

KUS121; KUS-121; KUS 121;

IUPAC/Chemical Name

4-amino-3-[2-[6-(4-fluoro-2-methylphenyl)-3-pyridinyl]diazenyl]-1-naphthalenesulfonic acid, monosodium salt

InChi Key

OEEZHMGRDYLKGJ-JGUILPGDSA-M

InChi Code

InChI=1S/C22H17FN4O3S.Na/c1-13-10-14(23)6-8-16(13)19-9-7-15(12-25-19)26-27-20-11-21(31(28,29)30)17-4-2-3-5-18(17)22(20)24;/h2-12H,24H2,1H3,(H,28,29,30);/q;+1/p-1/b27-26+;

SMILES Code

O=S(C1=C2C=CC=CC2=C(N)C(/N=N/C3=CC=C(C4=CC=C(F)C=C4C)N=C3)=C1)([O-])=O.[Na+]

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

>3 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:

A VCP modulator.

In vitro activity:

In in vitro experiments, this study evaluated cell viability and ATP levels of proximal tubular cells with or without KUS121 under endoplasmic reticulum (ER) stress conditions. KUS121 protected proximal tubular cells from cell death under ER stress. Reference: Am J Physiol Renal Physiol. 2022 May 1;322(5):F577-F586. https://pubmed.ncbi.nlm.nih.gov/35343850/

In vivo activity:

In vivo, in a rat PTOA model by cyclic compressive loading, intra-articular treatments of KUS121 significantly improved the modified Mankin scores and reduced damaged-cartilage volumes, as compared to vehicle treatment. Moreover, KUS121 markedly reduced the numbers of TUNEL-, CHOP-, MMP-13-, and ADAMTS-5-positive chondrocytes in the damaged knees. Reference: Sci Rep. 2020 Nov 27;10(1):20787. https://pubmed.ncbi.nlm.nih.gov/33247195/

Preparing Stock Solutions

The following data is based on the product molecular weight 458.44 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. Hata Y, Date R, Fujimoto D, Ikeda HO, Umemoto S, Kanki T, Nishiguchi Y, Mizumoto T, Hayata M, Kakizoe Y, Izumi Y, Kakizuka A, Mukoyama M, Kuwabara T. A novel VCP modulator KUS121 exerts renoprotective effects in ischemia-reperfusion injury with retaining ATP and restoring ERAD-processing capacity. Am J Physiol Renal Physiol. 2022 May 1;322(5):F577-F586. doi: 10.1152/ajprenal.00392.2021. Epub 2022 Mar 28. PMID: 35343850. 2. Iwai S, Ikeda HO, Mera H, Nishitani K, Saito M, Tsujikawa A, Kakizuka A. KUS121 attenuates the progression of monosodium iodoacetate-induced osteoarthritis in rats. Sci Rep. 2021 Aug 2;11(1):15651. doi: 10.1038/s41598-021-95173-6. PMID: 34341460; PMCID: PMC8329178. 3. Saito M, Nishitani K, Ikeda HO, Yoshida S, Iwai S, Ji X, Nakahata A, Ito A, Nakamura S, Kuriyama S, Yoshitomi H, Murata K, Aoyama T, Ito H, Kuroki H, Kakizuka A, Matsuda S. A VCP modulator, KUS121, as a promising therapeutic agent for post-traumatic osteoarthritis. Sci Rep. 2020 Nov 27;10(1):20787. doi: 10.1038/s41598-020-77735-2. Erratum in: Sci Rep. 2021 Mar 29;11(1):7442. PMID: 33247195; PMCID: PMC7695735. 4. Hasegawa T, Ikeda HO, Gotoh N, Iida K, Iwai S, Nakano N, Kakizuka A, Tsujikawa A. Effect of VCP modulators on gene expression profiles of retinal ganglion cells in an acute injury mouse model. Sci Rep. 2020 Mar 6;10(1):4251. doi: 10.1038/s41598-020-61160-6. PMID: 32144342; PMCID: PMC7060332.

In vitro protocol:

In vivo protocol:

1. Saito M, Nishitani K, Ikeda HO, Yoshida S, Iwai S, Ji X, Nakahata A, Ito A, Nakamura S, Kuriyama S, Yoshitomi H, Murata K, Aoyama T, Ito H, Kuroki H, Kakizuka A, Matsuda S. A VCP modulator, KUS121, as a promising therapeutic agent for post-traumatic osteoarthritis. Sci Rep. 2020 Nov 27;10(1):20787. doi: 10.1038/s41598-020-77735-2. Erratum in: Sci Rep. 2021 Mar 29;11(1):7442. PMID: 33247195; PMCID: PMC7695735. 2. Hasegawa T, Ikeda HO, Gotoh N, Iida K, Iwai S, Nakano N, Kakizuka A, Tsujikawa A. Effect of VCP modulators on gene expression profiles of retinal ganglion cells in an acute injury mouse model. Sci Rep. 2020 Mar 6;10(1):4251. doi: 10.1038/s41598-020-61160-6. PMID: 32144342; PMCID: PMC7060332.

1: Kinoshita H, Maki T, Yasuda K, Kishida N, Sasaoka N, Takagi Y, Kakizuka A, Takahashi R. KUS121, a valosin-containing protein modulator, attenuates ischemic stroke via preventing ATP depletion. Sci Rep. 2019 Aug 8;9(1):11519. doi: 10.1038/s41598-019-47993-w. PubMed PMID: 31395936; PubMed Central PMCID: PMC6687885. 2: Ide Y, Horie T, Saito N, Watanabe S, Otani C, Miyasaka Y, Kuwabara Y, Nishino T, Nakao T, Nishiga M, Nishi H, Nakashima Y, Nakazeki F, Koyama S, Kimura M, Tsuji S, Rodriguez RR, Xu S, Yamasaki T, Watanabe T, Yamamoto M, Yanagita M, Kimura T, Kakizuka A, Ono K. Cardioprotective Effects of VCP Modulator KUS121 in Murine and Porcine Models of Myocardial Infarction. JACC Basic Transl Sci. 2019 Oct 28;4(6):701-714. doi: 10.1016/j.jacbts.2019.06.001. eCollection 2019 Oct. PubMed PMID: 31709319; PubMed Central PMCID: PMC6834964. 3: Muraoka Y, Iida Y, Ikeda HO, Iwai S, Hata M, Iwata T, Nakayama M, Shimozawa N, Katakai Y, Kakizuka A, Yoshimura N, Tsujikawa A. KUS121, an ATP regulator, mitigates chorioretinal pathologies in animal models of age-related macular degeneration. Heliyon. 2018 May 14;4(5):e00624. doi: 10.1016/j.heliyon.2018.e00624. eCollection 2018 May. PubMed PMID: 29872758; PubMed Central PMCID: PMC5986307. 4: Hata M, Ikeda HO, Kikkawa C, Iwai S, Muraoka Y, Hasegawa T, Kakizuka A, Yoshimura N. KUS121, a VCP modulator, attenuates ischemic retinal cell death via suppressing endoplasmic reticulum stress. Sci Rep. 2017 Mar 20;7:44873. doi: 10.1038/srep44873. PubMed PMID: 28317920; PubMed Central PMCID: PMC5357950. 5: Hasegawa T, Muraoka Y, Ikeda HO, Tsuruyama T, Kondo M, Terasaki H, Kakizuka A, Yoshimura N. Neuoroprotective efficacies by KUS121, a VCP modulator, on animal models of retinal degeneration. Sci Rep. 2016 Aug 9;6:31184. doi: 10.1038/srep31184. PubMed PMID: 27503804; PubMed Central PMCID: PMC4977562. 6: Hata M, Ikeda HO. Modulation of valosin-containing protein by Kyoto University Substances (KUS) as a novel therapeutic strategy for ischemic neuronal diseases. Neural Regen Res. 2017 Aug;12(8):1252-1255. doi: 10.4103/1673-5374.213540. Review. PubMed PMID: 28966635; PubMed Central PMCID: PMC5607815. 7: Ikeda HO, Muraoka Y, Hata M, Sumi E, Ikeda T, Nakagawa T, Abe H, Tada H, Morita S, Kakizuka A, Yoshimura N, Tsujikawa A. Safety and effectiveness of a novel neuroprotectant, KUS121, in patients with non-arteritic central retinal artery occlusion: An open-label, non-randomized, first-in-humans, phase 1/2 trial. PLoS One. 2020 Feb 13;15(2):e0229068. doi: 10.1371/journal.pone.0229068. eCollection 2020. PubMed PMID: 32053676; PubMed Central PMCID: PMC7018138. 8: Kariya T, Ishikawa K. The Art of War in Drug Development. JACC Basic Transl Sci. 2019 Oct 28;4(6):715-716. doi: 10.1016/j.jacbts.2019.09.002. eCollection 2019 Oct. PubMed PMID: 31713541; PubMed Central PMCID: PMC6834934. 9: Nakano N, Ikeda HO, Hasegawa T, Muraoka Y, Iwai S, Tsuruyama T, Nakano M, Fuchigami T, Shudo T, Kakizuka A, Yoshimura N. Neuroprotective effects of VCP modulators in mouse models of glaucoma. Heliyon. 2016 Apr 19;2(4):e00096. doi: 10.1016/j.heliyon.2016.e00096. eCollection 2016 Apr. PubMed PMID: 27441270; PubMed Central PMCID: PMC4946081. 10: Hasegawa T, Ikeda HO, Gotoh N, Iida K, Iwai S, Nakano N, Kakizuka A, Tsujikawa A. Effect of VCP modulators on gene expression profiles of retinal ganglion cells in an acute injury mouse model. Sci Rep. 2020 Mar 6;10(1):4251. doi: 10.1038/s41598-020-61160-6. PubMed PMID: 32144342; PubMed Central PMCID: PMC7060332.