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MedKoo Cat#: 528308 | Name: IMD-0354
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Description:

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

IMD-0354 is a nuclear factor-kappaB (NF-κB) activation inhibitor potentially for the treatment of atopic dermatitis. IMD-0354 significantly reduces the accumulation of inflammation damage and oxidative lesions. Furthermore, IMD-0354 treatment could block IκBα degradation and suppress mRNA and protein level of nuclear factor (NF) -κB p65.IMD-0354. IMD-0354 exerts anti-asthmatic action, at least partially, by blocking the activation and clonal expansion of CD4(+) Teff cells in the MLNs, which, consequently, prevents infiltration of the lungs with activated CD4(+) Teff cells.

Chemical Structure

IMD-0354
IMD-0354
CAS#978-62-1

Theoretical Analysis

MedKoo Cat#: 528308

Name: IMD-0354

CAS#: 978-62-1

Chemical Formula: C15H8ClF6NO2

Exact Mass: 383.0148

Molecular Weight: 383.67

Elemental Analysis: C, 46.96; H, 2.10; Cl, 9.24; F, 29.71; N, 3.65; O, 8.34

Price and Availability

Size Price Availability Quantity
5mg USD 90.00 Ready to Ship
10mg USD 150.00 Ready to Ship
25mg USD 250.00 Ready to Ship
50mg USD 450.00 Ready to Ship
100mg USD 700.00 Ready to Ship
200mg USD 1,050.00 Ready to Ship
500mg USD 1,850.00 Ready to Ship
1g USD 2,850.00 Ready to Ship
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Related CAS #
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Synonym
IMD-0354; IMD 0354; IMD0354; IKK2 Inhibitor V
IUPAC/Chemical Name
N-(3,5-bis(trifluoromethyl)phenyl)-5-chloro-2-hydroxybenzamide
InChi Key
CHILCFMQWMQVAL-UHFFFAOYSA-N
InChi Code
InChI=1S/C15H8ClF6NO2/c16-9-1-2-12(24)11(6-9)13(25)23-10-4-7(14(17,18)19)3-8(5-10)15(20,21)22/h1-6,24H,(H,23,25)
SMILES Code
O=C(NC1=CC(C(F)(F)F)=CC(C(F)(F)F)=C1)C2=CC(Cl)=CC=C2O
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
Biological target:
IMD-0354 targets and inhibits IKK-β, a key component of the NF-κB signaling pathway, thereby modulating inflammatory responses. Additionally, it impacts glutamine metabolism by preventing the localization of the SLC1A5 transporter to the plasma membrane, reducing intracellular glutamine levels.
In vitro activity:
1. IMD-0354, an inhibitor of NF-κB signaling through selective blockade of IKK-β, was tested for its therapeutic potential in an experimental autoimmune uveoretinitis (EAU) model of uveitis. Systemic administration of IMD-0354 significantly reduced clinical and histological severity, inflammatory edema, and NF-κB p65 translocation in the retinas of EAU mice. Additionally, IMD-0354 markedly inhibited Th1/Th17-mediated pro-inflammatory cytokine levels in vitro, indicating its potential as a treatment for endogenous uveitis. Reference: Liu Y, Kitaichi N, Wu D, Hase K, Satoh M, Iwata D, Namba K, Kanda A, Noda K, Itai A, Iwabuchi K, Ishida S. Attenuation of experimental autoimmune uveoretinitis in mice by IKKβ inhibitor IMD-0354. Biochem Biophys Res Commun. 2020 May 7;525(3):589-594.
In vivo activity:
1. IMD-0354 was identified as a potent inhibitor of glutamine uptake by preventing the localization of the SLC1A5 transporter to the plasma membrane. This inhibition led to reduced intracellular glutamine levels, attenuated mTOR signaling, and suppressed melanoma cell growth, inducing cell-cycle arrest, autophagy, and apoptosis. Additionally, IMD-0354 effectively reduced melanoma growth in a xenograft model, highlighting its potential as a therapeutic agent targeting altered glutamine metabolism in cancer. Reference: Feng Y, Pathria G, Heynen-Genel S, Jackson M, James B, Yin J, Scott DA, Ronai ZA. Identification and Characterization of IMD-0354 as a Glutamine Carrier Protein Inhibitor in Melanoma. Mol Cancer Ther. 2021 May;20(5):816-832.
Solvent mg/mL mM
Solubility
DMSO 100.0 260.64
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 383.67 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.

Recalculate based on batch purity %
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:
Liu Y, Kitaichi N, Wu D, Hase K, Satoh M, Iwata D, Namba K, Kanda A, Noda K, Itai A, Iwabuchi K, Ishida S. Attenuation of experimental autoimmune uveoretinitis in mice by IKKβ inhibitor IMD-0354. Biochem Biophys Res Commun. 2020 May 7;525(3):589-594. doi: 10.1016/j.bbrc.2020.02.117. Epub 2020 Feb 27. PMID: 32115150. Kanduri M, Tobin G, Aleskog A, Nilsson K, Rosenquist R. The novel NF-κB inhibitor IMD-0354 induces apoptosis in chronic lymphocytic leukemia. Blood Cancer J. 2011 Mar;1(3):e12. doi: 10.1038/bcj.2011.9. Epub 2011 Mar 25. PMID: 22829125; PMCID: PMC3255277. Feng Y, Pathria G, Heynen-Genel S, Jackson M, James B, Yin J, Scott DA, Ronai ZA. Identification and Characterization of IMD-0354 as a Glutamine Carrier Protein Inhibitor in Melanoma. Mol Cancer Ther. 2021 May;20(5):816-832. doi: 10.1158/1535-7163.MCT-20-0354. Epub 2021 Feb 25. PMID: 33632871; PMCID: PMC8102370. Kanduri M, Tobin G, Aleskog A, Nilsson K, Rosenquist R. The novel NF-κB inhibitor IMD-0354 induces apoptosis in chronic lymphocytic leukemia. Blood Cancer J. 2011 Mar;1(3):e12. doi: 10.1038/bcj.2011.9. Epub 2011 Mar 25. PMID: 22829125; PMCID: PMC3255277.
In vitro protocol:
Liu Y, Kitaichi N, Wu D, Hase K, Satoh M, Iwata D, Namba K, Kanda A, Noda K, Itai A, Iwabuchi K, Ishida S. Attenuation of experimental autoimmune uveoretinitis in mice by IKKβ inhibitor IMD-0354. Biochem Biophys Res Commun. 2020 May 7;525(3):589-594. doi: 10.1016/j.bbrc.2020.02.117. Epub 2020 Feb 27. PMID: 32115150. Kanduri M, Tobin G, Aleskog A, Nilsson K, Rosenquist R. The novel NF-κB inhibitor IMD-0354 induces apoptosis in chronic lymphocytic leukemia. Blood Cancer J. 2011 Mar;1(3):e12. doi: 10.1038/bcj.2011.9. Epub 2011 Mar 25. PMID: 22829125; PMCID: PMC3255277.
In vivo protocol:
Feng Y, Pathria G, Heynen-Genel S, Jackson M, James B, Yin J, Scott DA, Ronai ZA. Identification and Characterization of IMD-0354 as a Glutamine Carrier Protein Inhibitor in Melanoma. Mol Cancer Ther. 2021 May;20(5):816-832. doi: 10.1158/1535-7163.MCT-20-0354. Epub 2021 Feb 25. PMID: 33632871; PMCID: PMC8102370. Kanduri M, Tobin G, Aleskog A, Nilsson K, Rosenquist R. The novel NF-κB inhibitor IMD-0354 induces apoptosis in chronic lymphocytic leukemia. Blood Cancer J. 2011 Mar;1(3):e12. doi: 10.1038/bcj.2011.9. Epub 2011 Mar 25. PMID: 22829125; PMCID: PMC3255277.
1: Zhou Y, Hong Y, Huang H. Triptolide Attenuates Inflammatory Response in Membranous Glomerulo-Nephritis Rat via Downregulation of NF-κB Signaling Pathway. Kidney Blood Press Res. 2016;41(6):901-910. doi: 10.1159/000452591. PubMed PMID: 27871079. 2: Ma ZY, Zhong ZG, Qiu MY, Zhong YH, Zhang WX. TGF-β1 activates the canonical NF-κB signaling to promote cell survival and proliferation in dystrophic muscle fibroblasts in vitro. Biochem Biophys Res Commun. 2016 Mar 18;471(4):576-81. doi: 10.1016/j.bbrc.2016.02.029. PubMed PMID: 26874278. 3: Maślanka T, Otrocka-Domagała I, Zuśka-Prot M, Mikiewicz M, Przybysz J, Jasiecka A, Jaroszewski JJ. IκB kinase β inhibitor, IMD-0354, prevents allergic asthma in a mouse model through inhibition of CD4(+) effector T cell responses in the lung-draining mediastinal lymph nodes. Eur J Pharmacol. 2016 Mar 15;775:78-85. doi: 10.1016/j.ejphar.2016.02.023. PubMed PMID: 26868187. 4: Olkkonen J, Kouri VP, Hynninen J, Konttinen YT, Mandelin J. Differentially Expressed in Chondrocytes 2 (DEC2) Increases the Expression of IL-1β and Is Abundantly Present in Synovial Membrane in Rheumatoid Arthritis. PLoS One. 2015 Dec 28;10(12):e0145279. doi: 10.1371/journal.pone.0145279. PubMed PMID: 26710124; PubMed Central PMCID: PMC4692547. 5: Kong XJ, Duan LJ, Qian XQ, Xu D, Liu HL, Zhu YJ, Qi J. Tumor-suppressive microRNA-497 targets IKKβ to regulate NF-κB signaling pathway in human prostate cancer cells. Am J Cancer Res. 2015 Apr 15;5(5):1795-804. PubMed PMID: 26175947; PubMed Central PMCID: PMC4497445. 6: Zhao J, Liu C, Bai Y, Wang TY, Kan H, Sun Q. IKK inhibition prevents PM2.5-exacerbated cardiac injury in mice with type 2 diabetes. J Environ Sci (China). 2015 May 1;31:98-103. doi: 10.1016/j.jes.2014.10.018. PubMed PMID: 25968264. 7: Chen YM, Chiang WC, Yang Y, Lai CF, Wu KD, Lin SL. Pentoxifylline Attenuates Proteinuria in Anti-Thy1 Glomerulonephritis via Downregulation of Nuclear Factor-κB and Smad2/3 Signaling. Mol Med. 2015 Apr 13;21:276-84. doi: 10.2119/molmed.2015.00023. PubMed PMID: 25879629; PubMed Central PMCID: PMC4503651. 8: Kinose Y, Sawada K, Makino H, Ogura T, Mizuno T, Suzuki N, Fujikawa T, Morii E, Nakamura K, Sawada I, Toda A, Hashimoto K, Isobe A, Mabuchi S, Ohta T, Itai A, Morishige K, Kurachi H, Kimura T. IKKβ Regulates VEGF Expression and Is a Potential Therapeutic Target for Ovarian Cancer as an Antiangiogenic Treatment. Mol Cancer Ther. 2015 Apr;14(4):909-19. doi: 10.1158/1535-7163.MCT-14-0696. PubMed PMID: 25637316. 9: Verstrepen L, Beyaert R. Receptor proximal kinases in NF-κB signaling as potential therapeutic targets in cancer and inflammation. Biochem Pharmacol. 2014 Dec 15;92(4):519-29. doi: 10.1016/j.bcp.2014.10.017. Review. PubMed PMID: 25449604. 10: Liu C, Fonken LK, Wang A, Maiseyeu A, Bai Y, Wang TY, Maurya S, Ko YA, Periasamy M, Dvonch T, Morishita M, Brook RD, Harkema J, Ying Z, Mukherjee B, Sun Q, Nelson RJ, Rajagopalan S. Central IKKβ inhibition prevents air pollution mediated peripheral inflammation and exaggeration of type II diabetes. Part Fibre Toxicol. 2014 Oct 30;11:53. doi: 10.1186/s12989-014-0053-5. PubMed PMID: 25358444; PubMed Central PMCID: PMC4226918. 11: Stegajev V, Kouri VP, Salem A, Rozov S, Stark H, Nordström DC, Konttinen YT. Activation of histamine H4 receptor inhibits TNFα/IMD-0354-induced apoptosis in human salivary NS-SV-AC cells. Apoptosis. 2014 Dec;19(12):1702-11. doi: 10.1007/s10495-014-1036-6. PubMed PMID: 25239604. 12: Lennikov A, Hiraoka M, Abe A, Ohno S, Fujikawa T, Itai A, Ohguro H. IκB kinase-β inhibitor IMD-0354 beneficially suppresses retinal vascular permeability in streptozotocin-induced diabetic mice. Invest Ophthalmol Vis Sci. 2014 Sep 9;55(10):6365-73. doi: 10.1167/iovs.14-14671. PubMed PMID: 25205865. 13: Oida K, Matsuda A, Jung K, Xia Y, Jang H, Amagai Y, Ahn G, Nishikawa S, Ishizaka S, Jensen-Jarolim E, Matsuda H, Tanaka A. Nuclear factor-ĸB plays a critical role in both intrinsic and acquired resistance against endocrine therapy in human breast cancer cells. Sci Rep. 2014 Feb 17;4:4057. doi: 10.1038/srep04057. PubMed PMID: 24531845; PubMed Central PMCID: PMC3925966. 14: Nishikawa S, Tanaka A, Matsuda A, Oida K, Jang H, Jung K, Amagai Y, Ahn G, Okamoto N, Ishizaka S, Matsuda H. A molecular targeting against nuclear factor-κB, as a chemotherapeutic approach for human malignant mesothelioma. Cancer Med. 2014 Apr;3(2):416-25. doi: 10.1002/cam4.202. PubMed PMID: 24510578; PubMed Central PMCID: PMC3987091. 15: Watanabe R, Azuma RW, Suzuki J, Ogawa M, Itai A, Hirata Y, Komuro I, Isobe M. Inhibition of NF-κB activation by a novel IKK inhibitor reduces the severity of experimental autoimmune myocarditis via suppression of T-cell activation. Am J Physiol Heart Circ Physiol. 2013 Dec;305(12):H1761-71. doi: 10.1152/ajpheart.00159.2013. PubMed PMID: 24097428. 16: Gomez-Cabrero A, Wrasidlo W, Reisfeld RA. IMD-0354 targets breast cancer stem cells: a novel approach for an adjuvant to chemotherapy to prevent multidrug resistance in a murine model. PLoS One. 2013 Aug 27;8(8):e73607. doi: 10.1371/journal.pone.0073607. PubMed PMID: 24014113; PubMed Central PMCID: PMC3754963. 17: He W, Zhang M, Zhao M, Davis LS, Blackwell TS, Yull F, Breyer MD, Hao CM. Increased dietary sodium induces COX2 expression by activating NFκB in renal medullary interstitial cells. Pflugers Arch. 2014 Feb;466(2):357-67. doi: 10.1007/s00424-013-1328-7. PubMed PMID: 23900806; PubMed Central PMCID: PMC3946848. 18: Kaisari S, Rom O, Aizenbud D, Reznick AZ. Involvement of NF-κB and muscle specific E3 ubiquitin ligase MuRF1 in cigarette smoke-induced catabolism in C2 myotubes. Adv Exp Med Biol. 2013;788:7-17. doi: 10.1007/978-94-007-6627-3_2. PubMed PMID: 23835952. 19: Hosokawa S, Haraguchi G, Sasaki A, Arai H, Muto S, Itai A, Doi S, Mizutani S, Isobe M. Pathophysiological roles of nuclear factor kappaB (NF-kB) in pulmonary arterial hypertension: effects of synthetic selective NF-kB inhibitor IMD-0354. Cardiovasc Res. 2013 Jul 1;99(1):35-43. doi: 10.1093/cvr/cvt105. PubMed PMID: 23631839. 20: Fuchimoto J, Kojima T, Kobayashi N, Ohkuni T, Ogasawara N, Masaki T, Obata K, Nomura K, Kondoh A, Shigyo T, Himi T, Sawada N. Hop water extract inhibits double-stranded RNA-induced thymic stromal lymphopoietin release from human nasal epithelial cells. Am J Rhinol Allergy. 2012 Nov-Dec;26(6):433-8. doi: 10.2500/ajra.2012.26.3814. PubMed PMID: 23232191.