Art. -Nr.: HY-13479

EC144

Name: EC144
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SKU: HY-13479
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EC144 is an orally active and selective Hsp90 inhibitor (IC₅₀ = 1.1 nM, K_i = 0.2 nM). EC144 inhibits NLRP3 inflammasome (IC₅₀ 99 nM), binds to the ATP-binding pocket of the N-terminal domain, blocks chaperone function and destabilizes client proteins, including JAK2, STAT3, Her-2, EGFR, IGFR, Akt, ErbB2 and cyclin D, with higher selectivity for cytoplasmic Hsp90 than for Grp94 and TNF-α-inducible protein 1 (TNFAIP1). EC144 also directly binds to the extracellular region of E-cadherin, disrupting E-cadherin-mediated adhesion and tight junction function, and exhibits species-specific binding to human, bovine and mouse E-cadherin, but does not bind rat or chicken E-cadherin, and does not interact with N-cadherin or VE-cadherin. EC144 blocks NLRP3 inflammasome priming and activation, ASC speck formation, caspase-1 activation, IL-1β release and pyroptotic cell death. EC144 is detectable at brain levels after oral administration and upregulates brain Hsp70. EC144 can be used for research on rheumatoid arthritis, Alzheimer's disease, intervertebral disc degeneration, peritonitis, gastric cancer and botulism.

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Reinheit : 98.01%
CAS. Nr.: 911397-80-3
Formel: C₂₁H₂₄ClN₅O₂
Molecular Weight:413.90

Speicherung:

4°C, sealed storage, away from moisture and light

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

EC144 Chemical Structure

CAS. Nr.: 911397-80-3

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[5]^[1]^[3]

HSP90

1.1 nM (IC₅₀)

HSP90

0.2 nM (Ki)

NLRP3

99 nM (IC₅₀)

Alle HSP Isoform-spezifische Produkte anzeigen :

Alle NOD-like Receptor (NLR) Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
MCF7	EC50	6.5 nM	Induction of HER2 degradation in human MCF-7 breast cancer cells incubated for 16 hrs with EC144 and quantified by flow cytometry. Induction of HER2 degradation in human MCF-7 breast cancer cells incubated for 16 hrs with EC144 and quantified by flow cytometry.	21131419
RAW264.7	EC50	20 nM	Inhibition of LPS-stimulated TNF-alpha production in mouse RAW 264.7 macrophage-like cells pre-incubated with EC144 for 4 hrs then stimulated with LPS for 4 hrs, quantified by ELISA. Inhibition of LPS-stimulated TNF-alpha production in mouse RAW 264.7 macrophage-like cells pre-incubated with EC144 for 4 hrs then stimulated with LPS for 4 hrs, quantified by ELISA.	21131419
RAW264.7	EC50	17.4 nM	Inhibition of LPS-stimulated Eotaxin production in mouse RAW 264.7 macrophage-like cells pre-incubated with EC144 for 4 hrs then stimulated with LPS for 8 hrs, quantified by RodentMAP multiplex cytokine array. Inhibition of LPS-stimulated Eotaxin production in mouse RAW 264.7 macrophage-like cells pre-incubated with EC144 for 4 hrs then stimulated with LPS for 8 hrs, quantified by RodentMAP multiplex cytokine array.	21131419
RAW264.7	EC50	45.4 nM	Inhibition of LPS-stimulated FGF basic production in mouse RAW 264.7 macrophage-like cells pre-incubated with EC144 for 4 hrs then stimulated with LPS for 8 hrs, quantified by RodentMAP multiplex cytokine array. Inhibition of LPS-stimulated FGF basic production in mouse RAW 264.7 macrophage-like cells pre-incubated with EC144 for 4 hrs then stimulated with LPS for 8 hrs, quantified by RodentMAP multiplex cytokine array.	21131419
RAW264.7	EC50	14.7 nM	Inhibition of LPS-stimulated GM-CSF production in mouse RAW 264.7 macrophage-like cells pre-incubated with EC144 for 4 hrs then stimulated with LPS for 8 hrs, quantified by RodentMAP multiplex cytokine array. Inhibition of LPS-stimulated GM-CSF production in mouse RAW 264.7 macrophage-like cells pre-incubated with EC144 for 4 hrs then stimulated with LPS for 8 hrs, quantified by RodentMAP multiplex cytokine array.	21131419
RAW264.7	EC50	21.1 nM	Inhibition of LPS-stimulated M-CSF production in mouse RAW 264.7 macrophage-like cells pre-incubated with EC144 for 4 hrs then stimulated with LPS for 8 hrs, quantified by RodentMAP multiplex cytokine array. Inhibition of LPS-stimulated M-CSF production in mouse RAW 264.7 macrophage-like cells pre-incubated with EC144 for 4 hrs then stimulated with LPS for 8 hrs, quantified by RodentMAP multiplex cytokine array.	21131419
RAW264.7	EC50	22.2 nM	Inhibition of LPS-stimulated MMP-9 production in mouse RAW 264.7 macrophage-like cells pre-incubated with EC144 for 4 hrs then stimulated with LPS for 8 hrs, quantified by RodentMAP multiplex cytokine array. Inhibition of LPS-stimulated MMP-9 production in mouse RAW 264.7 macrophage-like cells pre-incubated with EC144 for 4 hrs then stimulated with LPS for 8 hrs, quantified by RodentMAP multiplex cytokine array.	21131419
RAW264.7	EC50	20.1 nM	Inhibition of LPS-stimulated TNF-alpha production in mouse RAW 264.7 macrophage-like cells pre-incubated with EC144 for 4 hrs then stimulated with LPS for 8 hrs, quantified by RodentMAP multiplex cytokine array. Inhibition of LPS-stimulated TNF-alpha production in mouse RAW 264.7 macrophage-like cells pre-incubated with EC144 for 4 hrs then stimulated with LPS for 8 hrs, quantified by RodentMAP multiplex cytokine array.	21131419
RAW264.7	EC50	29.5 nM	Inhibition of LPS-stimulated IL-1alpha production in mouse RAW 264.7 macrophage-like cells pre-incubated with EC144 for 4 hrs then stimulated with LPS for 8 hrs, quantified by RodentMAP multiplex cytokine array. Inhibition of LPS-stimulated IL-1alpha production in mouse RAW 264.7 macrophage-like cells pre-incubated with EC144 for 4 hrs then stimulated with LPS for 8 hrs, quantified by RodentMAP multiplex cytokine array.	21131419
RAW264.7	EC50	20.5 nM	Inhibition of LPS-stimulated IL-6 production in mouse RAW 264.7 macrophage-like cells pre-incubated with EC144 for 4 hrs then stimulated with LPS for 8 hrs, quantified by RodentMAP multiplex cytokine array. Inhibition of LPS-stimulated IL-6 production in mouse RAW 264.7 macrophage-like cells pre-incubated with EC144 for 4 hrs then stimulated with LPS for 8 hrs, quantified by RodentMAP multiplex cytokine array.	21131419
RAW264.7	EC50	19.7 nM	Inhibition of LPS-stimulated IL-10 production in mouse RAW 264.7 macrophage-like cells pre-incubated with EC144 for 4 hrs then stimulated with LPS for 8 hrs, quantified by RodentMAP multiplex cytokine array. Inhibition of LPS-stimulated IL-10 production in mouse RAW 264.7 macrophage-like cells pre-incubated with EC144 for 4 hrs then stimulated with LPS for 8 hrs, quantified by RodentMAP multiplex cytokine array.	21131419
RAW264.7	EC50	40.0 nM	Inhibition of LPS-stimulated IL-11 production in mouse RAW 264.7 macrophage-like cells pre-incubated with EC144 for 4 hrs then stimulated with LPS for 8 hrs, quantified by RodentMAP multiplex cytokine array. Inhibition of LPS-stimulated IL-11 production in mouse RAW 264.7 macrophage-like cells pre-incubated with EC144 for 4 hrs then stimulated with LPS for 8 hrs, quantified by RodentMAP multiplex cytokine array.	21131419
RAW264.7	EC50	17.8 nM	Inhibition of LPS-stimulated LIF production in mouse RAW 264.7 macrophage-like cells pre-incubated with EC144 for 4 hrs then stimulated with LPS for 8 hrs, quantified by RodentMAP multiplex cytokine array. Inhibition of LPS-stimulated LIF production in mouse RAW 264.7 macrophage-like cells pre-incubated with EC144 for 4 hrs then stimulated with LPS for 8 hrs, quantified by RodentMAP multiplex cytokine array.	21131419
RAW264.7	EC50	39.4 nM	Inhibition of LPS-stimulated Oncostatin M production in mouse RAW 264.7 macrophage-like cells pre-incubated with EC144 for 4 hrs then stimulated with LPS for 8 hrs, quantified by RodentMAP multiplex cytokine array. Inhibition of LPS-stimulated Oncostatin M production in mouse RAW 264.7 macrophage-like cells pre-incubated with EC144 for 4 hrs then stimulated with LPS for 8 hrs, quantified by RodentMAP multiplex cytokine array.	21131419
RAW264.7	EC50	42.5 nM	Inhibition of LPS-stimulated SCF production in mouse RAW 264.7 macrophage-like cells pre-incubated with EC144 for 4 hrs then stimulated with LPS for 8 hrs, quantified by RodentMAP multiplex cytokine array. Inhibition of LPS-stimulated SCF production in mouse RAW 264.7 macrophage-like cells pre-incubated with EC144 for 4 hrs then stimulated with LPS for 8 hrs, quantified by RodentMAP multiplex cytokine array.	21131419
RAW264.7	EC50	23.1 nM	Inhibition of LPS-stimulated Tissue factor production in mouse RAW 264.7 macrophage-like cells pre-incubated with EC144 for 4 hrs then stimulated with LPS for 8 hrs, quantified by RodentMAP multiplex cytokine array. Inhibition of LPS-stimulated Tissue factor production in mouse RAW 264.7 macrophage-like cells pre-incubated with EC144 for 4 hrs then stimulated with LPS for 8 hrs, quantified by RodentMAP multiplex cytokine array.	21131419
RAW264.7	EC50	19.8 nM	Inhibition of LPS-stimulated IP-10 production in mouse RAW 264.7 macrophage-like cells pre-incubated with EC144 for 4 hrs then stimulated with LPS for 8 hrs, quantified by RodentMAP multiplex cytokine array. Inhibition of LPS-stimulated IP-10 production in mouse RAW 264.7 macrophage-like cells pre-incubated with EC144 for 4 hrs then stimulated with LPS for 8 hrs, quantified by RodentMAP multiplex cytokine array.	21131419
RAW264.7	EC50	12.7 nM	Inhibition of LPS-stimulated MDC production in mouse RAW 264.7 macrophage-like cells pre-incubated with EC144 for 4 hrs then stimulated with LPS for 8 hrs, quantified by RodentMAP multiplex cytokine array. Inhibition of LPS-stimulated MDC production in mouse RAW 264.7 macrophage-like cells pre-incubated with EC144 for 4 hrs then stimulated with LPS for 8 hrs, quantified by RodentMAP multiplex cytokine array.	21131419
RAW264.7	EC50	20.8 nM	Inhibition of LPS-stimulated MCP-1 production in mouse RAW 264.7 macrophage-like cells pre-incubated with EC144 for 4 hrs then stimulated with LPS for 8 hrs, quantified by RodentMAP multiplex cytokine array. Inhibition of LPS-stimulated MCP-1 production in mouse RAW 264.7 macrophage-like cells pre-incubated with EC144 for 4 hrs then stimulated with LPS for 8 hrs, quantified by RodentMAP multiplex cytokine array.	21131419
RAW264.7	EC50	24.0 nM	Inhibition of LPS-stimulated MCP-3 production in mouse RAW 264.7 macrophage-like cells pre-incubated with EC144 for 4 hrs then stimulated with LPS for 8 hrs, quantified by RodentMAP multiplex cytokine array. Inhibition of LPS-stimulated MCP-3 production in mouse RAW 264.7 macrophage-like cells pre-incubated with EC144 for 4 hrs then stimulated with LPS for 8 hrs, quantified by RodentMAP multiplex cytokine array.	21131419
RAW264.7	EC50	22.1 nM	Inhibition of LPS-stimulated MIP-1alpha production in mouse RAW 264.7 macrophage-like cells pre-incubated with EC144 for 4 hrs then stimulated with LPS for 8 hrs, quantified by RodentMAP multiplex cytokine array. Inhibition of LPS-stimulated MIP-1alpha production in mouse RAW 264.7 macrophage-like cells pre-incubated with EC144 for 4 hrs then stimulated with LPS for 8 hrs, quantified by RodentMAP multiplex cytokine array.	21131419
RAW264.7	EC50	21.4 nM	Inhibition of LPS-stimulated MIP-1beta production in mouse RAW 264.7 macrophage-like cells pre-incubated with EC144 for 4 hrs then stimulated with LPS for 8 hrs, quantified by RodentMAP multiplex cytokine array. Inhibition of LPS-stimulated MIP-1beta production in mouse RAW 264.7 macrophage-like cells pre-incubated with EC144 for 4 hrs then stimulated with LPS for 8 hrs, quantified by RodentMAP multiplex cytokine array.	21131419
RAW264.7	EC50	21.7 nM	Inhibition of LPS-stimulated MIP-3beta production in mouse RAW 264.7 macrophage-like cells pre-incubated with EC144 for 4 hrs then stimulated with LPS for 8 hrs, quantified by RodentMAP multiplex cytokine array. Inhibition of LPS-stimulated MIP-3beta production in mouse RAW 264.7 macrophage-like cells pre-incubated with EC144 for 4 hrs then stimulated with LPS for 8 hrs, quantified by RodentMAP multiplex cytokine array.	21131419
RAW264.7	EC50	23.0 nM	Inhibition of LPS-stimulated RANTES production in mouse RAW 264.7 macrophage-like cells pre-incubated with EC144 for 4 hrs then stimulated with LPS for 8 hrs, quantified by RodentMAP multiplex cytokine array. Inhibition of LPS-stimulated RANTES production in mouse RAW 264.7 macrophage-like cells pre-incubated with EC144 for 4 hrs then stimulated with LPS for 8 hrs, quantified by RodentMAP multiplex cytokine array.	21131419
RAW264.7	EC50	25.2 nM	Inhibition of LPS-stimulated TIMP-1 production in mouse RAW 264.7 macrophage-like cells pre-incubated with EC144 for 4 hrs then stimulated with LPS for 8 hrs, quantified by RodentMAP multiplex cytokine array. Inhibition of LPS-stimulated TIMP-1 production in mouse RAW 264.7 macrophage-like cells pre-incubated with EC144 for 4 hrs then stimulated with LPS for 8 hrs, quantified by RodentMAP multiplex cytokine array.	21131419
BMDM	IC50	99 nM	Inhibition of LPS and nigericin-induced ASC speck formation in ASC-mCherry-expressing immortalized bone marrow-derived macrophages when added together with LPS during priming, measured by imaging with a GE IN Cell Analyzer 6000. Inhibition of LPS and nigericin-induced ASC speck formation in ASC-mCherry-expressing immortalized bone marrow-derived macrophages when added together with LPS during priming, measured by imaging with a GE IN Cell Analyzer 6000.	32954500
BMDM	IC50	170 nM	Inhibition of LPS and nigericin-induced ASC speck formation in ASC-mCherry-expressing immortalized bone marrow-derived macrophages when added after LPS before nigericin activation, measured by imaging with a GE IN Cell Analyzer 6000. Inhibition of LPS and nigericin-induced ASC speck formation in ASC-mCherry-expressing immortalized bone marrow-derived macrophages when added after LPS before nigericin activation, measured by imaging with a GE IN Cell Analyzer 6000.	32954500
BMDM	IC50	150 nM	Inhibition of LPS and nigericin-induced caspase-1 activation in ASC-mCherry-expressing immortalized bone marrow-derived macrophages assessed by caspase-1 Glo assay. Inhibition of LPS and nigericin-induced caspase-1 activation in ASC-mCherry-expressing immortalized bone marrow-derived macrophages assessed by caspase-1 Glo assay.	32954500
MCF7	EC50	14 nM	Induction of Her-2 degradation in human MCF-7 breast cancer cells monitored with extracellular-directed fluorescent antibodies and flow cytometry. Induction of Her-2 degradation in human MCF-7 breast cancer cells monitored with extracellular-directed fluorescent antibodies and flow cytometry.	22938030

In Vitro

Anti-cancerCytokines & ChemokinesPyroptosisInflammasomeInnate ImmunityViral InfectionOthers

Anti-cancer

EC144 (16 h) inhibits Hsp90 in MCF-7 cells, inducing HER2 degradation with an EC₅₀ of 6.5 nM^[1].
EC144 induces Her-2 degradation in MCF-7 breast cancer cells with an EC₅₀ of 14 nM^[5].

Cytokines & Chemokines

Pyroptosis

EC144 (10 µM; 2 h + 2 h) inhibits NLRP3 inflammasome-dependent IL-1β secretion and pyroptotic cell death in iBMDMs^[3].

Inflammasome

EC144 inhibits NLRP3 inflammasome-dependent ASC speck formation in iBMDMs, acting primarily on the priming stage, with an IC₅₀ of 99 nM when present during LPS priming^[3].

Inflammasome

Innate Immunity

Cytokines & Chemokines

EC144 inhibits NLRP3 inflammasome assembly and prevents IL-1β secretion in bone marrow-derived macrophages with an IC₅₀ of 99 nM^[2].

Innate Immunity

EC144 (4-1000 nM; 4 h) inhibits LPS-induced activation of the MAPK pathways (ERK1/2, JNK1/2, and MEK1/2) in RAW 264.7 cells^[1].
EC144 (1-10 μM; 4 h) in RAW 264.7 cells, Hsp90 inhibition does not alter LPS-dependent activation of NF-κB p50^[1].

Innate Immunity

Cytokines & Chemokines

EC144 (4 h) inhibits LPS-stimulated TNF-α and IL-6 production in RAW 264.7 cells with an EC₅₀ of approximately 20 nM^[1].
EC144 (4 h) broadly inhibits LPS-induced production of multiple cytokines and chemokines in RAW 264.7 cells, with EC₅₀ values ranging from 12.7 to 45.4 nM^[1].

Innate Immunity

Inflammasome

Cytokines & Chemokines

EC144 (1 µM; 15 min + 4 h) inhibits LPS-induced priming in primary mouse BMDMs, reducing NLRP3 and pro-IL-1β expression and IL-6 production, independently of HSP70 induction^[3].

Pyroptosis

Inflammasome

EC144 inhibits NLRP3 inflammasome-dependent caspase-1 activation in iBMDMs with an IC₅₀ of 150 nM^[3].

Viral Infection

HSP90 inhibition by EC144 (1 μM; 24 h) in Huh7 WNV replicon cells alters the localization of NS1 and dsRNA relative to NS3 and NS5^[4].
EC144-mediated HSP90 inhibition (1 μM; 12-24 h) increases WNV replicon genomic RNA abundance and induces HSP70A mRNA in Huh7 WNV replicon cells^[4].
EC144 (1 μM; 12-24 h) inhibits HSP90 activity in Huh7 WNV replicon cells, leading to reduced abundance of HSP90 client kinases without affecting viral NS protein abundance^[4].
EC144 (1 μM; 12 h) inhibits HSP90 activity during WNV-TX infection in Vero cells, reducing the abundance of HSP90 client kinases without decreasing viral protein levels^[4].
EC144 (1 μM; 12 h) inhibits HSP90 activity during ZIKV Fortaleza infection in Vero cells, reducing the abundance of HSP90 client kinases without decreasing viral protein levels^[4].

Others

EC144 is a potent and selective inhibitor of cytoplasmic Hsp90, with a K_i of 0.2 nM, demonstrating selectivity over Grp94 and TRAP-1^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:

RAW 264.7
Concentration:

1000, 333, 111, 37, 12, 4 nM
Incubation Time:

4 h (pre-incubation); 30 min
Result:

Resulted in a dose-dependent decrease of phospho-ERK1/2 and phospho-JNK1/2.
Levels of phospho-p38 MAPK were also mildly decreased.
Markedly decreased MEK1/2 phosphorylation in a dose-dependent manner but did not alter levels of total MEK1/2, ERK1/2, JNK1/2, or p38 MAPK.

ELISA Assay^[1]

Cell Line:

RAW 264.7
Concentration:

10 or 1 μM
Incubation Time:

4 h (pre-incubation); 30 min
Result:

No decrease in NF-κB p50 binding activity relative to DMSO-treated, LPS-stimulated control cells was found.

Real Time qPCR^[3]

Cell Line:

Rat nucleus pulposus cells (NPCs)
Concentration:

100-500 nM
Incubation Time:

36 h
Result:

Partially reversed the M1-CM-induced elevated levels of Il1b, Il6, Tnf, Ccl2, and Ccl5.\nMarkedly decreased the mRNA levels of Mmp2, Mmp3, Mmp9, and Mmp13.
Prevented the M1-CM-induced decline of Col2a1 levels.

Western Blot Analysis^[3]

Cell Line:

Rat nucleus pulposus cells (NPCs)
Concentration:

100-500 nM
Incubation Time:

36 h
Result:

Dose-dependently increased the expression of HSP70.
Did not dramatically modify the levels of HSP90α and HSP90β.\nImpeded the activation of the JAK2-STAT3 pathway.
Confirmed that JAK2 and STAT3 specifically interacted with molecular chaperone HSP90.

ELISA Assay^[4]

Cell Line:

ASC-mCherry iBMDMs
Concentration:

10 µM
Incubation Time:

2 h (LPS) + 2 h (nigericin)
Result:

Inhibited both IL-1β release and cell death.

Immunofluorescence^[5]

Cell Line:

Huh7 WNV replicon cells
Concentration:

1 μM
Incubation Time:

24 h
Result:

Altered the localization of NS1 and dsRNA relative to NS3 and NS5, causing NS1 and dsRNA to shift from co-localization with the NS proteins to distribute as bright foci directly adjacent to NS3 and NS5.

Real Time qPCR^[5]

Cell Line:

Huh7 WNV replicon cells
Concentration:

1 μM
Incubation Time:

12-24 h
Result:

Significantly increased WNV replicon genomic RNA (gRNA) abundance by 24 h.
Significantly induced HSP70A mRNA.

Western Blot Analysis^[5]

Cell Line:

Huh7 WNV replicon cells
Concentration:

1 μM
Incubation Time:

12-24 h
Result:

Caused reduced abundance of the HSP90 client kinases Akt and ErbB2, but did not cause a decrease in replicon NS proteins.

Western Blot Analysis^[5]

Cell Line:

Vero cells infected with WNV-TX
Concentration:

1 μM
Incubation Time:

12 h
Result:

Decreased Akt and ErbB2 abundance, though little change to viral proteins (WNV E, NS1, NS5) was detected.

Western Blot Analysis^[5]

Cell Line:

Vero cells infected with ZIKV Fortaleza
Concentration:

1 μM
Incubation Time:

12 h
Result:

Decreased Akt and ErbB2 abundance, though little change to viral proteins (ZIKV E, NS1, NS3, NS5) was detected.
Quantification of band intensity showed that ZIKV protein levels did not decrease during HSP90 inhibition.

Parmacokinetics

Species	Dose	Route	C_max	T_max	AUC	T_1/2	Plasma Concentration	Brain Concentration	T_max (Plasma)	AUC_inf	T_1/2 (Plasma)
Mice^[1]	5 mg/kg	p.o.	835.3 ng/mL	/	/	/	/	/	1 h	2135.6 ng·h/mL	1.5 h
Rat^[1]	5 mg/kg	p.o.	/	/	/	5 h	/	/	/	/	/
Mice^[4]	30 mg/kg	p.o.	/	/	/	/	85 ng/mL	1293 ng/g	/	/	/
Mice^[6]	25 mg/kg	p.o.	1556 ng/mL	0.5 h	4419 ng·h/mL	1.5 h	/	/	/	/	/

In Vivo

Adaptive ImmunityCytokines & ChemokinesInnate ImmunityOthers

Adaptive Immunity

Cytokines & Chemokines

EC144 (0.5-5 mg/kg; p.o.; daily or every third day) dose-dependently ameliorates disease in a rat collagen-induced arthritis (CIA) model and blocks proinflammatory cytokine production^[1].
EC144 (5-10 mg/kg; p.o.; every other day) dose-dependently decreases disease severity in mouse CIA and suppresses the Ag-specific Ab response^[1].

Innate Immunity

EC144 (10-30 mg/kg; p.o.) is effective in vivo at a minimal effective dose of 10 mg/kg, where it completely inhibits inflammasome-dependent IL-1β release and reduces IL-6 levels in a murine peritonitis model^[3].

Innate Immunity

Cytokines & Chemokines

EC144 (2.5-10 mg/kg; p.o.; two gavages given 3 h apart) dose-dependently attenuates LPS-induced serum TNF-α production in mice^[1].
In vivo EC144 (10 mg/kg; p.o.; once daily; 3 days) treatment blocks activation of the Tpl2/MEK1/2/ERK1/2 pathway in LPS-stimulated primary CD11b⁺ PECs in mice^[1].

Others

EC144 (compound 40) (30 mg/kg; p.o.; single dose) inhibits Hsp90 in the brains of mice, as evidenced by up-regulation of brain Hsp70^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

DBA/1 (female)^[1]
Dosage:

2.5, 5, and 10 mg/kg
Administration:

p.o.; two gavages given 3 h apart
Result:

Produced a significant decrease in serum TNF-α induction at 2.5, 5, and 10 mg/kg.

Animal Model:

DA (female)^[1]
Dosage:

1.5 mg/kg (daily); 0.5 mg/kg (daily); 5 mg/kg (every third day); 1.5 mg/kg (every third day)
Administration:

p.o.; daily or every third day; starting on day 12
Result:

Developed little or no disease symptoms at 1.5 mg/kg daily or 5 mg/kg every third day.
Completely abrogated expression of mRNAs of proinflammatory cytokines TNF-α, IL-1β, and IL-6 at 5 mg/kg every third day.

Animal Model:

DBA/1 LacJ (female)^[1]
Dosage:

5, 8, and 10 mg/kg
Administration:

p.o.; every other day; beginning on day 21
Result:

Reduced disease incidence from 90 to 60% and reduced disease severity from a clinical score of 12 to 4 at 8 or 10 mg/kg.
Significantly decreased anti-chicken CII IgG1 and IgG2a levels at 8 mg/kg.
Showed minimal joint inflammation and an absence of cartilage and synovial lining damage and bone erosion at 10 mg/kg.

Animal Model:

DBA/1 (female) bearing acute systemic inflammation^[1]
Dosage:

10 mg/kg
Administration:

p.o.; once daily; 3 days
Result:

Dramatically lower levels of phospho-MEK1/2 and phospho-ERK1/2 in LPS-stimulated CD11b+ PECs.
Phosphorylated Tpl2 was not detected in LPS-stimulated CD11b+ PECs.

Animal Model:

C57BL6/J (male, 8-10 weeks old)^[4]
Dosage:

10-30 mg/kg; 0.1-10 mg/kg (repeat experiment)
Administration:

p.o.; single dose
Result:

Completely inhibited inflammasome-dependent IL-1β release at 10, 20, and 30 mg/kg.
Reduced IL-6 levels at 10, 20, and 30 mg/kg.
Achieved plasma concentrations of 46 ng/mL, 69 ng/mL, and 85 ng/mL for 10, 20, and 30 mg/kg doses, respectively.
Achieved brain concentrations of 448 ng/g, 1313 ng/g, and 1293 ng/g for 10, 20, and 30 mg/kg doses, respectively.
Was ineffective at 0.1 or 1 mg/kg and had a minimal effective dose of 10 mg/kg.

Animal Model:

B6D2F1 (female)^[6]
Dosage:

30 mg/kg
Administration:

p.o.; single dose
Result:

Significantly increased Hsp70 levels in whole brain homogenates at 30 mg/kg or higher compared to vehicle.

Related Protocols :

Chemical Information

CAS. Nr. 911397-80-3
Appearance Solid
Molecular Weight 413.90
Formel C₂₁H₂₄ClN₅O₂
Color Light brown to brown
SMILES

CC(O)(C)CC#CC1=CN(CC2=NC=C(C)C(OC)=C2C)C3=NC(N)=NC(Cl)=C31
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture and light

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 66.67 mg/mL (161.08 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.4160 mL

12.0802 mL

24.1604 mL

5 mM

0.4832 mL

2.4160 mL

4.8321 mL

10 mM

0.2416 mL

1.2080 mL

2.4160 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (6.04 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (6.04 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (315 KB)
SDS (252 KB)
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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Yun TJ, et al. EC144, a synthetic inhibitor of heat shock protein 90, blocks innate and adaptive immune responses in models of inflammation and autoimmunity. Journal of immunology (Baltimore, Md. : 1950). 2011 Jan 01;186(1):563-75.

[2]. Jha D, et al. Mechanistic and therapeutic role of NLRP3 inflammasome in the pathogenesis of Alzheimer's disease. Journal of neurochemistry. 2024 Oct;168(10):3574-3598.

[3]. Nizami S, et al. Inhibition of the NLRP3 inflammasome by HSP90 inhibitors. Immunology. 2021 Jan;162(1):84-91. [Content Brief]

[4]. Roby JA, et al. Flavivirus Nonstructural Protein NS5 Dysregulates HSP90 to Broadly Inhibit JAK/STAT Signaling. Cells. 2020 Apr 07;9(4):899.

[5]. Shi J, et al. EC144 is a potent inhibitor of the heat shock protein 90. Journal of medicinal chemistry. 2012 Sep 13;55(17):7786-95. [Content Brief]

[6]. Sugawara Y, et al. Botulinum hemagglutinin disrupts the intercellular epithelial barrier by directly binding E-cadherin. The Journal of cell biology. 2010 May 17;189(4):691-700.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.4160 mL	12.0802 mL	24.1604 mL	60.4011 mL
	5 mM	0.4832 mL	2.4160 mL	4.8321 mL	12.0802 mL
	10 mM	0.2416 mL	1.2080 mL	2.4160 mL	6.0401 mL
	15 mM	0.1611 mL	0.8053 mL	1.6107 mL	4.0267 mL
	20 mM	0.1208 mL	0.6040 mL	1.2080 mL	3.0201 mL
	25 mM	0.0966 mL	0.4832 mL	0.9664 mL	2.4160 mL
	30 mM	0.0805 mL	0.4027 mL	0.8053 mL	2.0134 mL
	40 mM	0.0604 mL	0.3020 mL	0.6040 mL	1.5100 mL
	50 mM	0.0483 mL	0.2416 mL	0.4832 mL	1.2080 mL
	60 mM	0.0403 mL	0.2013 mL	0.4027 mL	1.0067 mL
	80 mM	0.0302 mL	0.1510 mL	0.3020 mL	0.7550 mL
	100 mM	0.0242 mL	0.1208 mL	0.2416 mL	0.6040 mL

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EC144

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