2. Cell Cycle/DNA Damage Metabolic Enzyme/Protease
  3. HSP
  4. EV206

EV206 is a Hsp70 binder and apoptosis inducer that binds to the N-terminal domain of Hsp70, promotes Hsp70 degradation via the ubiquitin-proteasome system, and reduces Hsp70 protein stability. EV206 induces apoptotic cell death, inhibits colony formation, and downregulates the expression of cancer stem cell-related markers in non-small cell lung cancer cells. EV206 inhibits the growth of H460 xenograft tumors in nude mice and can be used for the research of non-small cell lung cancer.

For research use only. We do not sell to patients.

EV206

EV206 Chemical Structure

CAS No. : 2247047-81-8

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 1 publication(s) in Google Scholar

EV206 Related Antibodies

Top Publications Citing Use of Products

View All HSP Isoform Specific Products:

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HSP40 HSP70 HSP90 HSP105 HSF1 HSP HSPA5

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Description

EV206 is a Hsp70 binder and apoptosis inducer that binds to the N-terminal domain of Hsp70, promotes Hsp70 degradation via the ubiquitin-proteasome system, and reduces Hsp70 protein stability. EV206 induces apoptotic cell death, inhibits colony formation, and downregulates the expression of cancer stem cell-related markers in non-small cell lung cancer cells. EV206 inhibits the growth of H460 xenograft tumors in nude mice and can be used for the research of non-small cell lung cancer[1].

IC50 & Target

HSP70

 

Cellular Effect
Cell Line Type Value Description References
HGC-27 IC50
1.05 μM
Compound: 6k
Antiproliferative activity against human HGC-27 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human HGC-27 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 37099835]
LoVo IC50
1 μM
Compound: 6k
Antiproliferative activity against human LoVo cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human LoVo cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 37099835]
MGC-803 IC50
0.06 μM
Compound: 6k
Antiproliferative activity against human MGC-803 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human MGC-803 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 37099835]
RKO IC50
0.38 μM
Compound: 6k
Antiproliferative activity against human RKO cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human RKO cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 37099835]
SGC-7901 IC50
0.27 μM
Compound: 6k
Antiproliferative activity against human SGC-7901 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human SGC-7901 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 37099835]
SW480 IC50
0.38 μM
Compound: 6k
Antiproliferative activity against human SW480 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human SW480 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 37099835]
In Vitro

EV206 (1-10 μM; 30 min at 4°C) binds directly to the full-length Hsp70 protein and its N-terminal domain, but not the C-terminal domain[1].
EV206 (up to 250 μM; equilibrated at 20°C) exhibits a higher binding affinity for the Hsp70 N-terminal domain (Kd = 16.60 μM) than for the C-terminal domain (Kd = 42.27 μM) in a fluorescence-based equilibrium binding assay[1].
EV206 (0.05-0.5 μM; 48 h) inhibits the viability of therapy-naïve H1299, A549, H460, H226B, and PC9 NSCLC cells with IC50 values below 0.5 μM after 48 h treatment, as measured by a crystal violet assay[1].
EV206 (0.05-0.5 μM; 48 h) inhibits the viability of drug-resistant H1299/CsR, H1299/PmR, H460/PcR, H226B/PcR, and PC9/ER NSCLC cells with IC50 values below 0.5 μM after 48 h treatment, as measured by a crystal violet assay[1].
EV206 (0.05-0.5 μM; 2-3 week culture) dose-dependently inhibits anchorage-dependent colony formation in H1299, A549, H460, H226B, and PC9 NSCLC cells[1].
EV206 (0.1-0.5 μM; 2-3 week culture) dose-dependently inhibits anchorage-independent colony formation in H1299, A549, H460, H226B, and PC9 NSCLC cells[1].
EV206 (0.1-0.5 μM; 48 h) dose-dependently induces apoptotic cell death (measured by increased sub-G1 population) in H1299, A549, H460, H226B, and PC9 NSCLC cells[1].
EV206 (0.1-0.5 μM; 48 h) dose-dependently induces apoptosis in H1299, A549, H460, H226B, and PC9 NSCLC cells, as shown by increased cleaved PARP and cleaved caspase-3 levels[1].
EV206 (0.1-0.5 μM; 48 h) dose-dependently reduces Hsp70 and Akt protein levels, but not Hsp90 protein levels, in H1299, A549, and H460 NSCLC cells[1].
EV206 (0.1-0.25 μM; 48 h) reduces Hsp70 protein stability in H460 NSCLC cells via the ubiquitin-proteasome system, as shown by the reversal of Hsp70 downregulation when co-treated with the proteasome inhibitor MG132 (10 μM for 6 h)[1].
EV206 (0.05-0.25 μM; 2-3 week culture) dose-dependently inhibits sphere formation (a marker of CSC-like phenotype) in H1299, A549, and H460 NSCLC cells[1].
EV206 (0.05-0.25 μM; 48 h) reduces aldehyde dehydrogenase (ALDH) activity, a marker of CSC-like phenotype, in H460 NSCLC cells[1].
EV206 (0.1 μM; during sphere culture) significantly downregulates the mRNA expression of CSC-associated markers POU5F1, NANOG, and SOX2 in H460 NSCLC spheres[1].

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

EV206 Related Antibodies

Cell Viability Assay[1]

Cell Line: Therapy-naïve NSCLC cell lines (H1299, H460, A549, H226B, PC9)
Concentration: 0.05, 0.1, 0.5 μM
Incubation Time: 48 h
Result: Potently inhibited cell viability across all tested therapy-naïve NSCLC cell lines, with IC50 values of 0.35 μM (H1299), 0.23 μM (A549), 0.31 μM (H460), 0.38 μM (H226B), and 0.46 μM (PC9).

Cell Viability Assay[1]

Cell Line: Drug-resistant NSCLC cell lines (H1299/CsR, H1299/PmR, H460/PcR, H226B/PcR, PC9/ER)
Concentration: 0.05, 0.1, 0.5 μM
Incubation Time: 48 h
Result: Dose-dependently inhibited cell viability across all tested drug-resistant NSCLC cell lines, with IC50 values of 0.30 μM (H1299/CsR), 0.20 μM (H1299/PmR), 0.35 μM (H460/PcR), 0.30 μM (H226B/PcR), and 0.46 μM (PC9/ER).

Cell Proliferation Assay[1]

Cell Line: Therapy-naïve NSCLC cell lines (H1299, A549, H460, H226B, PC9)
Concentration: 0.05, 0.1, 0.5 μM
Incubation Time: 2-3 week culture
Result: Dose-dependently suppressed colony formation in all tested therapy-naïve NSCLC cell lines, with significant inhibition observed at all tested concentrations.

Cell Proliferation Assay[1]

Cell Line: Therapy-naïve NSCLC cell lines (H1299, A549, H460, H226B, PC9)
Concentration: 0.1, 0.25, 0.5 μM
Incubation Time: 2-3 week culture
Result: Dose-dependently suppressed soft agar colony formation in all tested therapy-naïve NSCLC cell lines, with significant inhibition observed at all tested concentrations.

Western Blot Analysis[1]

Cell Line: Therapy-naïve NSCLC cell lines (H1299, A549, H460)
Concentration: 0.1, 0.25, 0.5 μM
Incubation Time: 48 h
Result: Dose-dependently decreased Hsp70 and Akt protein levels across all tested therapy-naïve NSCLC cell lines.
Did not alter Hsp90 protein levels across all tested therapy-naïve NSCLC cell lines.

Western Blot Analysis[1]

Cell Line: H460 NSCLC cells
Concentration: 0.1, 0.25 μM (EV206); 10 μM (MG132)
Incubation Time: 48 h (EV206); final 6 h (MG132)
Result: Induced downregulation of Hsp70 protein levels in H460 cells.
Had this effect significantly blunted by co-treatment with MG132, indicating the effect is mediated via the ubiquitin-proteasome system.

Real Time qPCR[1]

Cell Line: H460 NSCLC spheres
Concentration: 0.1 μM
Incubation Time: during sphere culture
Result: Caused a marked decrease in the mRNA expression of POU5F1 (Oct4), NANOG, and SOX2, all CSC-associated markers.
In Vivo

EV206 (10 mg/kg; i.p.; every other day; 16 days) significantly inhibits H460 NSCLC xenograft tumor growth in Balb/c nude mice without causing detectable weight loss[1].

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

Animal Model: Balb/c nude (6-week-old; male and female; H460 NSCLC xenograft model)[1]
Dosage: 10 mg/kg
Administration: i.p.; every other day; 16 days
Result: Inhibited H460 tumor xenograft growth.
Showed no significant changes in mouse body weight relative to vehicle controls.
Molecular Weight

329.40

Formula

C21H19N3O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1C2=C(C=CC=C2)N(CC=C)C(N1CC3)C4=C3C5=CC=CC=C5N4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (151.79 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.0358 mL 15.1791 mL 30.3582 mL
5 mM 0.6072 mL 3.0358 mL 6.0716 mL
View the Complete Stock Solution Preparation Table

* 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.62%

SDS (252 KB)

COA (256 KB) HNMR (266 KB) LCMS (93 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.0358 mL 15.1791 mL 30.3582 mL 75.8956 mL
5 mM 0.6072 mL 3.0358 mL 6.0716 mL 15.1791 mL
10 mM 0.3036 mL 1.5179 mL 3.0358 mL 7.5896 mL
15 mM 0.2024 mL 1.0119 mL 2.0239 mL 5.0597 mL
20 mM 0.1518 mL 0.7590 mL 1.5179 mL 3.7948 mL
25 mM 0.1214 mL 0.6072 mL 1.2143 mL 3.0358 mL
30 mM 0.1012 mL 0.5060 mL 1.0119 mL 2.5299 mL
40 mM 0.0759 mL 0.3795 mL 0.7590 mL 1.8974 mL
50 mM 0.0607 mL 0.3036 mL 0.6072 mL 1.5179 mL
60 mM 0.0506 mL 0.2530 mL 0.5060 mL 1.2649 mL
80 mM 0.0379 mL 0.1897 mL 0.3795 mL 0.9487 mL
100 mM 0.0304 mL 0.1518 mL 0.3036 mL 0.7590 mL
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EV206 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

EV2062247047-81-8EV 206EV-206HSPHeat shock proteinsHsp70non-small cell lung cancer cellsaldehyde dehydrogenaseapoptosisNANOGcancer stem cellsH460 xenograft tumorsnude miceubiquitin-proteasome systemPOU5F1Inhibitorinhibitorinhibit

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