HR-19011

Name: HR-19011
Brand: MedChemExpress
SKU: HY-147831
Rating: 4.5 (1 reviews)

Cat. No.: HY-147831 Purity: 99.64%: Data Sheet
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HR-19011 is an eIF2α phosphorylation activator targeting heme-regulated inhibitor HRI (EIF2AK1). HR-19011 exhibits growth inhibitory activity against K562 cells with an IC₅₀ value of 3.91 µM. HR-19011 inhibits the growth of hematologic malignancies by targeting HRI to activate the integrated stress response via the HRI-eIF2α-ATF4 axis. HR-19011 shows good safety in vivo. HR-19011 can be used for research on hematologic malignancies (leukemia).

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

HR-19011 Chemical Structure

CAS No. : 2851820-52-3

Size	Stock	Quantity

Free Sample (0.1 - 0.2 mg)	Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

IC₅₀ & Target

eIF2

Cellular Effect

Cell Line	Type	Value	Description	References
K562	IC₅₀	4 μM Compound: 40	Antiproliferative activity against human K562 cells incubated for 72 hrs by CCK8 assay Antiproliferative activity against human K562 cells incubated for 72 hrs by CCK8 assay	[PMID: 35716517]
PBMC	IC₅₀	19.3 μM Compound: 40	Antiproliferative activity against human PBMC cells incubated for 72 hrs by CCK8 assay Antiproliferative activity against human PBMC cells incubated for 72 hrs by CCK8 assay	[PMID: 35716517]

In Vitro

HR-19011 (compound 40) (1.25-20 μM, 72 h) shows an anticancer activity with IC₅₀ values of 4 and 19.3 μM in K562 and human peripheral blood mononuclear cells (PBMC) cell, shows a strong cancer cell selectivity with a SI value of 4.83 in PBMC cells^[1].
HR-19011 (0-10 μM, 24 h) activate eIF2α phosphorylation in an eIF2α/ATF4/CHOP pathway-dependent manner in K562 cells^[1].
HR9011 exhibits cell growth inhibitory activity with an IC₅₀ value of 3.91 µM in K562 cells transfected with nontargeting control shRNA, while the IC₅₀ value increases to 8.03 µM in K562 cells stably transfected with HRI-specific shRNA^[1].

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

Western Blot Analysis^[1]

Cell Line:	K562 cells
Concentration:	0, 2.5, 5 and 10 μM
Incubation Time:	24 h
Result:	Significantly increased the phosphorylation levels of eIF2α in a dose dependent manner. Upregulated the expression of the downstream effector proteins ATF4 and CHOP.

In Vivo

HR9011 (i.p., one week) demonstrates good safety n Balb/c mice, with no significant tissue damage, body weight loss, or mortality observed and exhibits significant antitumor activity in tumor-inducing mouse models ^[2].

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

Molecular Weight

523.43

Formula

C₂₅H₁₉F₆N₃O₃

CAS No.

2851820-52-3

Appearance

Solid

Color

White to yellow

SMILES

N#CC1=CC(C(F)(F)F)=CC(NC2=C(C(C2=O)=O)N[C@@H]3CC[C@@H](OC4=CC=C(C=C4)C(F)(F)F)CC3)=C1

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 : 25 mg/mL (47.76 mM; ultrasonic and warming and heat to 60°C; 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	1.9105 mL	9.5524 mL	19.1048 mL
5 mM	0.3821 mL	1.9105 mL	3.8210 mL
10 mM	0.1910 mL	0.9552 mL	1.9105 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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.64%

Select Batch:

Data Sheet (277 KB) SDS (251 KB)

COA (253 KB) HNMR (132 KB) RP-HPLC (162 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[1]. Jinsook Kwak, et al. A bioisosteric approach to the discovery of novel N-aryl-N'-[4-(aryloxy)cyclohexyl]squaramide-based activators of eukaryotic initiation factor 2 alpha (eIF2α) phosphorylation. Eur J Med Chem. 2022 May 29;239:114501. [Content Brief]

[2]. Min Jung Kim, et al. A Novel eIF2α-Phosphorylating Agent HR-19011 Exhibits Cell Growth Inhibitory Effects in K562 Cells through Hri Activation. Blood. Volume 144, Supplement 1, 5 November 2024, Page 7469

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.9105 mL	9.5524 mL	19.1048 mL	47.7619 mL
	5 mM	0.3821 mL	1.9105 mL	3.8210 mL	9.5524 mL
	10 mM	0.1910 mL	0.9552 mL	1.9105 mL	4.7762 mL
	15 mM	0.1274 mL	0.6368 mL	1.2737 mL	3.1841 mL
	20 mM	0.0955 mL	0.4776 mL	0.9552 mL	2.3881 mL
	25 mM	0.0764 mL	0.3821 mL	0.7642 mL	1.9105 mL
	30 mM	0.0637 mL	0.3184 mL	0.6368 mL	1.5921 mL
	40 mM	0.0478 mL	0.2388 mL	0.4776 mL	1.1940 mL

HR-19011 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:

HR-190112851820-52-3HR19011HR 19011Eukaryotic Initiation Factor (eIF)Epigenetic Reader DomainK562PBMCEukaryotic initiation factor 2eIF2αAnticancer activityATFCHOPInhibitorinhibitorinhibit

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HR-19011

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