Grp94 Inhibitor-1

Name: Grp94 Inhibitor-1
Brand: MedChemExpress
SKU: HY-112910
Rating: 5.0 (2 reviews)

Cat. No.: HY-112910 Purity: 98.72%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Grp94 Inhibitor-1 is a potent, selective Grp94 inhibitor with an IC₅₀ value of 2 nM, and over 1000-fold selectivity to Grp94 against Hsp90α.

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

Grp94 Inhibitor-1 Chemical Structure

CAS No. : 2234897-35-7

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 55	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 55	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 50	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 70	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 195	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 300	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 2 publication(s) in Google Scholar

2 Publications Citing Use of MCE Grp94 Inhibitor-1

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HSP40 HSP70 HSP90 HSP105 HSF1 HSP HSPA5

Biological Activity
Purity & Documentation
References
Customer Review

Description

Grp94 Inhibitor-1 is a potent, selective Grp94 inhibitor with an IC₅₀ value of 2 nM, and over 1000-fold selectivity to Grp94 against Hsp90α^[1].

IC₅₀ & Target^[1]

GRP94

2 nM (IC₅₀)

In Vitro

Grp94-specific clients include a subset of integrin subunits such as integrin α2 and integrin αL. Their maturation and trafficking to the cell surface are dependent on the Grp94 chaperone function but have no association with cytoplasmic Hsp90α.
Grp94 Inhibitor-1 (1-5 μM; 36 hours) significantly downregulated the cell surface expression levels of integrin α2 and integrin αL in a dose-dependent manner in panc1 cells^[1].

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

Western Blot Analysis^[1]

Cell Line:	Panc1 cells
Concentration:	1 μM; 2.5 μM; 5 μM
Incubation Time:	36 hours
Result:	Decreased integrin α2 and integrin αL protein expression.

In Vivo

Grp94 Inhibitor-1 (intraperitoneal injection,qid.; coadminbistration 10 mg/kg or 30 mg/kg; 8 days) does not attenuate the colon shortening, but decreases disease activity index (DAI) scores. It also TNFα and IL-6 levels in the serum and colonic tissues and significantly reduces the p65 expression in colonic tissues, especially those in the 30 mg/kg dose group^[1].

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

Animal Model:	C57BL/6 mice (male, 20-22 g)^[1]
Dosage:	10 mg/kg or 30 mg/kg
Administration:	Intraperitoneal injection,qid.; coadminbistration 10 mg/kg or 30 mg/kg
Result:	Decreased disease activity index (DAI) scores in UC mices.

Molecular Weight

352.47

Formula

C₂₂H₂₈N₂O₂

CAS No.

2234897-35-7

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=CC(C2=CC=C(C(C)C)C=C2)=CC=C1N[C@H]3CC[C@H](O)CC3)N

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 250 mg/mL (709.28 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	2.8371 mL	14.1856 mL	28.3712 mL
5 mM	0.5674 mL	2.8371 mL	5.6742 mL
10 mM	0.2837 mL	1.4186 mL	2.8371 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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: ≥ 2.08 mg/mL (5.90 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (5.90 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (5.90 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 98.72%

Select Batch:

Data Sheet (277 KB) SDS (251 KB)

COA (251 KB) LCMS (104 KB)

Handling Instructions (2659 KB)

References

[1]. Jiang F, et al. Discovery of a Potent Grp94 Selective Inhibitor with Anti-Inflammatory Efficacy in a Mouse Model of Ulcerative Colitis. J Med Chem. 2018 Nov 8;61(21):9513-9533. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.8371 mL	14.1856 mL	28.3712 mL	70.9280 mL
	5 mM	0.5674 mL	2.8371 mL	5.6742 mL	14.1856 mL
	10 mM	0.2837 mL	1.4186 mL	2.8371 mL	7.0928 mL
	15 mM	0.1891 mL	0.9457 mL	1.8914 mL	4.7285 mL
	20 mM	0.1419 mL	0.7093 mL	1.4186 mL	3.5464 mL
	25 mM	0.1135 mL	0.5674 mL	1.1348 mL	2.8371 mL
	30 mM	0.0946 mL	0.4729 mL	0.9457 mL	2.3643 mL
	40 mM	0.0709 mL	0.3546 mL	0.7093 mL	1.7732 mL
	50 mM	0.0567 mL	0.2837 mL	0.5674 mL	1.4186 mL
	60 mM	0.0473 mL	0.2364 mL	0.4729 mL	1.1821 mL
	80 mM	0.0355 mL	0.1773 mL	0.3546 mL	0.8866 mL
	100 mM	0.0284 mL	0.1419 mL	0.2837 mL	0.7093 mL