Progerinin (Synonyms: SLC-D011)

Cat. No.: HY-159834 Purity: 99.74%: Data Sheet
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Progerinin (SLC-D011) is an orally active progerin-lamin A binding inhibitor. Progerinin selectively binds to the C-terminal region of progerin, disrupting its interaction with lamin A and promoting progerin degradation while sparing wild-type lamin A, B, and C. Progerinin ameliorates nuclear deformation, increases H3K9me3 levels, and reduces progerin expression in HGPS patient-derived fibroblasts. Progerinin extends lifespan in Lmna^G609G/G609G mice and Lmna^G609G/+ mice, improves body weight, hair morphology, cardiac function, and histological phenotypes. Progerinin can be used for the study of Hutchinson-Gilford progeria syndrome (HGPS).

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

Progerinin Chemical Structure

CAS No. : 2249696-72-6

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Biological Activity
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Description

In Vitro

Progerinin (100 nM, 3 d) reduces progerin expression, induces H3K9me3 and cyclin B1 expression, and increases Ki67-positive cells in HGPS-derived fibroblasts^[1].
Progerinin (2 μM, 7 d) decreases progerin and p16/INK4A levels, restores H3K9me3 expression, and has no significant effect on normal fibroblasts in HGPS-derived fibroblasts^[1].
Progerinin (5 μM, 7 d) inhibits progerin-lamin A interaction, ameliorates nuclear deformation, blocks cellular senescence (reduces SA-β-gal staining), and promotes cell proliferation in HGPS cells^[1].
Progerinin (500 nM, 3 d) commonly reduces progerin level, induces H3K9me3 and cyclin B1 expression in different HGPS cells (AG11513, AG03199, AG11498, AG03198)^[1].
Progerinin (100 nM, 24 h) reduces exogenous GFP-progerin expression in HEK293 cells transiently transfected with GFP-progerin vector^[1].
Progerinin (5 μM, 30 min) blocks the interaction between lamin A (GST-LA) and GFP-progerin in HEK293 cells during GST-pull-down assay^[1].

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

In Vivo

Progerinin (20 mg/kg, i.p., twice weekly) increases body weight, extends lifespan and ameliorates gross morphology in Lmna^G609G/G609G mice^[1].
Progerinin (50 mg/kg, p.o., daily in Monoolein (HY-128754)-based solution, 8 weeks) improves gross morphology, increases body weight and extends lifespan in Lmna^G609G/G609G mice^[1]. Progerinin (10 mg/mL, p.o., daily in Monoolein-based solution) extends lifespan of Lmna^G609G/+ mice^[1].

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

Animal Model:	Lmna^G609G/G609G mice
Dosage:	20 mg/kg
Administration:	i.p., twice weekly starting from 5 or 32 weeks old
Result:	Increased body weight, extends lifespan. Ameliorated gross morphology. Improved gross morphology (hair status and body size).

Animal Model:	Lmna^G609G/G609G mice
Dosage:	50 mg/kg
Administration:	p.o., daily in monoolein-based solution, 8 weeks
Result:	Improved gross morphology. Increased body weight and extended lifespan. Reduced progerin level. Increased H3K9me3 expression in lung/liver/kidney. Improved grip strength and heart rate. Alleviated kyphosis and dental abnormalities. Reduced tissue fibrosis.

Clinical Trial

Molecular Weight

362.42

Formula

C₂₃H₂₂O₄

CAS No.

2249696-72-6

Appearance

Solid

Color

White to off-white

SMILES

CC1(OC2=CC(OC(C=C3)=O)=C3C=C2C[C@@H]1OC/C=C/C4=CC=CC=C4)C

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 : 100 mg/mL (275.92 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	2.7592 mL	13.7961 mL	27.5923 mL
5 mM	0.5518 mL	2.7592 mL	5.5185 mL
10 mM	0.2759 mL	1.3796 mL	2.7592 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

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: ≥ 2.5 mg/mL (6.90 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.
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% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.90 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 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: 99.74%

Select Batch:

Data Sheet (272 KB) SDS (251 KB)

COA (245 KB) HNMR (135 KB) RP-HPLC (168 KB) NP-HPLC (124 KB) LCMS (103 KB)

Handling Instructions (2659 KB)

References

[1]. Kang SM, et al. Progerinin, an optimized progerin-lamin A binding inhibitor, ameliorates premature senescence phenotypes of Hutchinson-Gilford progeria syndrome. Commun Biol. 2021 Jan 4;4(1):5. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.7592 mL	13.7961 mL	27.5923 mL	68.9807 mL
	5 mM	0.5518 mL	2.7592 mL	5.5185 mL	13.7961 mL
	10 mM	0.2759 mL	1.3796 mL	2.7592 mL	6.8981 mL
	15 mM	0.1839 mL	0.9197 mL	1.8395 mL	4.5987 mL
	20 mM	0.1380 mL	0.6898 mL	1.3796 mL	3.4490 mL
	25 mM	0.1104 mL	0.5518 mL	1.1037 mL	2.7592 mL
	30 mM	0.0920 mL	0.4599 mL	0.9197 mL	2.2994 mL
	40 mM	0.0690 mL	0.3449 mL	0.6898 mL	1.7245 mL
	50 mM	0.0552 mL	0.2759 mL	0.5518 mL	1.3796 mL
	60 mM	0.0460 mL	0.2299 mL	0.4599 mL	1.1497 mL
	80 mM	0.0345 mL	0.1725 mL	0.3449 mL	0.8623 mL
	100 mM	0.0276 mL	0.1380 mL	0.2759 mL	0.6898 mL

Progerinin Related Classifications

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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:

Progerinin2249696-72-6SLC-D011DNA/RNA SynthesisHutchinson-Gilford progeria syndrome (HGPS)progerin-lamin A bindingH3K9me3Inhibitorinhibitorinhibit

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