PELP1-IN-1

Name: PELP1-IN-1
Brand: MedChemExpress
SKU: HY-159613
Rating: 4.5 (1 reviews)

Cat. No.: HY-159613 Purity: 99.28%: Data Sheet
COA

SDS
Handling Instructions
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PELP1-IN-1 is a PELP1 inhibitor and an apoptosis inducer with no cytotoxic activity against non-cancer cell lines. PELP1-IN-1 targets wild-type, mutant and drug-resistant ER⁺ breast cancer, and promotes PELP1 degradation through the proteasome pathway. As an analog of SMIP34 (HY-169903), PELP1-IN-1 is applicable to the research of estrogen receptor α-positive breast cancer.

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

PELP1-IN-1 Chemical Structure

CAS No. : 946262-80-2

Size	Stock	Quantity
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
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100 mg	Get quote

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Based on 1 publication(s) in Google Scholar

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Biological Activity
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References
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Description

IC₅₀ & Target

PELP1^[1]

In Vitro

PELP1-IN-1 (SM1) (10 μM; 12-48 h) inhibits migration and invasion of ZR75, MCF7 and MT-ER⁺ breast cancer cells, reduces soft agar colony formation, promotes apoptosis (Annexin V staining, increased caspase 3/7 activity) and induces S-phase cell cycle arrest^[1].
PELP1-IN-1 (10 μM; 48 h) downregulates the expression of estrogen response- and cell cycle-related genes, upregulates genes involved in the apoptosis and p53 pathways, and inhibits ER-PELP1 downstream signaling in ZR75 and MCF7 cells^[1].

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

Apoptosis Analysis^[1]

Cell Line:	ZR75, MCF7, MCF7(Y537S), MCF7(D538G), ZR75(Y537S), ZR75(D538G)
Concentration:	10 μM
Incubation Time:	24-48 h
Result:	Induced apoptosis in both WT-ER⁺ and MT-ER⁺ breast cancer cells, as indicated by increased Annexin V-positive cells and enhanced caspase 3/7 enzymatic activity.

Parmacokinetics

Species	Dose	Route	AUC_0-t	AUC_0-∞	MRT_0-t	MRT_0-∞	T_1/2	T_max	CL	V_d	C_max	Bioavailability
Mice^[2]	1 mg/kg	i.v.	970.4 ng·h/mL	986.7 ng·h/mL	1.6 h	1.8 h	1.3 h	0.1 h	1.2 L/h/kg	2.1 L/kg	583.4 ng/mL	/
Mice^[2]	1 mg/kg	i.v.	970.4 ng·h/mL	986.7 ng·h/mL	1.6 h	1.8 h	1.3 h	0.1 h	1.2 L/h/kg	2.1 L/kg	583.4 ng/mL	/
Mice^[2]	1 mg/kg	i.v.	970.4 ng·h/mL	986.7 ng·h/mL	1.6 h	1.8 h	1.3 h	0.1 h	1.2 L/h/kg	2.1 L/kg	583.4 ng/mL	/
Mice^[2]	2 mg/kg	p.o.	1261.6 ng·h/mL	1419.6 ng·h/mL	2.1 h	3.2 h	2.5 h	0.8 h	1.5 L/h/kg	4.9 L/kg	614.8 ng/mL	65.0 %
Mice^[2]	2 mg/kg	p.o.	1261.6 ng·h/mL	1419.6 ng·h/mL	2.1 h	3.2 h	2.5 h	0.8 h	1.5 L/h/kg	4.9 L/kg	614.8 ng/mL	65.0 %
Mice^[2]	2 mg/kg	p.o.	1261.6 ng·h/mL	1419.6 ng·h/mL	2.1 h	3.2 h	2.5 h	0.8 h	1.5 L/h/kg	4.9 L/kg	614.8 ng/mL	65.0 %
Mice^[2]	4 mg/kg	p.o.	3023.6 ng·h/mL	3050.8 ng·h/mL	1.6 h	1.7 h	1.2 h	0.8 h	1.4 L/h/kg	2.4 L/kg	1716.6 ng/mL	77.9 %
Mice^[2]	4 mg/kg	p.o.	3023.6 ng·h/mL	3050.8 ng·h/mL	1.6 h	1.7 h	1.2 h	0.8 h	1.4 L/h/kg	2.4 L/kg	1716.6 ng/mL	77.9 %
Mice^[2]	4 mg/kg	p.o.	3023.6 ng·h/mL	3050.8 ng·h/mL	1.6 h	1.7 h	1.2 h	0.8 h	1.4 L/h/kg	2.4 L/kg	1716.6 ng/mL	77.9 %
Mice^[2]	8 mg/kg	p.o.	6149.6 ng·h/mL	6208.9 ng·h/mL	1.6 h	1.7 h	1.1 h	0.8 h	1.3 L/h/kg	2.0 L/kg	3045.6 ng/mL	79.2 %
Mice^[2]	8 mg/kg	p.o.	6149.6 ng·h/mL	6208.9 ng·h/mL	1.6 h	1.7 h	1.1 h	0.8 h	1.3 L/h/kg	2.0 L/kg	3045.6 ng/mL	79.2 %
Mice^[2]	8 mg/kg	p.o.	6149.6 ng·h/mL	6208.9 ng·h/mL	1.6 h	1.7 h	1.1 h	0.8 h	1.3 L/h/kg	2.0 L/kg	3045.6 ng/mL	79.2 %

Molecular Weight

443.88

Formula

C₂₀H₁₅ClFN₅O₂S

CAS No.

946262-80-2

Appearance

Solid

Color

White to off-white

SMILES

O=C1C2=C(N(C3=CC=C(Cl)C=C3)N=C2)N=C(SCC(NCC4=CC=C(F)C=C4)=O)N1

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 : 4.57 mg/mL (10.30 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	2.2529 mL	11.2643 mL	22.5286 mL
5 mM	0.4506 mL	2.2529 mL	4.5057 mL
10 mM	0.2253 mL	1.1264 mL	2.2529 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: 99.28%

Select Batch:

Data Sheet (272 KB) SDS (251 KB)

COA (249 KB) HNMR (265 KB) LCMS (105 KB)

Handling Instructions (2659 KB)

References

[1]. Altwegg KA, et al. A First-in-Class Inhibitor of ER Coregulator PELP1 Targets ER+ Breast Cancer. Cancer Res. 2022;82(20):3830-3844. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.2529 mL	11.2643 mL	22.5286 mL	56.3215 mL
	5 mM	0.4506 mL	2.2529 mL	4.5057 mL	11.2643 mL
	10 mM	0.2253 mL	1.1264 mL	2.2529 mL	5.6322 mL

PELP1-IN-1 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:

PELP1-IN-1946262-80-2ApoptosisEstrogen Receptor/ERRmammary epithelial cellsovarian epithelial cellswild-type ER+ breast cancertherapy-resistant ER+ breast cancerendometrial epithelial cellsPELP1mutant ER+ breast cancerproteasome pathwayestrogen receptor alpha-positive breast cancersInhibitorinhibitorinhibit

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PELP1-IN-1

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PELP1-IN-1 Related Antibodies

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References

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PELP1-IN-1 Related Antibodies

Molarity Calculator

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Complete Stock Solution Preparation Table

PELP1-IN-1 Related Classifications

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