Cat. No.: HY-103021

LY3200882

13 Cited Publications

Customer Review

Based on 13 publication(s) in Google Scholar

LY3200882 is a potent, highly selective, ATP-competitive and orally active TGF-β receptor type 1 (ALK5) inhibitor with an IC₅₀ of 38.2 nM. LY3200882 inhibits various pro-tumorigenic activities and is also used as an immune modulatory agent.

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

Purity: 99.87%
CAS No.: 1898283-02-7
Formula: C₂₄H₂₉N₅O₃
Molecular Weight:435.52

Storage:

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

LY3200882 Chemical Structure

CAS No.: 1898283-02-7

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (13)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target

IC50: 38.2 nM (TGF-β receptor type 1 (ALK5))^[2]

All TGF-β Receptor Isoforms :

In Vitro

LY3200882 potently inhibits TGFβ mediated SMAD phosphorylation in vitro in tumor and immune cells in a dose dependent fashion^[1].
LY3200882 shows potent anti-tumor activity in the orthotopic 4T1-LP model of triple negative breast cancer and this activity correlated with enhanced tumor infiltrating lymphocytes in the tumor microenvironment^[1].
In in vitro immune suppression assays, LY3200882 has shown the ability to rescue TGFβ1 suppressed or T regulatory cell suppressed naive T cell activity and restore proliferation^[1].
LY3200882 inhibits NIH₃T₃ cell viability with an IC₅₀ of 82.9 nM^[2].

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

In Vivo

LY3200882 (60 mg/kg; oral gavage; twice a day; for 21 days; BALB/C female mice) treatment significantly delays tumor growth in CT26 model^[2].
LY3200882 potently inhibits TGFβ mediated SMAD phosphorylation in vivo in subcutaneous tumors in a dose dependent fashion^[1].
LY3200882 has shown anti-metastatic activity in vivo in an experimental metastasis tumor model (intravenous EMT6-LM2 model of triple negative breast cancer)^[1].

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

Animal Model:

BALB/C female mice (5-8-week-old) injected with CT26 cells^[2]
Dosage:

60 mg/kg
Administration:

Oral gavage; twice a day; for 21 days
Result:

A statistically significant tumor growth delay in CT26 model was observed.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1898283-02-7
Appearance Solid
Molecular Weight 435.52
Formula C₂₄H₂₉N₅O₃
Color Off-white to light yellow
SMILES

OC(C)(C)C1=NC=CC(NC2=NC=CC(OC3=CN(C4CC4)N=C3C5CCOCC5)=C2)=C1
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

Publications (13)

All Cell Proliferation/Viability AssayApoptosis AnalysisCell Migration/Invasion AssayWBHistological Imaging/Staining

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Journal Impact Factor

Nat Genet

TGF-β builds a dual immune barrier in colorectal cancer by impairing T cell recruitment and instructing immunosuppressive SPP1+ macrophages. [Abstract]

2025 Dec;57(12):3050-3065. PMID: 41203813
Biomaterials

The programmed site-specific delivery of LY3200882 and PD-L1 siRNA boosts immunotherapy for triple-negative breast cancer by remodeling tumor microenvironment. [Abstract]

2022 May;284:121518. PMID: 35462305
Sci Adv

A deubiquitination module essential for Treg fitness in the tumor microenvironment. [Abstract]

2022 Nov 25;8(47):eabo4116. PMID: 36427305
J Biol Eng

Enhancing the therapeutic efficacy of gemcitabine in bladder cancer through TGF-β1 inhibition and pluronic F-127-based microsphere delivery. [Abstract]

2025 Jul 11;19(1):62. PMID: 40646590

LY3200882 purchased from MedChemExpress. Usage Cited in: J Biol Eng. 2025 Jul 11;19(1):62. [Abstract]

Bladder cancer cell lines 5637 and SW780 were treated with varying concentrations of LY3200882 (0, 1, 2.5, or 5 µM) for 48 h and assessed for cell viability using CCK8 assay.

LY3200882 purchased from MedChemExpress. Usage Cited in: J Biol Eng. 2025 Jul 11;19(1):62. [Abstract]

Cells were treated with 2.5 µM LY2109761 or LY3200882 and examined for cell apoptosis by Flow cytometry.

LY3200882 purchased from MedChemExpress. Usage Cited in: J Biol Eng. 2025 Jul 11;19(1):62. [Abstract]

Cell invasion capabilities using a Transwell assay treated with 2.5 µM LY2109761 or LY3200882.

LY3200882 purchased from MedChemExpress. Usage Cited in: J Biol Eng. 2025 Jul 11;19(1):62. [Abstract]

The protein levels of Ki-67, Cleaved-caspase 3, E-cadherin, MMP-2, and MMP-9 using Immunoblotting treated with 2.5 µM LY2109761 or LY3200882.

LY3200882 purchased from MedChemExpress. Usage Cited in: J Biol Eng. 2025 Jul 11;19(1):62. [Abstract]

Histological analysis of tumor tissues treated with LY3200882 (10 mg/kg) using H&E staining.
J Invest Dermatol

Identification of Small-Molecule Inhibitors Targeting Different Signaling Pathways in Cancer-Associated Fibroblast Reprogramming Under Tumor-Stroma Interaction. [Abstract]

2024 Jun 5:S0022-202X(24)00392-0. PMID: 38848988
Mar Drugs

Anti-Inflammatory Azaphilones from the Edible Alga-Derived Fungus Penicillium sclerotiorum. [Abstract]

2021 Sep 22;19(10):529. PMID: 34677428
FASEB J

Myeloid-specific blockade of Notch signaling alleviates murine pulmonary fibrosis through regulating monocyte-derived Ly6clo MHCIIhi alveolar macrophages recruitment and TGF-β secretion. [Abstract]

2020 Aug;34(8):11168-11184. PMID: 32638441
Bioengineering (Basel)

Proteoglycans Enhance the Therapeutic Effect of BMSC Transplantation on Osteoarthritis. [Abstract]

2024 Nov 20;11(11):1167. PMID: 39593826
Cytokine

Bone marrow mesenchymal stem cells paracrine TGF-β1 to mediate the biological activity of osteoblasts in bone repair. [Abstract]

2023 Apr:164:156139. PMID: 36738525
Biol Reprod

Increased EHD1 in trophoblasts causes RSM by activating TGFβ signaling. [Abstract]

2024 Jul 16:ioae110. PMID: 39012723
Res Sq

2025 Sep 26.
Patent

US20240238274A1.
ACS Comb Sci

Benzimidazolyl-pyrazolo[3,4- b]pyridinones, Selective Inhibitors of MOLT-4 Leukemia Cell Growth and Sea Urchin Embryo Spiculogenesis: Target Quest. [Abstract]

2019 Dec 9;21(12):805-816. PMID: 31689077

Solvent & Solubility

In Vitro:

DMSO : 33.33 mg/mL (76.53 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2961 mL

11.4805 mL

22.9611 mL

5 mM

0.4592 mL

2.2961 mL

4.5922 mL

10 mM

0.2296 mL

1.1481 mL

2.2961 mL

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

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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 (5.74 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (5.74 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.74 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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Huaxing Pei, et al. Abstract 955: LY3200882, a novel, highly selective TGFβRI small molecule inhibitor. AACR; Cancer Res 2017;77(13 Suppl):Abstract nr 955.

[2]. Xu G, et al. Synthesis and biological evaluation of 4-(pyridin-4-oxy)-3-(3,3-difluorocyclobutyl)-pyrazole derivatives as novel potent transforming growth factor-β type 1 receptor inhibitors. Eur J Med Chem. 2020 Apr 29;198:112354. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2961 mL	11.4805 mL	22.9611 mL	57.4026 mL
	5 mM	0.4592 mL	2.2961 mL	4.5922 mL	11.4805 mL
	10 mM	0.2296 mL	1.1481 mL	2.2961 mL	5.7403 mL
	15 mM	0.1531 mL	0.7654 mL	1.5307 mL	3.8268 mL
	20 mM	0.1148 mL	0.5740 mL	1.1481 mL	2.8701 mL
	25 mM	0.0918 mL	0.4592 mL	0.9184 mL	2.2961 mL
	30 mM	0.0765 mL	0.3827 mL	0.7654 mL	1.9134 mL
	40 mM	0.0574 mL	0.2870 mL	0.5740 mL	1.4351 mL
	50 mM	0.0459 mL	0.2296 mL	0.4592 mL	1.1481 mL
	60 mM	0.0383 mL	0.1913 mL	0.3827 mL	0.9567 mL

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LY3200882

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

TGF-beta/Smad Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Reprogramming Compound Library

Orally Active Compound Library

Anti-Breast Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Osteogenesis Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Cytokine Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Fibrosis Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) LY3200882

All TGF-β Receptor Isoforms

Biological Activity

Chemical Information

Publications (13)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

LY3200882 Related Classifications

Cat. No.: HY-103021