country

Change Language

EN - English
FR - Français
DE - Deutsch
ES - Español
JA - 日本語
KO - 한국어

Country or Region:

United States

Product Name	Size / Unit Price	Qty

Total: USD 0.00 Checkout

Cat. No.: HY-189468

Copy Link Print Information

PROTAC SHP2 degrader-1

PROTAC SHP2 degrader-1 is a potent SHP2 PROTAC degrader with a DC₅₀ of 7.406 μM. PROTAC SHP2 degrader-1 recruits DCAF16 E3 ligase to induce ubiquitination and proteasomal degradation of SHP2, thereby inhibiting the RAS/MAPK and PI3K/AKT/mTOR signaling pathways while simultaneously inducing IFN-γ/JAK/STAT1, apoptosis, and cell cycle arrest. PROTAC SHP2 degrader-1 can be used for cancer research.
(Pink: SHP2 ligand (HY-100388); Blue: DCAF16 ligand (HY-189472); Black: linker).

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

CAS No.: 3128784-74-4
Formula: C₃₈H₄₈Cl₃N₇O₄
Molecular Weight:773.19

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

PROTAC SHP2 degrader-1 Chemical Structure

CAS No.: 3128784-74-4

Price

Stock

Quantity

Amount: USD 0.00

* Please select Quantity before adding items.

Use of MCE Products

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

PROTAC SHP2 degrader-1 is a potent SHP2 PROTAC degrader with a DC₅₀ of 7.406 μM. PROTAC SHP2 degrader-1 recruits DCAF16 E3 ligase to induce ubiquitination and proteasomal degradation of SHP2, thereby inhibiting the RAS/MAPK and PI3K/AKT/mTOR signaling pathways while simultaneously inducing IFN-γ/JAK/STAT1, apoptosis, and cell cycle arrest. PROTAC SHP2 degrader-1 can be used for cancer research^[1]. (Pink: SHP2 ligand (HY-100388); Blue: DCAF16 ligand (HY-189472); Black: linker).

IC₅₀ & Target

^[1]

DCAF16

All PROTACs Isoforms :

All PARP Isoforms :

All JNK Isoforms :

All p38 MAPK Isoforms :

All Akt Isoforms :

All mTOR Isoforms :

All STAT Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
HeLa	IC₅₀	2.317 μM	Antiproliferative activity against human HeLa cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay. Antiproliferative activity against human HeLa cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay.	42600470
HCT-116	IC₅₀	5.21 μM	Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay. Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay.	42600470
SW480	IC₅₀	4.39 μM	Antiproliferative activity against human SW480 cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay. Antiproliferative activity against human SW480 cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay.	42600470
KYSE-520 cell line	IC₅₀	1.923 μM	Antiproliferative activity against human KYSE520 cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay. Antiproliferative activity against human KYSE520 cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay.	42600470
HeLa	DC₅₀	7.406 μM	Degradation of SHP2 in human HeLa cells assessed as half-maximal degradation concentration by Western blot analysis. Degradation of SHP2 in human HeLa cells assessed as half-maximal degradation concentration by Western blot analysis.	42600470

In Vitro

PROTAC SHP2 degrader-1 (compound SK8) (24 h) exhibits potent antiproliferative activity against HeLa (IC₅₀ = 2.317 μM), HCT116 (IC₅₀ = 5.21 μM), SW480 (IC₅₀ = 4.39 μM), and KYSE520 (IC₅₀ = 1.923 μM) cells, but shows no significant cytotoxicity against HEK293T cells^[1].
PROTAC SHP2 degrader-1 (1.875-30 μM; 3-36 h) induces SHP2 degradation in HeLa cells in a dose- and time-dependent manner, with a DC₅₀ of 7.406 μM^[1].
PROTAC SHP2 degrader-1 (15 μM; 6 h) promotes the physical interaction between SHP2 and DCAF16 in HeLa cells^[1].
PROTAC SHP2 degrader-1 (1.25-2.5 μM; 10 days) inhibits HeLa colony formation^[1].
PROTAC SHP2 degrader-1 (1-5 μM; 12-24 h) induces cell cycle arrest at S phase, inhibits cell migration and invasion, and induces apoptosis in HeLa cells^[1].

PROTAC SHP2 degrader-1 (3.75-15 μM; 24 h) triggers the mitochondria-mediated intrinsic apoptosis pathway in HeLa cells, inhibits MAPK activation more effectively than enzymatic inhibition, and potently suppresses PI3K/AKT/mTOR signaling^[1].
PROTAC SHP2 degrader-1 (15 μM; 12 h) enhances IFN-γ (HY-P7025)-induced STAT1 phosphorylation and upregulates the mRNA expression levels of MHC class I molecule-related genes in HeLa and 4T1 cells^[1].
PROTAC SHP2 degrader-1 (15 μM; 12 h) enhances CD8⁺ T cell activation in a co-culture system of 4T1 and mouse splenic immune cells^[1].

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

Western Blot Analysis^[1]

Cell Line:

HeLa
Concentration:

1.875, 3.75, 7.5, 15, 30 μM
Incubation Time:

3, 6, 12, 24, 36 h
Result:

Exhibited the most potent SHP2 degradation activity, degrading SHP2 in a concentration-dependent and time-dependent manner.

Cell Proliferation Assay^[1]

Cell Line:

HeLa
Concentration:

1.25, 2.5 μM
Incubation Time:

10 days
Result:

Inhibited HeLa colony growth.

Cell Cycle Analysis^[1]

Cell Line:

HeLa
Concentration:

2.5, 5 μM
Incubation Time:

24 h
Result:

Arrested the cell cycle in S phase, causing a more substantial accumulation of cells in S phase compared to SHP099.

Cell Migration Assay ^[1]

Cell Line:

HeLa
Concentration:

1, 2 μM
Incubation Time:

12, 24 h
Result:

Induced a dose-dependent reduction in HeLa cell migration, showing a stronger effect than SHP099.

Cell Invasion Assay^[1]

Cell Line:

HeLa
Concentration:

2 μM
Incubation Time:

24 h
Result:

Exhibited greater efficacy than SHP099 in inhibiting vertical migration (invasion) of HeLa cells.

Apoptosis Analysis^[1]

Cell Line:

HeLa
Concentration:

2.5, 5 μM
Incubation Time:

24 h
Result:

Induced HeLa cell apoptosis in a dose-dependent manner.

Chemical Information

CAS No. 3128784-74-4
Molecular Weight 773.19
Formula C₃₈H₄₈Cl₃N₇O₄
SMILES

ClC1=C(Cl)C(C2=NC=C(N3CCC(NC(CCCCCCCCNC(COC4=CC=C(N(C(CCl)=O)CCC5)C5=C4)=O)=O)(C)CC3)N=C2N)=CC=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Pang X, et al. Discovery of DCAF16-based PROTACs as SHP2 degraders. Bioorganic chemistry. 2026 Oct 05;181:110372.

Calculators

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)

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.

Bioz

MOQ

Minimum order quantity

100 mg

Get Quote In-stock

Other size

Get Quote

Amount: USD 0.00

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent:

Product Name:
CAS No.:
Species:
Purity:
Quantity:

PROTAC SHP2 degrader-1

All PROTACs Isoforms

All PARP Isoforms

All JNK Isoforms

All p38 MAPK Isoforms

All Akt Isoforms

All mTOR Isoforms

All STAT Isoforms