Cat. No.: HY-179157A

MA203 hydrochloride

Name: MA203 hydrochloride
Brand: MedChemExpress
SKU: HY-179157A
Price: 380.00 USD
Availability: InStock
Rating: 5 (1 reviews)

Customer Review

Based on 1 Customer Validation

MA203 hydrochloride is a selective CHK1 PROTAC degrader. MA203 targets activated CHK1 for degradation by recruiting the CRBN E3 ubiquitin ligase, thereby completely abolishing both its catalytic and non-catalytic functions and ultimately triggering DNA replication catastrophe and apoptosis. MA203 hydrochloride can be used in research related to pancreatic ductal adenocarcinoma, colorectal cancer, and acute lymphoblastic leukemia.
(Pink: Chk1 ligand (HY-179158); Blue: Cereblon ligand (HY-41547); Black: linker (HY-22391)).

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

Formula: C₃₈H₄₆ClN₉O₈
Molecular Weight:792.28

Storage:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

MA203 hydrochloride Chemical Structure

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

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

Biological Activity

Description

MA203 hydrochloride is a selective CHK1 PROTAC degrader. MA203 targets activated CHK1 for degradation by recruiting the CRBN E3 ubiquitin ligase, thereby completely abolishing both its catalytic and non-catalytic functions and ultimately triggering DNA replication catastrophe and apoptosis. MA203 hydrochloride can be used in research related to pancreatic ductal adenocarcinoma, colorectal cancer, and acute lymphoblastic leukemia^[1]. (Pink: Chk1 ligand (HY-179158); Blue: Cereblon ligand (HY-41547); Black: linker (HY-22391)).

IC₅₀ & Target

^[1]

Chk1

Bax

Bcl-xL

All PROTACs Isoforms :

All Checkpoint Kinase (Chk) Isoforms :

All DNA/RNA Synthesis Isoforms :

All Bcl-2 Family Isoforms :

All Caspase Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
MIA PaCa-2	DC₅₀	1.51 μM	Half-maximal CHK1 degradation in human MIA PaCa-2 pancreatic ductal adenocarcinoma cells treated with MA203 in combination with 0.5 mM HU for 24 h, assessed by immunoblot analysis of CHK1 protein levels. Half-maximal CHK1 degradation in human MIA PaCa-2 pancreatic ductal adenocarcinoma cells treated with MA203 in combination with 0.5 mM HU for 24 h, assessed by immunoblot analysis of CHK1 protein levels.	41104666
MOLT-4	DC₅₀	5.35 μM	Half-maximal CHK1 degradation in human MOLT-4 acute lymphocytic leukemia cells treated with MA203 in combination with 0.5 mM HU for 24 h, assessed by immunoblot analysis of CHK1 protein levels. Half-maximal CHK1 degradation in human MOLT-4 acute lymphocytic leukemia cells treated with MA203 in combination with 0.5 mM HU for 24 h, assessed by immunoblot analysis of CHK1 protein levels.	41104666
MOLT-4	DC₅₀	387.4 nM	Half-maximal CHK1 degradation in human MOLT-4 acute lymphocytic leukemia cells treated with MA203 in combination with 2 μM cytarabine for 24 h, assessed by immunoblot analysis of CHK1 protein levels. Half-maximal CHK1 degradation in human MOLT-4 acute lymphocytic leukemia cells treated with MA203 in combination with 2 μM cytarabine for 24 h, assessed by immunoblot analysis of CHK1 protein levels.	41104666

In Vitro

MA203 (2 μM; 3-24 h) hydrochloride, in combination with HU (HY-B0313), significantly reduces CHK1 protein levels and upregulates γH2AX phosphorylation levels in MIA PaCa-2, MOLT-4, and HCT116 cells in a time- and concentration-dependent manner^[1].

MA203 (2 μM; 24 h) hydrochloride, with or without HU treatment, degrades CHK1 in MOLM-13 and RS4-11 cells^[1].
MA203 (0.5-10 μM; 24 h) hydrochloride, in combination with HU treatment, dose-dependently upregulates γH2AX phosphorylation and p-ATM (S1981) levels, significantly increases γH2AX foci, and exacerbates DNA single-strand breaks in MIA PaCa-2 and MOLT-4 cells^[1].
MA203 (2 μM; 24 h) hydrochloride, in combination with 1 mM HU treatment, upregulates γH2AX phosphorylation levels in MOLT-4 and HCT116 cells^[1].
MA203 (1-5 μM; 24 h) hydrochloride, in combination with Ara-C (HY-13605) treatment, synergistically enhances Ara-C cytotoxicity in MOLT-4 cells, does not affect cell viability and activation status in activated T and B cells, and does not significantly impair cell survival in mouse hematopoietic stem cells (HSCs)^[1].

MA203 (2 μM; 7 days) hydrochloride inhibits cell proliferation in MOLT-4 cells but exerts no effect on RPE1 cells^[1].

MA203 (1-10 μM; 48 h) hydrochloride, in combination with HU treatment, induces apoptosis in MIA PaCa-2, HCT116, MOLT-4, and MOLM-13 cells, but does not affect cell viability in RPE1, HS-5, and PBMCs^[1].

MA203 (2 μM; 16-48 h) hydrochloride, in combination with 1 mM HU treatment, downregulates the protein expression of TCF1/7, CDCA7, RRM2, ORC1, WRN, and claspin, reduces p-CHK1 (S296) levels, promotes G1 phase arrest, increases the proportion of sub-G1 cells, upregulates BAX, BIM, and NOXA while downregulating BCL-XL and XIAP, significantly increases the loss of mitochondrial membrane potential, and enhances the cleavage of caspase-8, caspase-3, and PARP1 in MIA PaCa-2 cells^[1].

MA203 hydrochloride potently binds to purified human CHK1 protein, with a binding rate of 97% at 1.0 μM^[1].

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

Western Blot Analysis^[1]

Cell Line:

MIA PaCa-2, MOLT-4
Concentration:

2 μM
Incubation Time:

3, 6, 10, 16, 24 h
Result:

Degraded CHK1 in combination with HU, without affecting off-target proteins such as CHK2 and GSPT.
Decreased CHK1 levels and altered its phosphorylation status in a time-dependent manner.

Immunofluorescence^[1]

Cell Line:

MIA PaCa-2
Concentration:

2 μM
Incubation Time:

24 h
Result:

Significantly increased the accumulation of γH2AX foci in combination with HU.

Cell Viability Assay^[1]

Cell Line:

MIA PaCa-2, HCT116, MOLT-4, MOLM-13
Concentration:

2 μM
Incubation Time:

24 h or 48 h
Result:

Significantly induced early and late apoptosis in combination with HU.

Cell Cycle Analysis^[1]

Cell Line:

MIA PaCa-2
Concentration:

2 μM
Incubation Time:

24 h and 48 h
Result:

Promoted G1 phase arrest and increased the proportion of cells in the subG1 phase in combination with HU.

Cell Proliferation Assay^[1]

Cell Line:

MOLT-4 and RPE1
Concentration:

2 μM
Incubation Time:

7 days
Result:

Inhibited the proliferation of leukemia cells, but did not affect normal cells.

Western Blot Analysis^[1]

Cell Line:

MIA PaCa-2
Concentration:

2 μM
Incubation Time:

24 h and 48 h
Result:

Downregulated key proteins involved in DNA repair and replication (such as WRN, TCF1/7) and modulated the expression of apoptosis-related BCL2 family proteins.

In Vivo

MA203 (12 μM; administered in growth medium; 48 h) hydrochloride exerts anti-leukemic effects with no obvious toxicity in a zebrafish larva model xenografted with fluorescently labeled MOLT-4 cells^[1].

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

Animal Model:

wild-type AB strain (2 days post-fertilization)^[2]
Dosage:

12 μM
Administration:

immersion; continuous; 48 h
Result:

Inhibited the MOLT-4 tumor burden xenografted in zebrafish.

Related Protocols :

Chemical Information

Appearance Solid
Molecular Weight 792.28
Formula C₃₈H₄₆ClN₉O₈
SMILES

O=C1CCC(N2C(C(C=CC=C3NCCCCCCCNC(C4=CC(OC[C@H]5OCCNC5)=C(NC(NC6=CN=C(C)C=N6)=O)C=C4)=O)=C3C2=O)=O)C(N1)=O.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (63.11 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

1.2622 mL

6.3109 mL

12.6218 mL

5 mM

0.2524 mL

1.2622 mL

2.5244 mL

10 mM

0.1262 mL

0.6311 mL

1.2622 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

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

Mass Mass

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Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Ashry R, et al. Identification of a Proteolysis-Targeting-Chimera that Addresses Activated Checkpoint Kinase-1 Reveals its Non-Catalytic Functions in Tumor Cells. Angewandte Chemie (International ed. in English). 2025 Dec 01;64(49):e202514788. [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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.2622 mL	6.3109 mL	12.6218 mL	31.5545 mL
	5 mM	0.2524 mL	1.2622 mL	2.5244 mL	6.3109 mL
	10 mM	0.1262 mL	0.6311 mL	1.2622 mL	3.1554 mL
	15 mM	0.0841 mL	0.4207 mL	0.8415 mL	2.1036 mL
	20 mM	0.0631 mL	0.3155 mL	0.6311 mL	1.5777 mL
	25 mM	0.0505 mL	0.2524 mL	0.5049 mL	1.2622 mL
	30 mM	0.0421 mL	0.2104 mL	0.4207 mL	1.0518 mL
	40 mM	0.0316 mL	0.1578 mL	0.3155 mL	0.7889 mL
	50 mM	0.0252 mL	0.1262 mL	0.2524 mL	0.6311 mL
	60 mM	0.0210 mL	0.1052 mL	0.2104 mL	0.5259 mL

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MA203 hydrochloride

All PROTACs Isoforms

All Checkpoint Kinase (Chk) Isoforms

All DNA/RNA Synthesis Isoforms

All Bcl-2 Family Isoforms

All Caspase Isoforms