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Cat. No.: HY-179157

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MA203

MA203 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 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)).

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

화학식: C₃₈H₄₅N₉O₈
분자량:755.82

보관:

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

Data Sheet (285 KB)

MA203 Chemical Structure

Amount: USD 0.00

* 장바구니에 담기 전 물품의 수량을 선택해 주십시오.

Use of MCE Products

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

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

MA203 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 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 :

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

분자량 755.82
화학식 C₃₈H₄₅N₉O₈
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
선적

Room temperature in continental US; may vary elsewhere.
보관

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

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (285 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]. 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]

Calculators

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

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

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Other size

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Amount: USD 0.00

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
순도&문서
References

상품명:
Cat. No.:
수량:
MCE Japan Authorized Agent:

상품명:
CAS No.:
Species:
Purity:
수량:

MA203

All PROTACs Isoforms

All Checkpoint Kinase (Chk) Isoforms

All DNA/RNA Synthesis Isoforms

All Bcl-2 Family Isoforms

All Caspase Isoforms