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Cat. No.: HY-184431

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YTB53

YTB53 is a MNK1 and MNK2 inhibitor with IC₅₀s of 37 nM and 9 nM, respectively. YTB53 inhibits PDGFRα, TRKB and FLT3 in leukemia cells. YTB53 induces cell cycle arrest, apoptosis, pyroptosis, and mitochondrial dysfunction. YTB53 exhibits antiangiogenic effects. YTB53 can be used for the study of acute myeloid leukemia (AML).

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화학식: C₁₈H₁₃N₃O₂
분자량:303.31

보관:

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

YTB53 Chemical Structure

Amount: USD 0.00

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Use of MCE Products

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

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

Biological Activity

제품 설명

IC₅₀ & Target^[1]

MNK1

37 nM (IC₅₀)

MNK2

9 nM (IC₅₀)

FLT3

0.47 nM (IC₅₀)

PDGFRα

TrkB

All MNK Isoforms :

All PDGFR Isoforms :

All Trk Receptor Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
MV4-11	IC50	2 nM	Inhibits cell growth of MV4-11 cells for 72 h. Inhibits cell growth of MV4-11 cells for 72 h.	42223949

In Vitro

YTB53 (copmound 31) (72 h) inhibits cell growth of MV4-11 cells with an IC₅₀ of 2 nM^[1].
YTB53 (1 μM; 2 h) inhibits eIF4E phosphorylation at Ser209 in HEK293T cells^[1].
YTB53 (1 μM) exhibits strong inhibitory activity against PDGFRα (98.88%) and TRKB (97.43%). YTB53 inhibits FLT3 with an IC₅₀ of 0.470 nM^[1].
YTB53 (0.1-10 μM; 24 h) inhibits eIF4E phosphorylation at Ser209 in MV4-11 cells^[1].
YTB53 (0.05-0.2 μM; 24 h) induces cell cycle arrest in MV4-11 cells^[1].
YTB53 (0.05-0.2 μM; 48 h) induces cell apoptosis and pyroptosis in MV4-11 cells^[1].
YTB53 (0.05-0.2 μM; 24 h) effectively triggeres a substantial increase in ROS generation and a concurrent decrease in mitochondrial membrane potential^[1].
YTB53 (0.05-0.2 μM; 0-24 h) exerts a dual antiangiogenic action, suppressing both endothelial morphogenesis and migration in human umbilical vein endothelial cells (HUVECs)^[1].

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

Western Blot Analysis^[1]

Cell Line:

HEK293T cells
Concentration:

1 μM
Incubation Time:

2 h
Result:

Demonstrated the most potent activity, nearly completely abolishing p-eIF4E levels at 1 μM.

Western Blot Analysis^[1]

Cell Line:

MV4-11 cells
Concentration:

0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM
Incubation Time:

24 h
Result:

Completely inhibited the expression of p-eIF4E even at a low concentration of 0.3 μM, while a concentration of 0.1 μM exhibited partial inhibition.

Cell Cycle Analysis^[1]

Cell Line:

MV4-11 cells
Concentration:

0.05 μM, 0.1 μM, 0.2 μM
Incubation Time:

24 h
Result:

Showed a 24 h treatment induced a concentration-dependent arrest at the G0/G1 phase.

Western Blot Analysis^[1]

Cell Line:

MV4-11 cells
Concentration:

0.05 μM, 0.1 μM, 0.2 μM
Incubation Time:

24 h
Result:

Inhibited cyclin E-CDK2 activity.
Pronounced downregulation of cyclin B1 and its kinase partner CDC2 (CDK1) disables the core engine required for G2/M progression.
Increased the phosphorylated p53 (p-p53) protein levels.
Decreased the total p53 protein levels.

Apoptosis Analysis^[1]

Cell Line:

MV4-11 cells
Concentration:

0.05 μM, 0.1 μM, 0.2 μM
Incubation Time:

48 h
Result:

Led to a dose-dependent increase in the proportion of cells undergoing apoptosis.
Revealed a coordinated downregulation of the antiapoptotic proteins Bcl-2 and Bcl-XL, alongside a reduction in the pro-apoptotic protein Bax-a change.
Decreased the inactive forms of caspase-8, caspase-9, and caspase-3.
The levels of both full-length and cleaved PARP remained largely unchanged.

ELISA Assay^[1]

Cell Line:

MV4-11 cells
Concentration:

0.05 μM, 0.1 μM, 0.2 μM
Incubation Time:

24 h
Result:

Led to significantly elevated levels of lactate dehydrogenase (LDH) and the pro-inflammatory cytokine IL-18.

Western Blot Analysis^[1]

Cell Line:

MV4-11 cells
Concentration:

0.05 μM, 0.1 μM, 0.2 μM
Incubation Time:

24 h
Result:

Showed a significant increase in NLRP3 (NOD-like receptor protein 3) protein levels.
Decreased the level of full-length GSDMD (Gasdermin D).

Parmacokinetics

Species	Dose	Route	C_max	T_max	T_1/2	AUC_0-t	F	V_d	CL
Rat^[1]	10 mg/kg	p.o.	6.26 ng/mL	0.333 h	1.03 h	6.91 ng·h/mL	0.4 %	/	/
Rat^[1]	5 mg/kg	i.v.	2925 ng/mL	0.083 h	0.258 h	866 ng·h/mL	/	2.17 L/kg	97.2 mL/h/kg

In Vivo

YTB53 (copmound 31) (10-40 mg/kg; s.c.; once a day; 14 days) achieves significant dose-dependent antitumor efficacy against MV4-11 mouse xenografts without eliciting overt systemic toxicity^[1].

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

Animal Model:

Female BALB/c nude mice received a 200 μL subcutaneous injection into the right axillary containing a 1:1 (v/v) mixture of human acute myeloid leukemia MV4-11 cells and Matrigel^[1].
Dosage:

10 mg/kg, 20 mg/kg, 40 mg/kg
Administration:

s.c.; once a day; 14 days
Result:

Significantly inhibited tumor growth in a dose-dependent manner.
H&E staining revealed no evidence of inflammatory infiltrates, fibrosis, or architectural disruption in these tissues.
Did not significantly suppress ki-67 expression at low and medium doses (10 and 20 mg/kg) but markedly reduced its levels at the highest dose (40 mg/kg).
Significantly downregulated the expression of p-eIF4E, p53, caspase-9, and Bcl-2.
Elicited a strong inflammatory response at lower doses. However, as the dose increased, the level of inflammation decreased markedly.

Chemical Information

분자량 303.31
화학식 C₁₈H₁₃N₃O₂
SMILES

O=C(N)C1=CC=C(C=C1)C2=CN=C(O2)C3=CC4=CC=CC=C4N3
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

Handling Instructions (2659 KB)

References

[1]. Chen X, et al. Discovery of YTB53, a Marine-Derived MNK-Active Anti-Acute Myeloid Leukemia Lead with Multi-Kinase Activity. J Med Chem. 2026 Jun 11;69(11):13404-13433. [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.

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MOQ

Minimum order quantity

100 mg

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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:
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상품명:
CAS No.:
Species:
Purity:
수량:

YTB53

All MNK Isoforms

All PDGFR Isoforms

All Trk Receptor Isoforms

Biological Activity

Chemical Information

순도&문서

References

Calculators

Help & FAQs

YTB53 Related Classifications

HY-184431 Related Classifications

Bioz