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Cat. No.: HY-191092

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YP200

YP200 is a potent and selective HDAC11 inhibitor (IC₅₀ 0.058 μM). YP200 stabilizes SHMT2 and induces SHMT2 protein accumulation. YP200 induces Apoptosis and G0/G1 cell cycle arrest. YP200 does not affect the levels of acetylated α-tubulin or acetylated histone H3. YP200 reduces the expression of Ki67 and Cyclin D1 in tumor tissues. YP200 can be used for research on non-small cell lung cancer (NSCLC).

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

Formula: C₃₁H₃₈N₄O₄
Molecular Weight:530.66

Storage:

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

Data Sheet (281 KB)

YP200 Chemical Structure

Price

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Amount: USD 0.00

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Use of MCE Products

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

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

Biological Activity

Description

IC₅₀ & Target

^[1]

HDAC11

0.058 μM (IC₅₀)

HDAC6

5.98 μM (IC₅₀)

SHMT2

All HDAC Isoforms :

All SHMT Isoforms :

SHMT1
SHMT2

All CDK Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC50	7.12 μM	Antiproliferative activity against human A549 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay. Antiproliferative activity against human A549 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.	5451896
PC-9	IC50	8.45 μM	Antiproliferative activity against human PC-9 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay. Antiproliferative activity against human PC-9 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.	5451896
HCC827	IC50	3.14 μM	Antiproliferative activity against human HCC827 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay. Antiproliferative activity against human HCC827 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.	5451896
NCI-H1299	IC50	3.82 μM	Antiproliferative activity against human NCI-H1299 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay. Antiproliferative activity against human NCI-H1299 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.	5451896

In Vitro

Anti-cancerApoptosisCell Cycle RegulationProtein/Amino Acid MetabolismOthers

Anti-cancer

YP200 (72 h) reduces viability of A549, PC-9, HCC827, and NCI-H1299 NSCLC cells with IC₅₀ values of 7.12, 8.45, 3.14, and 3.82 µM, respectively^[1].
YP200 does not alter acetylated α-tubulin or acetylated histone H3 levels in NSCLC cells^[1].

Anti-cancer

Apoptosis

YP200 (2.5-10 µM; 72 h) induces concentration-dependent apoptosis in A549 cells, reaching 98.41% apoptotic population at 10.0 µM after 72 h^[1].

Anti-cancer

Cell Cycle Regulation

YP200 (1.25-5 µM; 24 h) induces G0/G1 cell cycle arrest in A549 cells, with 86.8% of cells in G0/G1 at 5.0 µM after 24 h^[1].

Protein/Amino Acid Metabolism

YP200 (0.2-20 µM; 24 h) increases SHMT2 accumulation in HEK293T cells at 0.2, 2.0, and 20 µM after 24 h^[1].

Others

YP200 (up to 10 µM) is a potent HDAC11 inhibitor with IC₅₀ 0.058 µM and 103-fold selectivity over HDAC6 in recombinant enzyme assays^[1].

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

Cell Viability Assay^[1]

Cell Line:

human NSCLC cell lines A549, PC-9, HCC827, and NCI-H1299; normal cell lines
Concentration:

increasing concentrations
Incubation Time:

72 h
Result:

IC₅₀ values were 7.12 µM in A549, 8.45 µM in PC-9, 3.14 µM in HCC827, and 3.82 µM in NCI-H1299 cells.
IC₅₀ against normal cell lines was >10 µM.

Apoptosis Analysis^[1]

Cell Line:

A549 human NSCLC cells
Concentration:

2.5, 5.0, and 10.0 µM
Incubation Time:

72 h
Result:

At 2.5 µM, Q2 was 32.50% and Q3 was 1.91%; at 5.0 µM, Q2 was 54.61% and Q3 was 2.44%; at 10.0 µM, Q2 was 85.53% and Q3 was 12.88%.
At 10.0 µM for 72 h, the apoptotic population increased to 98.41%.

Cell Cycle Analysis^[1]

Cell Line:

A549 human NSCLC cells
Concentration:

1.25, 2.5, and 5.0 µM
Incubation Time:

24 h
Result:

Induced G0/G1 phase arrest, with the G0/G1 fraction reaching 86.8% at 5.0 µM.

Western Blot Analysis^[1]

Cell Line:

HEK293T cells
Concentration:

0.2, 2.0, and 20 µM (YP200); 50 µM (Alk14)
Incubation Time:

24 h
Result:

Induced dose-dependent accumulation of SHMT2 at 0.2, 2.0, and 20 µM.

Parmacokinetics

Species	Dose	Route	C_max	T_max	AUC_0-last	Bioavailability	T_1/2	MRT_0-last	F
Mice^[1]	10 mg/kg	p.o.	167.07 μg/L	5.00 min	147.78 μg/L·h	/	122.00 min	112.00 min	6.25 %
Mice^[1]	10 mg/kg	i.v.	3548.14 μg/L	5.00 min	2363.98 μg/L·h	/	104.00 min	72.00 min	/
Mice^[1]	10 mg/kg	i.p.	1935.96 μg/L	16.68 min	4227.69 μg/L·h	100.00 %	/	/	/

In Vivo

Anti-cancerCell Cycle Regulation

Anti-cancer

Cell Cycle Regulation

YP200 (25-50 mg/kg; intraperitoneal; once daily; day 1 to day 20) suppresses tumor growth in the NSCLC PDX model and decreases tumor Ki67 and Cyclin D1 expression^[1].

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

Animal Model:

NOD/SCID (male, 4-6 weeks old)^[1]
Dosage:

25 mg/kg; 50 mg/kg
Administration:

intraperitoneal; once daily; day 1 to day 20
Result:

Suppressed tumor growth at both 25 mg/kg and 50 mg/kg; a clear dose-dependent difference between the two doses was not established.
Ki67 and Cyclin D1 expression in tumor tissue decreased dose-dependently with increasing dose.

Related Protocols :

Chemical Information

Molecular Weight 530.66
Formula C₃₁H₃₈N₄O₄
SMILES

O=C(NO)C(C=C1)=C(OC)C=C1CN2C3=CC=C(C(NCCNC[C@]4(CC5C6)CC6CC(C5)C4)=O)C=C3C=C2
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 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]. Yang X, et al. Development of a Potent and Isoform-Selective HDAC11 Inhibitor with Anti-Tumor Efficacy against Non-Small Cell Lung Cancer[J]. Journal of Medicinal Chemistry.

Calculators

Molarity Calculator

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

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

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

Product Name:
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YP200

All HDAC Isoforms

All SHMT Isoforms

All CDK Isoforms