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

Referencia número: HY-186045

Copy Link Print Information

SKLB06489

SKLB06489 is a selective and orally active inhibitor of type I PRMT enzymes, with IC₅₀ values of 64.55 nM (PRMT1), 4.21 nM (PRMT6), and 51.27 nM (PRMT8). SKLB06489 inhibits cell proliferation, colony formation, DNA replication, and DNA damage repair in cancer cells. SKLB06489 induces G0/G1-phase cell cycle arrest and apoptosis in cancer cells. SKLB06489 enhances intracellular cholesterol efflux via ABCA1 and ABCG1 upregulation, disrupts cholesterol metabolic homeostasis, and suppresses tumor growth in subcutaneous xenograft models. SKLB06489 can be used for the research of triple-negative breast cancer (TNBC).

Para uso exclusivo en investigación. No vendemos a pacientes.

Fòrmula: C₂₅H₃₃N₅O
Peso molecular:419.56

Almacenamiento:

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

Data Sheet (277 KB)

SKLB06489 Chemical Structure

Tamaño

Precio

Stock

Cantidad

Amount: USD 0.00

* Seleccione Cantidad antes de agregar artículos.

Use of MCE Products

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

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Pureza y Documentación
Referencias
Calculators
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

IC₅₀ & Target

PRMT1

64.55 nM (IC₅₀)

PRMT6

4.21 nM (IC₅₀)

PRMT8

51.27 nM (IC₅₀)

Ver todos los productos específicos de isoformas Histone Methyltransferase :

Ver todos los productos específicos de isoformas DNA/RNA Synthesis :

In Vitro

SKLB06489 (40 μM; 8 h) selectively and stably binds to PRMT1 and PRMT6 in HEK293T cells, enhancing their thermal stability^[1].
SKLB06489 (5-7 days) dose-dependently inhibits proliferation of MDA-MB-231, Hs578T, and BT549 TNBC cells with IC₅₀ values in the low micromolar range^[1].
SKLB06489 (2.5-20 μM; 12-14 days) dose-dependently inhibits colony formation in MDA-MB-231, Hs578T, and BT549 TNBC cells^[1].
SKLB06489 (2.5-10 μM; 6 days) dose-dependently reduces ADMA levels in MDA-MB-231 and Hs578T TNBC cells, indicating inhibition of type I PRMT enzymatic activity in cells^[1].
SKLB06489 (5-20 μM; 1-3 days) dose- and time-dependently inhibits DNA replication in MDA-MB-231, Hs578T, and BT549 TNBC cells^[1].
SKLB06489 (10 μM; 24 h) impairs DNA damage repair in MDA-MB-231 and Hs578T TNBC cells, with a more pronounced effect than MS023 in Hs578T cells^[1].
SKLB06489 (5-20 μM; 24 h) dose-dependently induces G₀/G₁ phase cell cycle arrest in MDA-MB-231, Hs578T, and BT549 TNBC cells^[1].
SKLB06489 (5-20 μM; 72 h) dose-dependently induces apoptosis in MDA-MB-231, Hs578T, and BT549 TNBC cells^[1].
SKLB06489 (10 μM; 4 days) upregulates ABCA1 and ABCG1 mRNA expression in MDA-MB-231 and Hs578T TNBC cells^[1].
SKLB06489 (5-10 μM; 4 days) dose-dependently enhances cholesterol efflux (increasing medium cholesterol) and reduces intracellular cholesterol in MDA-MB-231 and Hs578T TNBC cells^[1].
SKLB06489 (5-10 μM) upregulates ABCG1 protein levels in MDA-MB-231 and Hs578T TNBC cells^[1].

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

Western Blot Analysis^[1]

Cell Line:

MDA-MB-231 and Hs578T cells
Concentration:

2.5 μM, 5 μM, 10 μM
Incubation Time:

6 days
Result:

Dose-dependently reduced ADMA levels without affecting PRMT1 or PRMT6 expression.

Cell Cycle Analysis^[1]

Cell Line:

MDA-MB-231, Hs578T, and BT549 cells
Concentration:

5 μM, 10 μM, 20 μM
Incubation Time:

24 h
Result:

Dose-dependently increased the proportion of cells in G₀/G₁ phase and decreased the proportion in S phase.

Apoptosis Analysis^[1]

Cell Line:

MDA-MB-231, Hs578T, and BT549 cells
Concentration:

5 μM, 10 μM, 20 μM
Incubation Time:

72 h
Result:

Dose-dependently increased the percentage of apoptotic cells (early + late) in MDA-MB-231 (5.9% to 41.8% and 82.9%), Hs578T (20.7% to 68.4% and 79.9%), and BT549 (6.5% to 49.1% and 92.3%) cells at 10 and 20 μM, respectively.

Real Time qPCR^[1]

Cell Line:

MDA-MB-231 and Hs578T cells
Concentration:

10 μM
Incubation Time:

4 days
Result:

Significantly upregulated ABCA1 (15.93-fold in MDA-MB-231, 13.90-fold in Hs578T) and ABCG1 (4.64-fold in MDA-MB-231, 3.79-fold in Hs578T) mRNA expression.

Parmacokinetics

Species	Dose	Route	T_1/2	C_max	AUC_last	AUC_inf	T_max	Bioavailability
Mice^[1]	2 mg/kg	i.v.	3.47 h	2867 ng/mL	659 ng·h/mL	676 ng·h/mL	/	/
Mice^[1]	5 mg/kg	p.o.	4.26 h	262 ng/mL	1452 ng·h/mL	1495 ng·h/mL	1.00 h	88.4 %

In Vivo

SKLB06489 (40-80 mg/kg; i.g.; daily; 33 days) suppresses MDA-MB-231 tumor growth in vivo with a TGI of 58.4% at 80 mg/kg, inhibiting cell proliferation and inducing apoptosis^[1].

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

Animal Model:

BALB/c nude (female, aged 4-5 weeks, 6-week-old) bearing DA-MB-231 cells^[1]
Dosage:

40 mg/kg; 80 mg/kg
Administration:

i.g.; daily; 33 days
Result:

Dose-dependently suppressed tumor growth; had a tumor growth inhibition (TGI) value of 58.4% at 80 mg/kg; reduced tumor weight compared to vehicle control; increased cleaved caspase-3-positive cells; decreased Ki67-positive cells in tumor tissues.

Related Protocols :

Chemical Information

Peso molecular 419.56
Fòrmula C₂₅H₃₃N₅O
SMILES

CNCCN(CC1=NNC2=CC=C(C=C21)C3=CC=C(C=C3)NC(C4CCCCC4)=O)C
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (277 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)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Zhou SY, et al. Discovery of a potent and orally bioavailable type Ⅰ PRMTs inhibitor for triple-negative breast cancer treatment. Acta Pharmacol Sin. Published online January 16, 2026. [Content Brief]

Calculators

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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

Obtener un presupuesto En stock

Other size

Obtener un presupuesto

Amount: USD 0.00

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Pureza y Documentación
Referencias

Nombre del producto:
Referencia número:
Cantidad:
MCE Japan Authorized Agent:

Nombre del producto:
No. CAS:
Species:
Pureza:
Cantidad:

SKLB06489

Ver todos los productos específicos de isoformas Histone Methyltransferase

Ver todos los productos específicos de isoformas DNA/RNA Synthesis