2. Epigenetics Apoptosis Cell Cycle/DNA Damage Membrane Transporter/Ion Channel
  3. Histone Methyltransferase Apoptosis DNA/RNA Synthesis ATP-binding cassette (ABC) transporters
  4. 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).

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SKLB06489

SKLB06489 Chemical Structure

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SKLB06489 Related Antibodies

Top Publications Citing Use of Products

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EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 NSD3/WHSC1L1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

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View All Isoforms
RNASE L DNA Polymerases RNA Polymerases Helicases DNA Ligase

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Description

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)[1].

IC50 & Target

PRMT1

64.55 nM (IC50)

PRMT6

4.21 nM (IC50)

PRMT8

51.27 nM (IC50)

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.

SKLB06489 Related Antibodies

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 T1/2 Cmax AUClast AUCinf Tmax 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.
Molecular Weight

419.56

Formula

C25H33N5O
SMILES

CNCCN(CC1=NNC2=CC=C(C=C21)C3=CC=C(C=C3)NC(C4CCCCC4)=O)C
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
References
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SKLB06489 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SKLB06489SKLB 06489SKLB-06489Histone MethyltransferaseApoptosisDNA/RNA SynthesisATP-binding cassette (ABC) transportersATP-binding cassette transportersHEK293T cellsMDA-MB-231ABCG1Hs578TABCA1PRMT1BT549PRMT6PRMT8triple-negative breast cancerInhibitorinhibitorinhibit

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