Cat. No.: HY-173119

SKLB-D18

Name: SKLB-D18
Brand: MedChemExpress
SKU: HY-173119
Price: 200.00 USD
Availability: InStock
Rating: 5 (1 reviews)

고객리뷰

Based on 1 Customer Validation

SKLB-D18 is an orally active ERK1/2/ERK5 inhibitor, with an IC₅₀ of 38.69 nM and a K_d of 126.9 nM against human ERK1, an IC₅₀ of 40.12 nM and a K_d of 209.8 nM against ERK2, and an IC₅₀ of 59.72 nM and a K_d of 468.2 nM against ERK5. SKLB-D18 inhibits cancer cell proliferation, induces G0/G1 cell cycle arrest and apoptosis. SKLB-D18 reduces the levels of p-ERK5, p-RSKp90, p-c-Myc and c-Myc, and upregulates the level of p-ERK1/2, thereby inhibiting the ERK1/2/5 pathway in cells. SKLB-D18 increases LC3B-II accumulation, and decreases the levels of p62, p-mTOR and p-p70S6K. SKLB-D18 elevates the levels of ROS, lipid peroxidation and free ferrous ions, reduces the levels of NCOA4 and GPX4, and induces ferritin autophagy-dependent ferroptosis in cancer cells. SKLB-D18 exhibits antitumor activity in a triple-negative breast cancer xenograft mouse model. SKLB-D18 can be used in research related to triple-negative breast cancer.

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

Purity: 98.06%
화학식: C₂₂H₂₅ClN₆O₂S
분자량:472.99

보관:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

SKLB-D18 Chemical Structure

사이즈

가격

재고

수량

Amount: USD 0.00

* 장바구니에 담기 전 물품의 수량을 선택해 주십시오.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

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

Biological Activity

제품 설명

IC₅₀ & Target^[1]

ERK1

38.69 nM (IC₅₀)

ERK1

126.9 nM (Kd)

ERK2

40.12 nM (IC₅₀)

ERK2

209.8 nM (Kd)

ERK5

59.72 nM (IC₅₀)

ERK5

468.2 nM (Kd)

All ERK Isoforms :

All mTOR Isoforms :

In Vitro

SKLB-D18 (1 μM) exhibits high selectivity for ERK1, ERK2 and ERK5, with inhibition rates of 96%, 94% and 83% respectively at the concentration of 1 μM^[1].
SKLB-D18 (0-20 μM; 72 h) potently inhibits the proliferation of MDA-MB-231 (IC₅₀ 0.93 μM) and MDA-MB-468 (IC₅₀ 1.05 μM) in vitro, and this activity depends on the expression of ERK1/2/5^[1].
SKLB-D18 (2 μM; 2 h) directly binds to ERK1/2 and ERK5 proteins in intact MDA-MB-231 and MDA-MB-468 cells^[1].
SKLB-D18 (1-5 μM; 24 h) reduces the levels of p-ERK5, p-RSKp90, p-c-Myc and c-Myc in a dose-dependent manner, while upregulating the level of p-ERK1/2, thereby inhibiting the ERK1/2/5 pathway in MDA-MB-231 and MDA-MB-468 cells^[1].
SKLB-D18 (1-5 μM; 14 days) potently and dose-dependently inhibits the long-term clonogenic proliferation of MDA-MB-231 and MDA-MB-468 cells^[1].
SKLB-D18 (1-5 μM; 24 h) induces dose-dependent G0/G1 cell cycle arrest in MDA-MB-231 and MDA-MB-468 cells^[1].
SKLB-D18 (0.5-2 μM; 16 h) potently and dose-dependently inhibits the migration of MDA-MB-231 and MDA-MB-468 cells^[1].
SKLB-D18 (1-5 μM; 24 h) activates complete autophagic flux in MDA-MB-231 and MDA-MB-468 cells by inhibiting the mTOR/p70S6K pathway. After 24 h of treatment, increased accumulation of LC3B-II, and decreased levels of p62, p-mTOR and p-p70S6K are observed^[1].
SKLB-D18 (1-5 μM; 24 h) induces ferritinophagy-dependent ferroptosis in MDA-MB-231 and MDA-MB-468 cells by increasing the levels of ROS, lipid peroxidation and free ferrous ions, and decreasing the levels of NCOA4 and GPX4^[1].

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

Cell Viability Assay^[1]

Cell Line:

Triple-negative breast cancer (TNBC) cell lines MDA-MB-231, MDA-MB-468, MDA-MB-436, BT549; ERK1/2/5 knockdown MDA-MB-231 and MDA-MB-468 cells
Concentration:

0-20 μM
Incubation Time:

72 h
Result:

Inhibited cell viability in a dose-dependent manner, with IC₅₀ values of 0.93 μM (MDA-MB-231), 1.05 μM (MDA-MB-468), 2.31 μM (MDA-MB-436), and 3.21 μM (BT549).
Reduced anti-proliferative activity significantly in ERK1/2/5 knockdown MDA-MB-231 and MDA-MB-468 cells, with IC₅₀ values of 14.81 μM and 19.84 μM, respectively.

Western Blot Analysis^[1]

Cell Line:

MDA-MB-231 and MDA-MB-468 TNBC cells
Concentration:

1-5 μM
Incubation Time:

24 h
Result:

Reduced phosphorylated ERK5 (p-ERK5), phosphorylated RSKp90 (p-RSKp90), phosphorylated c-Myc (p-c-Myc), and total c-Myc levels in both cell lines in a dose-dependent manner.
Increased phosphorylated ERK1/2 (p-ERK1/2) levels in a dose-dependent manner, while total ERK1/2 and ERK5 levels remained unchanged.
Showed superior inhibition of p-ERK5, p-RSKp90, p-c-Myc, and c-Myc at 5 μM compared to a combination of BVD-523 and XMD8-92.

Cell Proliferation Assay^[1]

Cell Line:

MDA-MB-231 and MDA-MB-468 TNBC cells
Concentration:

1-5 μM
Incubation Time:

14 days
Result:

Reduced colony formation in both cell lines in a dose-dependent manner.

Cell Cycle Analysis^[1]

Cell Line:

MDA-MB-231 and MDA-MB-468 TNBC cells
Concentration:

1-5 μM
Incubation Time:

24 h
Result:

Induced G0/G1 phase cell cycle arrest in both MDA-MB-231 and MDA-MB-468 cells in a dose-dependent manner, with significant arrest observed at all tested concentrations.

Cell Migration Assay ^[1]

Cell Line:

MDA-MB-231 and MDA-MB-468 TNBC cells
Concentration:

0.5-2 μM
Incubation Time:

16 h
Result:

Reduced the number of migrated cells in both cell lines in a dose-dependent manner.

Cell Autophagy Assay^[1]

Cell Line:

MDA-MB-231 and MDA-MB-468 TNBC cells
Concentration:

1-5 μM (LC3/p62 immunoblotting); 5 μM (LC3 immunofluorescence, mTOR/p70S6K immunoblotting, autophagic flux assay with ±10 nM bafilomycin A1)
Incubation Time:

24 h
Result:

Increased LC3B-II accumulation and reduced p62 levels in a dose-dependent manner.
Enhanced LC3 fluorescence intensity.
Induced complete autophagic flux, as confirmed by mRFP-GFP-LC3 assay with reduced green fluorescence when co-treated with bafilomycin A1.
Reduced phosphorylated mTOR (p-mTOR) and phosphorylated p70S6K (p-p70S6K) levels.

Parmacokinetics

Species	Dose	Route	T_1/2	C_max	AUC_0-t	AUC_0-∞	V_ss	V_z	CL	Bioavailability
Rat^[1]	10 mg/kg	p.o.	3.71 h	53.71 ng/mL	303.93 ng·h/mL	456.92 ng·h/mL	/	/	/	22.42 %
Rat^[1]	1 mg/kg	i.v.	2.01 h	58.72 ng/mL	135.56 ng·h/mL	143.25 ng·h/mL	16990.99 mL/kg	20240.48 mL/kg	116.52 mL/min/kg	/

In Vivo

SKLB-D18 (25-50 mg/kg; p.o.; once daily; for 16 consecutive days) inhibits triple-negative breast cancer tumor growth in a dose-dependent manner in subcutaneous xenograft mouse models^[1].

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

Animal Model:

BALB/c-nu nude mice (female, 6 weeks old, 17-19 g, subcutaneous xenograft model)^[1]
Dosage:

25 mg/kg; 50 mg/kg
Administration:

p.o.; daily; 16 days
Result:

Achieved a tumor inhibition rate of 59.23% relative to the control group at 25 mg/kg.
Achieved a tumor inhibition rate of 79.88% relative to the control group at 50 mg/kg, which was superior to the combination of BVD-523 and XMD8-92 (72.66% inhibition).
Caused a dose-dependent decrease in Ki-67-positive tumor cells, with less than 20% Ki-67-positive area in the 50 mg/kg group.
Induced a dose-dependent accumulation of p-ERK1/2 in tumor tissues, while dose-dependently inhibiting p-ERK5 expression, with stronger p-ERK5 inhibition at 50 mg/kg than the BVD-523 and XMD8-92 combination group.
Showed no significant body weight loss or major organ toxicity in either treatment group.

Chemical Information

Appearance Solid
분자량 472.99
화학식 C₂₂H₂₅ClN₆O₂S
Color Off-white to light yellow
SMILES

CN(C)CC1=CC=CC(NC2=NC(C3=CSC(C(NN4CCOCC4)=O)=C3)=C(Cl)C=N2)=C1
선적

Room temperature in continental US; may vary elsewhere.

보관

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

용액&용해도

In Vitro:

DMSO : 35 mg/mL (74.00 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1142 mL

10.5710 mL

21.1421 mL

5 mM

0.4228 mL

2.1142 mL

4.2284 mL

10 mM

0.2114 mL

1.0571 mL

2.1142 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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)

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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]. Xiao H, et al. A first-in-class selective inhibitor of ERK1/2 and ERK5 overcomes drug resistance with a single-molecule strategy. Signal Transduct Target Ther. 2025;10(1):70. Published 2025 Feb 20. [Content Brief]

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.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.1142 mL	10.5710 mL	21.1421 mL	52.8552 mL
	5 mM	0.4228 mL	2.1142 mL	4.2284 mL	10.5710 mL
	10 mM	0.2114 mL	1.0571 mL	2.1142 mL	5.2855 mL
	15 mM	0.1409 mL	0.7047 mL	1.4095 mL	3.5237 mL
	20 mM	0.1057 mL	0.5286 mL	1.0571 mL	2.6428 mL
	25 mM	0.0846 mL	0.4228 mL	0.8457 mL	2.1142 mL
	30 mM	0.0705 mL	0.3524 mL	0.7047 mL	1.7618 mL
	40 mM	0.0529 mL	0.2643 mL	0.5286 mL	1.3214 mL
	50 mM	0.0423 mL	0.2114 mL	0.4228 mL	1.0571 mL
	60 mM	0.0352 mL	0.1762 mL	0.3524 mL	0.8809 mL

Bioz

Keywords

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

상품명:
CAS No.:
Species:
Purity:
수량:

SKLB-D18

All ERK Isoforms

All mTOR Isoforms

Biological Activity

Chemical Information

용액&용해도

순도&문서

References

Help & FAQs

Complete Stock Solution Preparation Table

SKLB-D18 Related Classifications

HY-173119 Related Classifications

Bioz