PROTAC MLKL Degrader-1

Name: PROTAC MLKL Degrader-1
Brand: MedChemExpress
SKU: HY-156591
Rating: 4.5 (0 reviews)

Cat. No.: HY-156591 Purity: 99.76%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

PROTAC MLKL Degrader-1 is a selective MLKL PROTAC degrader with a DC₅₀ of 2.4 μM. PROTAC MLKL Degrader-1 blocks necroptosis without modulating the phosphorylation of RIPK1 or RIPK3, and exhibits a linear correlation between MLKL levels and necroptotic cell death.
(Pink: Mixed Lineage Kinase Target protein ligand; Blue: Cereblon ligand (HY-W249500); Black: linker).

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PROTAC MLKL Degrader-1 화학구조

CAS No. : 3032600-90-8

사이즈	재고	수량
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	해외재고보유	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	해외재고보유	Estimated Time of Arrival: December 31
Solid
5 mg	해외재고보유	Estimated Time of Arrival: December 31
10 mg	해외재고보유	Estimated Time of Arrival: December 31
25 mg	해외재고보유	Estimated Time of Arrival: December 31
50 mg	해외재고보유	Estimated Time of Arrival: December 31
100 mg	해외재고보유	Estimated Time of Arrival: December 31
200 mg	견적 받기
500 mg	견적 받기

or 대량구매 문의

* 장바구니에 담기 전 물품의 수량을 선택해 주십시오.

This product is a controlled substance and not for sale in your territory.

고객리뷰

Based on 1 Customer Validation

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

Biological Activity
순도&문서
References
고객리뷰

제품 설명

PROTAC MLKL Degrader-1 is a selective MLKL PROTAC degrader with a DC₅₀ of 2.4 μM. PROTAC MLKL Degrader-1 blocks necroptosis without modulating the phosphorylation of RIPK1 or RIPK3, and exhibits a linear correlation between MLKL levels and necroptotic cell death^[1]. (Pink: Mixed Lineage Kinase Target protein ligand; Blue: Cereblon ligand (HY-W249500); Black: linker).

IC₅₀ & Target^[1]

Cereblon

Cellular Effect

Cell Line	Type	Value	Description	References
HT-29	EC₅₀	1.2 μM Compound: 36	Protection against TSZ-induced necroptosis in human HT-29 cells assessed as cell viability incubated for 24 hrs by CellTiter Glo assay Protection against TSZ-induced necroptosis in human HT-29 cells assessed as cell viability incubated for 24 hrs by CellTiter Glo assay	[PMID: 37535857]

In Vitro

PROTAC MLKL Degrader-1 (Compound 36) (0.1-10 μM; 2-24 h) dose-dependently degrades MLKL in HT29 cells, with a DC₅₀ of 2.4 μM. It achieves a degradation rate of > 90% within 5 h at a concentration of 10 μM, and this effect lasts for up to 24 h^[1].
PROTAC MLKL Degrader-1 (0.1-10 μM; 24 h) dose-dependently protects HT29 cells against TSZ-induced necroptosis, with an EC₅₀ of 1.2 μM^[1].

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

Cell Viability Assay^[1]

Cell Line:	HT29 colon cancer cells
Concentration:	0.1, 0.3, 1, 3 and 10 μM
Incubation Time:	24 h
Result:	Protected cells from necroptosis in a dose-dependent manner, reaching 100% protection at 10 μM, with an EC₅₀ of 1.2 μM. Demonstrated anti-necroptotic efficacy that correlated linearly with the extent of MLKL degradation.

분자량

948.05

화학식

C₄₆H₅₅F₂N₉O₉S

CAS No.

3032600-90-8

Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(C1=C(NN=C1C2=CC=C(C=C2)NS(C(F)F)(=O)=O)NC3=CC=CC(OCCCCCCCC(N4CCC5(CCN(CC5)C(C6=CC=C(C(N7CCC(NC7=O)=O)=C6)OC)=O)CC4)=O)=C3)N

선적

Room temperature in continental US; may vary elsewhere.

보관

4°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

용액&용해도

In Vitro:

DMSO : 100 mg/mL (105.48 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.0548 mL	5.2740 mL	10.5480 mL
5 mM	0.2110 mL	1.0548 mL	2.1096 mL
10 mM	0.1055 mL	0.5274 mL	1.0548 mL

View the Complete Stock Solution Preparation Table

* 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 (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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In Vivo Dissolution Calculator

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순도&문서

Purity: 99.76%

Select Batch:

Data Sheet (270 KB) SDS (252 KB)

COA (245 KB) HNMR (322 KB) RP-HPLC (257 KB) LCMS (138 KB)

Handling Instructions (2659 KB)

References

[1]. Rathje OH, et al. PROTACs Targeting MLKL Protect Cells from Necroptosis. J Med Chem. 2023;66(16):11216-11236. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.0548 mL	5.2740 mL	10.5480 mL	26.3699 mL
	5 mM	0.2110 mL	1.0548 mL	2.1096 mL	5.2740 mL
	10 mM	0.1055 mL	0.5274 mL	1.0548 mL	2.6370 mL
	15 mM	0.0703 mL	0.3516 mL	0.7032 mL	1.7580 mL
	20 mM	0.0527 mL	0.2637 mL	0.5274 mL	1.3185 mL
	25 mM	0.0422 mL	0.2110 mL	0.4219 mL	1.0548 mL
	30 mM	0.0352 mL	0.1758 mL	0.3516 mL	0.8790 mL
	40 mM	0.0264 mL	0.1318 mL	0.2637 mL	0.6592 mL
	50 mM	0.0211 mL	0.1055 mL	0.2110 mL	0.5274 mL
	60 mM	0.0176 mL	0.0879 mL	0.1758 mL	0.4395 mL
	80 mM	0.0132 mL	0.0659 mL	0.1318 mL	0.3296 mL
	100 mM	0.0105 mL	0.0527 mL	0.1055 mL	0.2637 mL