製品番号: HY-189213

YZ-17

YZ-17 is a PROTAC degrader targeting PRMT5, with DC₅₀ = 2.2 μM (HCC1806 cells). YZ-17 recruits CRBN E3 ligase and induces PRMT5 degradation through the ubiquitin-proteasome system, inhibiting PRMT5-mediated symmetric dimethylarginine modification. YZ-17 co-degrades the PRMT5 adaptor protein MEP50 via a CRBN-dependent mechanism. YZ-17 induces G1 phase cell cycle arrest and inhibits colony formation in cancer cells. YZ-17 exhibits antiproliferative activity in various cancer cells. YZ-17 shows antitumor efficacy in a triple-negative breast cancer xenograft mouse model. YZ-17 can be used for research on triple-negative breast cancer.
(Pink: PRMT5 Target protein ligand; Blue: Cereblon ligand (HY-14658); Black: linker).

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分子式: C₄₉H₅₃N₇O₆
分子量:835.99

保管条件:

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

YZ-17 構造式

価格（税別）

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

Use of MCE Products

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

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- Parmacokinetics
- 体内実験
化学情報
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
Bioz

生物活性

製品説明

YZ-17 is a PROTAC degrader targeting PRMT5, with DC₅₀ = 2.2 μM (HCC1806 cells). YZ-17 recruits CRBN E3 ligase and induces PRMT5 degradation through the ubiquitin-proteasome system, inhibiting PRMT5-mediated symmetric dimethylarginine modification. YZ-17 co-degrades the PRMT5 adaptor protein MEP50 via a CRBN-dependent mechanism. YZ-17 induces G1 phase cell cycle arrest and inhibits colony formation in cancer cells. YZ-17 exhibits antiproliferative activity in various cancer cells. YZ-17 shows antitumor efficacy in a triple-negative breast cancer xenograft mouse model. YZ-17 can be used for research on triple-negative breast cancer^[1]. (Pink: PRMT5 Target protein ligand; Blue: Cereblon ligand (HY-14658); Black: linker).

IC₅₀ & Target

^[1]

PRMT5

PROTACs アイソフォーム固有の製品をすべて表示 :

Histone Methyltransferase アイソフォーム固有の製品をすべて表示 :

Cellular Effect

Cell Line	Type	Value	Description	References
HCC1806	DC₅₀	2.2 μM	Concentration-dependent PRMT5 degradation in HCC1806 triple-negative breast cancer cells assessed by Western blot analysis after 24 h incubation. Concentration-dependent PRMT5 degradation in HCC1806 triple-negative breast cancer cells assessed by Western blot analysis after 24 h incubation.	42566881
HCC1937	DC₅₀	3.3 μM	Concentration-dependent PRMT5 degradation in HCC1937 triple-negative breast cancer cells assessed by Western blot analysis after 24 h incubation. Concentration-dependent PRMT5 degradation in HCC1937 triple-negative breast cancer cells assessed by Western blot analysis after 24 h incubation.	42566881
HCC1806	DC₅₀	2.0 μM	Concentration-dependent MEP50 degradation in HCC1806 triple-negative breast cancer cells assessed by Western blot analysis after 24 h incubation. Concentration-dependent MEP50 degradation in HCC1806 triple-negative breast cancer cells assessed by Western blot analysis after 24 h incubation.	42566881
HCC1937	DC₅₀	2.9 μM	Concentration-dependent MEP50 degradation in HCC1937 triple-negative breast cancer cells assessed by Western blot analysis after 24 h incubation. Concentration-dependent MEP50 degradation in HCC1937 triple-negative breast cancer cells assessed by Western blot analysis after 24 h incubation.	42566881
HCC1806	IC50	3.3 μM	Antiproliferative activity against HCC1806 triple-negative breast cancer cells assessed by CCK-8 assay after 24 h incubation followed by 3 h CCK-8 reagent incubation. Antiproliferative activity against HCC1806 triple-negative breast cancer cells assessed by CCK-8 assay after 24 h incubation followed by 3 h CCK-8 reagent incubation.	42566881
HCC1937	IC50	2.6 μM	Antiproliferative activity against HCC1937 triple-negative breast cancer cells assessed by CCK-8 assay after 24 h incubation followed by 3 h CCK-8 reagent incubation. Antiproliferative activity against HCC1937 triple-negative breast cancer cells assessed by CCK-8 assay after 24 h incubation followed by 3 h CCK-8 reagent incubation.	42566881
MDA-MB-231	IC50	3.6 μM	Antiproliferative activity against MDA-MB-231 triple-negative breast cancer cells assessed by CCK-8 assay after 24 h incubation followed by 3 h CCK-8 reagent incubation. Antiproliferative activity against MDA-MB-231 triple-negative breast cancer cells assessed by CCK-8 assay after 24 h incubation followed by 3 h CCK-8 reagent incubation.	42566881
MDA-MB-468	IC50	3.7 μM	Antiproliferative activity against MDA-MB-468 triple-negative breast cancer cells assessed by CCK-8 assay after 24 h incubation followed by 3 h CCK-8 reagent incubation. Antiproliferative activity against MDA-MB-468 triple-negative breast cancer cells assessed by CCK-8 assay after 24 h incubation followed by 3 h CCK-8 reagent incubation.	42566881
MCF-10A	IC50	>8.0 μM	Antiproliferative activity against normal MCF10A human breast epithelial cells assessed by CCK-8 assay after 24 h incubation followed by 3 h CCK-8 reagent incubation. Antiproliferative activity against normal MCF10A human breast epithelial cells assessed by CCK-8 assay after 24 h incubation followed by 3 h CCK-8 reagent incubation.	42566881

体外実験

YZ-17 (1-5 μM; 12 h) achieves 61.29% PRMT5 degradation at 5 μM in HCC1806 cells^[1].
YZ-17 (0.5-6.0 μM; 24 h) potently degrades PRMT5 (DC₅₀ = 2.2 μM) and its associated adaptor protein MEP50 (DC₅₀ = 2.0 μM) in HCC1806 cells, and degrades PRMT5 (DC₅₀ = 3.3 μM) and MEP50 (DC₅₀ = 2.9 μM) in HCC1937 cells^[1].
YZ-17 (0.5-6.0 μM; 24 h) effectively inhibits the catalytic activity of PRMT5, and treatment at 6 μM for 24 h almost completely eliminates PRMT5-dependent sDMA modification in HCC1806 cells^[1].
YZ-17 (4.5 μM; 6-36 h) degrades PRMT5 and MEP50 in a time-dependent manner, with nearly complete elimination of both proteins in HCC1806 and HCC1937 cells after treatment at 4.5 μM for 36 h^[1].
YZ-17 (4.5 μM; 24 h initial treatment, followed by 6 h co-incubation period) mediates the degradation of PRMT5 and MEP50 through a classic PROTAC mechanism, a process that requires simultaneous binding to CRBN and PRMT5 and depends on an intact ubiquitin-proteasome system^[1].
YZ-17 (0-8.0 μM; 24 h) exhibits potent and selective antiproliferative activity against triple-negative breast cancer cell lines (IC₅₀ range: 2.6-3.7 μM), with minimal toxicity to normal mammary epithelial MCF10A cells^[1].
YZ-17 (1-5 μM; 24 h) induces concentration-dependent G1 phase cell cycle arrest in HCC1806 and HCC1937 triple-negative breast cancer cells^[1].
YZ-17 (0.5-2.0 μM; 24 h initial treatment, followed by 14 days of culture without treatment) potently and persistently inhibits the clonogenic growth of triple-negative breast cancer cells, almost completely eliminating colony formation in HCC1806 and HCC1937 cells at 2 μM^[1].
YZ-17 (1-5 μM; 48 h) inhibits the proliferation of HCC1806 triple-negative breast cancer cells by up to 96.0% after 48 h of treatment at a concentration of 5 μM^[1].

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

Western Blot Analysis^[1]

Cell Line:

HCC1806 triple-negative breast cancer cells
Concentration:

1, 5 μM
Incubation Time:

12 h
Result:

Reduced PRMT5 protein levels by 53.16% at 1 μM, and by 61.29% at 5 μM after 12 h of treatment, representing the highest PRMT5 degradation activity among the evaluated targeted chimeric degrader series at these concentrations.

Western Blot Analysis^[1]

Cell Line:

HCC1806 and HCC1937 triple-negative breast cancer cell lines
Concentration:

0.5, 1, 2, 4, 6, 6.0 μM
Incubation Time:

24 h
Result:

Degraded PRMT5 in a concentration-dependent manner, with a DC50 value of 2.2 μM in HCC1806 cells and 3.3 μM in HCC1937 cells.
Degraded the PRMT5 adaptor protein MEP50 in a concentration-dependent manner, with a DC50 value of 2.0 μM in HCC1806 cells and 2.9 μM in HCC1937 cells.\nReduced sDMA levels by 70.31% at 4 μM, and by 91.94% at 6 μM in HCC1806 cells.
Reduced sDMA levels by 51.95% at 4 μM, and by 71.56% at 6 μM in HCC1937 cells.

Western Blot Analysis^[1]

Cell Line:

HCC1806 and HCC1937 triple-negative breast cancer cell lines
Concentration:

4.5 μM
Incubation Time:

6, 12, 24, 36 h
Result:

Achieved substantial PRMT5 and MEP50 degradation within 24 h, and reached near-complete degradation of both proteins by 36 h in both tested TNBC cell lines.

Western Blot Analysis^[1]

Cell Line:

HCC1806 triple-negative breast cancer cells
Concentration:

4.5 μM
Incubation Time:

24 h initial treatment, followed by 6 h co-incubation period
Result:

Was significantly attenuated in its induced PRMT5 and MEP50 degradation by the CRBN ligand pomalidomide, the NEDD8-activating enzyme inhibitor MLN4924, the proteasome inhibitor MG132, and the parental PRMT5 inhibitor PJ-68, confirming the degradation process is dependent on CRBN recruitment, functional cullin neddylation, active proteasome function, and direct PRMT5 binding by YZ-17.

Cell Viability Assay^[1]

Cell Line:

HCC1806, HCC1937, MDA-MB-231, MDA-MB-468 triple-negative breast cancer cell lines, and normal MCF10A human breast epithelial cells
Concentration:

0-8.0 μM
Incubation Time:

24 h
Result:

Exhibited potent antiproliferative activity across the four tested TNBC cell lines, with IC50 values of 3.3 μM in HCC1806, 2.6 μM in HCC1937, 3.6 μM in MDA-MB-231, and 3.7 μM in MDA-MB-468.
Showed very low toxicity toward normal MCF10A breast epithelial cells, with an IC50 value greater than 8.0 μM, producing only 24.04% inhibition at 8 μM.

Cell Cycle Analysis^[1]

Cell Line:

HCC1806 and HCC1937 triple-negative breast cancer cell lines
Concentration:

1, 5 μM
Incubation Time:

24 h
Result:

Induced G1 phase cell cycle arrest in both HCC1806 and HCC1937 cells in a concentration-dependent manner.

Cell Viability Assay^[1]

Cell Line:

HCC1806 triple-negative breast cancer cells
Concentration:

1, 5 μM
Incubation Time:

48 h
Result:

Produced 31.4% cell viability inhibition at 1 μM, and 96.0% cell viability inhibition at 5 μM.

Parmacokinetics

Species	Dose	Route	T_1/2	T_max	C_max	AUC_0-t	AUC_0-∞	MRT_0-t	MRT_0-∞
Rat^[1]	10 mg/kg	i.p.	3.73 h	0.44 h	329.38 ng/mL	1157.86 ng·h/mL	1426.97 ng·h/mL	2.87 h	4.61 h
Rat^[1]	20 mg/kg	p.o.	0.62 h	1.00 h	141.00 ng/mL	475.74 ng·h/mL	716.23 ng·h/mL	3.02 h	7.65 h

体内実験

YZ-17 (30 mg/kg; i.p.; every other day; 4 total injections) exerts in vivo antitumor efficacy with a 44.12% tumor growth inhibition rate at 30 mg/kg administered every other day via intraperitoneal injection, without observable toxicity to body weight, kidney or liver in the HCC1806 TNBC xenograft mouse model^[1].

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

Animal Model:

nude mice (Female, 6 weeks old)^[1]
Dosage:

30 mg/kg
Administration:

i.p.; every other day; 4 total injections (8-day study period)
Result:

Achieved a tumor growth inhibition (TGI) of 44.12%.
Showed no significant changes in mouse body weight during the study period.
Produced serum levels of creatinine (Cr), alanine aminotransferase (ALT), and aspartate aminotransferase (AST) comparable to control group levels, with no detectable adverse effects on kidney or liver function.

化学情報

分子量 835.99
分子式 C₄₉H₅₃N₇O₆
SMILES

O=C(NC1CCN(CC2CN(C3=CC4=C(C(N(C(CC5)C(NC5=O)=O)C4=O)=O)C=C3)C2)CC1)COC6=CC=C7C(C(CCC7)NCC8=CC(C9=C(C=CC=C9)N%10CC)=C%10C=C8)=C6
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

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

純度とドキュメンテーション

取扱説明書 (2659 KB)

参考文献

[1]. Li Y, et al. Discovery of novel cereblon-recruiting PRMT5 degraders with in vivo efficacy against triple-negative breast cancer. European journal of medicinal chemistry. 2026 Nov 15;318:119199. [Content Brief]

Calculators

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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.

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YZ-17

PROTACs アイソフォーム固有の製品をすべて表示

Histone Methyltransferase アイソフォーム固有の製品をすべて表示

生物活性