RSL3

RSL3 ((1S,3R)-RSL3) 是一種谷胱甘肽過氧化物酶 4 (GPX4) 的抑制劑 (ferroptosis 激動(dòng)劑)，可降低 GPX4 的表達(dá)，誘導(dǎo)頭頸部癌細(xì)胞的肥大性死亡。在 HN3 耐受細(xì)胞中，可增加 p62 和 Nrf2 的蛋白水平，使 Keap1 滅活。貨號(hào)：HY-100218A ，CAS：1219810-16-8

參數(shù)品牌：MCE

產(chǎn)品參數(shù)

品牌：MCE

型號(hào)：HY-100218A

起訂量：1

規(guī)格:：2mg

價(jià)格:：￥950

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RSL3 (Synonyms: (1S,3R)-RSL3)

RSL3 ((1S,3R)-RSL3) 是一種谷胱甘肽過氧化物酶 4 (GPX4) 的抑制劑 (ferroptosis 激動(dòng)劑)，可降低 GPX4 的表達(dá)，誘導(dǎo)頭頸部癌細(xì)胞的肥大性死亡。在 HN3 耐受細(xì)胞中，可增加 p62 和 Nrf2 的蛋白水平，使 Keap1 滅活。

生物活性

RSL3 ((1S,3R)-RSL3) is an inhibitor of glutathione peroxidase 4 (GPX4) (ferroptosis activator), reduces the expression of GPX4 protein, and induces ferroptotic death of head and neck cancer cell. RSL3 increases the expression of p62 and Nrf2 and inactivates Keap1 in HN3-rslR cells^[1].

IC₅₀ & Target

Glutathione peroxidase 4^[1]

體外研究(In Vitro)

RSL3 (0-8 μM, 72 hours) potently reduces the viability of HN3 cells, with IC₅₀s of 0.48 μM in HN3 and 5.8 μM in HN3-rslR cells, respectively^[1].

RSL3 (0-8 μM, 24 hours) reduces the expression of GPX4 protein, increases the expression of p62 and Nrf2 and inactivates Keap1 in HN3-rslR cells^[1].

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

Cell Viability Assay^[1]

Cell Line:	HN3 cells, HN3-rslR cells
Concentration:	0-8 μM
Incubation Time:	72 hours
Result:	Showed IC₅₀s of 0.48 μM in HN3 and 5.8 μM in HN3-rslR cells, respectively^[1].

體內(nèi)研究(In Vivo)

RSL3 (100 mg/kg, Intratumorally twice per week for 20 days) significantly inhibits the growth of tumor in combination with trigonelline in mice bearing HN3R cells.

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

Animal Model:	Ten-week-old athymic BALB/c male nude mice (nu/nu) bearing HN3R cells^[1]
Dosage:	100 mg/kg in combination with trigonelline (50 mg/kg)
Administration:	Intratumorally twice per week for 20 days
Result:	Significantly reduced the volume of tumor combined with trigonelline in mice.

分子量：440.88

Formula：C₂₃H₂₁ClN₂O₅

CAS 號(hào)：1219810-16-8

運(yùn)輸條件：Room temperature in continental US; may vary elsewhere.

儲(chǔ)存方式：

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性數(shù)據(jù)

In Vitro:

DMSO : 250 mg/mL (567.05 mM; Need ultrasonic)

配制儲(chǔ)備液

濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg

1 mM	2.2682 mL	11.3410 mL	22.6819 mL
5 mM	0.4536 mL	2.2682 mL	4.5364 mL
10 mM	0.2268 mL	1.1341 mL	2.2682 mL

*

請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 儲(chǔ)存時(shí)，請?jiān)?6 個(gè)月內(nèi)使用，-20°C 儲(chǔ)存時(shí)，請?jiān)?1 個(gè)月內(nèi)使用。

In Vivo:

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：

——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

1.

請依序添加每種溶劑： 50% PEG300 50% saline
Solubility: 20 mg/mL (45.36 mM); Suspended solution; Need ultrasonic
2.

請依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: 5 mg/mL (11.34 mM); Suspended solution; Need ultrasonic
3.

請依序添加每種溶劑： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.67 mM); Clear solution
4.

請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (4.72 mM); Clear solution
5.

請依序添加每種溶劑： 10% DMF 90% corn oil
Solubility: ≥ 0.56 mg/mL (1.27 mM); Clear solution

參考文獻(xiàn)

[1]. Shin D, et al. Nrf2 inhibition reverses resistance to GPX4 inhibitor-induced ferroptosis in head and neck cancer. Free Radic Biol Med. 2018 Dec;129:454-462.

RSL3

RSL3 ((1S,3R)-RSL3) 是一種谷胱甘肽過氧化物酶 4 (GPX4) 的抑制劑 (ferroptosis 激動(dòng)劑)，可降低 GPX4 的表達(dá)，誘導(dǎo)頭頸部癌細(xì)胞的肥大性死亡。在 HN3 耐受細(xì)胞中，可增加 p62 和 Nrf2 的蛋白水平，使 Keap1 滅活。貨號(hào)：HY-100218A ，CAS：1219810-16-8

品牌：MCE

型號(hào)：HY-100218A

起訂量：1

規(guī)格:：2mg

價(jià)格:：￥950

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產(chǎn)品詳情

RSL3 (Synonyms: (1S,3R)-RSL3)

RSL3 ((1S,3R)-RSL3) 是一種谷胱甘肽過氧化物酶 4 (GPX4) 的抑制劑 (ferroptosis 激動(dòng)劑)，可降低 GPX4 的表達(dá)，誘導(dǎo)頭頸部癌細(xì)胞的肥大性死亡。在 HN3 耐受細(xì)胞中，可增加 p62 和 Nrf2 的蛋白水平，使 Keap1 滅活。

生物活性

RSL3 ((1S,3R)-RSL3) is an inhibitor of glutathione peroxidase 4 (GPX4) (ferroptosis activator), reduces the expression of GPX4 protein, and induces ferroptotic death of head and neck cancer cell. RSL3 increases the expression of p62 and Nrf2 and inactivates Keap1 in HN3-rslR cells^[1].

IC₅₀ & Target

Glutathione peroxidase 4^[1]

體外研究(In Vitro)

RSL3 (0-8 μM, 72 hours) potently reduces the viability of HN3 cells, with IC₅₀s of 0.48 μM in HN3 and 5.8 μM in HN3-rslR cells, respectively^[1].

RSL3 (0-8 μM, 24 hours) reduces the expression of GPX4 protein, increases the expression of p62 and Nrf2 and inactivates Keap1 in HN3-rslR cells^[1].

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

Cell Viability Assay^[1]

Cell Line:	HN3 cells, HN3-rslR cells
Concentration:	0-8 μM
Incubation Time:	72 hours
Result:	Showed IC₅₀s of 0.48 μM in HN3 and 5.8 μM in HN3-rslR cells, respectively^[1].

體內(nèi)研究(In Vivo)

RSL3 (100 mg/kg, Intratumorally twice per week for 20 days) significantly inhibits the growth of tumor in combination with trigonelline in mice bearing HN3R cells.

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

Animal Model:	Ten-week-old athymic BALB/c male nude mice (nu/nu) bearing HN3R cells^[1]
Dosage:	100 mg/kg in combination with trigonelline (50 mg/kg)
Administration:	Intratumorally twice per week for 20 days
Result:	Significantly reduced the volume of tumor combined with trigonelline in mice.

分子量：440.88

Formula：C₂₃H₂₁ClN₂O₅

CAS 號(hào)：1219810-16-8

運(yùn)輸條件：Room temperature in continental US; may vary elsewhere.

儲(chǔ)存方式：

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性數(shù)據(jù)

In Vitro:

DMSO : 250 mg/mL (567.05 mM; Need ultrasonic)

配制儲(chǔ)備液

濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg

1 mM	2.2682 mL	11.3410 mL	22.6819 mL
5 mM	0.4536 mL	2.2682 mL	4.5364 mL
10 mM	0.2268 mL	1.1341 mL	2.2682 mL

*

請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 儲(chǔ)存時(shí)，請?jiān)?6 個(gè)月內(nèi)使用，-20°C 儲(chǔ)存時(shí)，請?jiān)?1 個(gè)月內(nèi)使用。

In Vivo:

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：

——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

1.

請依序添加每種溶劑： 50% PEG300 50% saline
Solubility: 20 mg/mL (45.36 mM); Suspended solution; Need ultrasonic
2.

請依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: 5 mg/mL (11.34 mM); Suspended solution; Need ultrasonic
3.

請依序添加每種溶劑： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.67 mM); Clear solution
4.

請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (4.72 mM); Clear solution
5.

請依序添加每種溶劑： 10% DMF 90% corn oil
Solubility: ≥ 0.56 mg/mL (1.27 mM); Clear solution

參考文獻(xiàn)

[1]. Shin D, et al. Nrf2 inhibition reverses resistance to GPX4 inhibitor-induced ferroptosis in head and neck cancer. Free Radic Biol Med. 2018 Dec;129:454-462.

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RSL3

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RSL3 (Synonyms: (1S,3R)-RSL3)

RSL3

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RSL3 (Synonyms: (1S,3R)-RSL3)