PROTAC BRD2/BRD4 degrader-1

发表于2026年1月10日由上海金畔生物科技有限公司

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

PROTAC BRD2/BRD4 degrader-1

PROTAC BRD2/BRD4 degrader-1 (compound 15) 是一种高效、选择性的 BET 蛋白 BRD4 和 BRD2 降解剂，由Cereblon配体和BET配体相连。PROTAC BRD2/BRD4 degrader-1 快速诱导 BRD4 和 BRD2 的可逆、持久和选择性去除。它能够抑制肿瘤生长并具有低毒性。PROTAC BRD2/BRD4 degrader-1 由 BET 抑制剂、 linker 和 cereblon (CRBN)/cullin 4A 配体组成。

PROTAC BRD2/BRD4 degrader-1 Chemical Structure

CAS No. : 2570470-42-5

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生物活性

PROTAC BRD2/BRD4 degrader-1 (compound 15) is a potent and selective BET protein BRD4 and BRD2 degrader, connected by ligands for Cereblon and BET. PROTAC BRD2/BRD4 degrader-1 rapidly induces reversible, long-lasting, and unexpectedly selective removal of BRD4 and BRD2 over BRD3. It effectively inhibits solid tumors with low cytotoxic effect. PROTAC BRD2/BRD4 degrader-1 is composed of the BET inhibitor, a linker, and the ligand thalidomide for cereblon (CRBN)/cullin 4A^[1].

IC₅₀ & Target^[1]

BRD4

BRD2

Cereblon

体外研究
(In Vitro)

PROTAC BRD2/BRD4 degrader-1 (100 nM; ≥8 hours) shows anti-proliferation activity with IC₅₀ value of 12.25 nM, and the BRD4 protein is reduced very efficiently at treatment time of ≥8 h in MV4-11 cells^[1].
PROTAC BRD2/BRD4 degrader-1 (100 nM; ≥8 hours) shows anti-proliferation activity with IC₅₀ value of 12.25 nM, and the BRD4 protein is reduced very efficiently at treatment time of ≥8 h in MV4-11 cells^[1].
PROTAC BRD2/BRD4 degrader-1 (1 nM, 3 nM, 0.1 μM, 0.3 μM; 24-48 hours) induces MV4-11 apoptosis lines^[1].
PROTAC BRD2/BRD4 degrader-1 exhibits excellent anti-proliferative activity in 6 leukemia cell lines of NCI. Among them, the GI₅₀ values of the three leukemia cell lines were lower than 50 nM, consistent with the activity of leukemia MV4-11 cells^[1].
PROTAC BRD2/BRD4 degrader-1 has good anti-proliferation activity including prostate Cancer (22RV1 IC₅₀: 0.081 μM), colon cancer (colo-205 IC₅₀: 0.1557 μM) and thyroid cancer(TT IC₅₀: 0.037451 μM)^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[1]

Cell Line:	MV4-11 leukemia cells
Concentration:	100 nM
Incubation Time:	≥8 hours
Result:	The BRD4 protein was reduced very efficiently.

Western Blot Analysis^[1]

Cell Line:	MV4-11 leukemia cells
Concentration:	10 , 50, 100, 500 nM
Incubation Time:	18 hours
Result:	Performed depletion selectivity for BRD4 and BRD2 over BRD3, with good selectivity intra-BET proteins selectivity.

分子量

766.82

Formula

C₃₉H₃₈N₆O₉S

CAS 号

2570470-42-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

参考文献

[1]. Jiang F, et al. Discovery of novel small molecule induced selective degradation of the bromodomain and extra-terminal (BET) bromodomain protein BRD4 and BRD2 with cellular potencies. Bioorg Med Chem. 2019 Nov 11:115181.

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PROTAC BRD4 Degrader-10

发表于2026年1月5日由上海金畔生物科技有限公司

PROTAC BRD4 Degrader-10

PROTAC BRD4 Degrader-10 (compound 8b) 是一种有效的由von Hippel-Lindau配体和BRD4配体相连的PROTAC 。PROTAC BRD4 Degrader-10 可与 STEAP1 和 CLL1 抗体偶联从而降解 PC3 前列腺癌细胞中的 BRD4 蛋白，DC₅₀ 值分别为 1.3 nM 和 18 nM。

PROTAC BRD4 Degrader-10 Chemical Structure

CAS No. : 2417370-49-9

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生物活性	PROTAC BRD4 Degrader-10 (compound 8b) is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. PROTAC BRD4 Degrader-10 can be conjugated with STEAP1 and CLL1 antibodies to degrade the BRD4 protein in PC3 prostate cancer cells, with a DC₅₀ of 1.3 nM and 18 nM, respectively^[1].
分子量	1312.50
Formula	C₅₉H₇₁F₂N₉O₁₅S₄
CAS 号	2417370-49-9
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献	[1]. Dragovich PS, et, al. Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 2: Improvement of In Vitro Antiproliferation Activity and In Vivo Antitumor Efficacy. J Med Chem. 2021 Mar 11;64(5):2576-2607.

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PROTAC BRD4 Degrader-13

发表于2026年1月5日由上海金畔生物科技有限公司

PROTAC BRD4 Degrader-13

PROTAC BRD4 Degrader-13 (compound 9d) 是由von Hippel-Lindau配体和BRD4配体相连的PROTAC。PROTAC BRD4 Degrader-13 可与 STEAP1 和 CLL1 抗体偶联从而降解 PC3 前列腺癌细胞中的 BRD4 蛋白，DC₅₀ 值分别为 0.025 nM 和 6.0 nM。

PROTAC BRD4 Degrader-13 Chemical Structure

CAS No. : 2417370-71-7

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生物活性	PROTAC BRD4 Degrader-13 (compound 9d) is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. PROTAC BRD4 Degrader-13 can be conjugated with STEAP1 and CLL1 antibodies to degrade the BRD4 protein in PC3 prostate cancer cells, with a DC₅₀ of 0.025 nM and 6.0 nM, respectively^[1].
分子量	1492.54
Formula	C₆₈H₈₅F₂N₁₁O₁₇P₂S₂
CAS 号	2417370-71-7
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献	[1]. Dragovich PS, et, al. Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 2: Improvement of In Vitro Antiproliferation Activity and In Vivo Antitumor Efficacy. J Med Chem. 2021 Mar 11;64(5):2576-2607.

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PROTAC BRD4 Degrader-11

发表于2026年1月5日由上海金畔生物科技有限公司

PROTAC BRD4 Degrader-11

PROTAC BRD4 Degrader-11 (compound 9a) 是一种有效的由von Hippel-Lindau配体和BRD4配体相连的PROTAC。PROTAC BRD4 Degrader-11 可与 STEAP1 和 CLL1 抗体偶联从而降解 PC3 前列腺癌细胞中的 BRD4 蛋白，DC₅₀ 值分别为 0.23 nM 和 0.38 nM。

PROTAC BRD4 Degrader-11 Chemical Structure

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生物活性	PROTAC BRD4 Degrader-11 (compound 9a) is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. PROTAC BRD4 Degrader-11 can be conjugated with STEAP1 and CLL1 antibodies to degrade the BRD4 protein in PC3 prostate cancer cells, with a DC₅₀ of 0.23 nM and 0.38 nM, respectively^[1].
分子量	1292.56
Formula	C₆₁H₇₅F₂N₉O₁₂S₄
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献	[1]. Dragovich PS, et, al. Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 2: Improvement of In Vitro Antiproliferation Activity and In Vivo Antitumor Efficacy. J Med Chem. 2021 Mar 11;64(5):2576-2607.

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PROTAC BRD4 Degrader-12

发表于2026年1月5日由上海金畔生物科技有限公司

PROTAC BRD4 Degrader-12

PROTAC BRD4 Degrader-12 (compound 9c) 是一种由von Hippel-Lindau配体和BRD4配体相连的PROTAC。PROTAC BRD4 Degrader-12 可与 STEAP1 和 CLL1 抗体偶联从而降解 PC3 前列腺癌细胞中的 BRD4 蛋白，DC₅₀ 值分别为 0.39 nM 和 0.24 nM。

PROTAC BRD4 Degrader-12 Chemical Structure

CAS No. : 2417370-90-0

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生物活性	PROTAC BRD4 Degrader-12 (compound 9c) is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. PROTAC BRD4 Degrader-12 can be conjugated with STEAP1 and CLL1 antibodies to degrade the BRD4 protein in PC3 prostate cancer cells, with a DC₅₀ of 0.39 nM and 0.24 nM, respectively^[1].
分子量	1306.58
Formula	C₆₂H₇₇F₂N₉O₁₂S₄
CAS 号	2417370-90-0
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献	[1]. Dragovich PS, et, al. Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 2: Improvement of In Vitro Antiproliferation Activity and In Vivo Antitumor Efficacy. J Med Chem. 2021 Mar 11;64(5):2576-2607.

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PROTAC BRD4 Degrader-14

发表于2026年1月5日由上海金畔生物科技有限公司

PROTAC BRD4 Degrader-14

PROTAC BRD4 Degrader-14 是一种由von Hippel-Lindau配体和BRD4配体相连的PROTAC，对 BRD4 BD1 和 BD2 的 IC₅₀ 值分别为 1.8 nM 和 1.7 nM。PROTAC BRD4 Degrader-14 能够有效降解 PC3 前列腺癌细胞中的 BRD4 蛋白。

PROTAC BRD4 Degrader-14 Chemical Structure

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生物活性	PROTAC BRD4 Degrader-14 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4, with IC₅₀s of 1.8 nM and 1.7 nM for BRD4 BD1 and BD2, respectively. PROTAC BRD4 Degrader-14 is capable of potently degrading the BRD4 protein in PC3 prostate cancer cells^[1].
分子量	1150.27
Formula	C₅₇H₆₁F₂N₉O₁₁S₂
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献	[1]. Dragovich PS, et, al. Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 2: Improvement of In Vitro Antiproliferation Activity and In Vivo Antitumor Efficacy. J Med Chem. 2021 Mar 11;64(5):2576-2607.

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PROTAC CDK2/9 Degrader-1

发表于2026年1月4日由上海金畔生物科技有限公司

PROTAC CDK2/9 Degrader-1 纯度: 99.85%

PROTAC CDK2/9 Degrader-1 (Compound F3) 是 CDK2 (DC₅₀=62 nM) 和 CDK9 (DC₅₀=33 nM) 的有效双降解剂。PROTAC CDK2/9 Degrader-1 通过有效阻断前列腺癌 PC-3 细胞S期和 G2/M 期的细胞周期，抑制前列腺癌 PC-3 细胞增殖 (IC₅₀=0.12 µM)。PROTAC CDK2/9 Degrader-1 是一种 CDK 抑制剂与 Cereblon 配体结合的 PROTAC。

PROTAC CDK2/9 Degrader-1 Chemical Structure

CAS No. : 2408641-24-5

规格	价格	是否有货
5 mg	￥7500	In-stock
10 mg	￥12500	In-stock
25 mg	￥24500	In-stock
50 mg	￥37500	In-stock
100 mg		询价
200 mg		询价

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PROTAC CDK2/9 Degrader-1 相关产品

•相关化合物库:

Bioactive Compound Library Plus

生物活性

PROTAC CDK2/9 Degrader-1 (Compound F3) is a potent dual degrader for CDK2 (DC₅₀=62 nM) and CDK9 (DC₅₀=33 nM). PROTAC CDK2/9 Degrader-1 suppresses prostate cancer PC-3 cell proliferation (IC₅₀=0.12 µM) by effectively blocking the cell cycle in S and G2/M phases. PROTAC CDK2/9 Degrader-1 is a PROTAC by tethering CDK inhibitor with Cereblon ligand^[1].

IC₅₀ & Target^[1]

CDK2

62 nM (DC₅₀)

CDK9

33 nM (DC₅₀)

Cereblon

体外研究
(In Vitro)

PROTAC CDK2/9 Degrader-1 (0.25-3 μM; 48 hours) induces cell cycle blockage at the G2/M phase^[1].
PROTAC CDK2/9 Degrader-1 (500 nM; 2-24 hours) down-regulates the Mcl-1 protein level in PC-3 cells^[1].
PROTAC CDK2/9 Degrader-1 effectively degrades CDK2/9 in cell lines MCF-7, HCT-116 and 22Rv1, which all have high CDK2/9 expression^[1].
PROTAC CDK2/9 Degrader-1 inhibits both CDK2 and CDK9, with IC₅₀ as 7.42 nM and 14.50 nM, respectively^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis^[1]

Cell Line:	PC-3 cells
Concentration:	500 nM
Incubation Time:	2, 4, 8, 16, 24 hours
Result:	Down-regulated the Mcl-1 protein level in PC-3 cells.

Western Blot Analysis^[1]

Cell Line:	PC-3 cells
Concentration:	0.25, 1, 3 μM
Incubation Time:	48 hours
Result:	Induced cell cycle blockage at the G2/M phase.

分子量

815.84

Formula

C₄₀H₄₁N₁₃O₇

CAS 号

2408641-24-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

溶解性数据

In Vitro:

DMSO : 55 mg/mL (67.42 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.2257 mL	6.1287 mL	12.2573 mL
5 mM	0.2451 mL	1.2257 mL	2.4515 mL
10 mM	0.1226 mL	0.6129 mL	1.2257 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: 5 mg/mL (6.13 mM); Suspended solution; Need ultrasonic

此方案可获得 5 mg/mL (6.13 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

以 1 mL 工作液为例，取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Zhou F, et al. Development of selective mono or dual PROTAC degrader probe of CDK isoforms. Eur J Med Chem. 2019 Dec 6;187:111952.

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PROTAC B-Raf degrader 1

发表于2026年1月4日由上海金畔生物科技有限公司

PROTAC B-Raf degrader 1 纯度: 99.18%

PROTAC B-Raf degrader 1 (compound 2) 是基于 Cereblon 配体的一种 B-Raf PROTAC。有抗肿瘤活性。

PROTAC B-Raf degrader 1 Chemical Structure

CAS No. : 2364367-27-9

规格	价格	是否有货
5 mg	￥5800	In-stock
10 mg	￥9800	In-stock
50 mg		询价
100 mg		询价

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PROTAC B-Raf degrader 1 相关产品

•相关化合物库:

Bioactive Compound Library Plus

生物活性

PROTAC B-Raf degrader 1 (compound 2) is a proteolysis targeting chimera (PROTAC) for the degradation of B-Raf based on Cereblon ligand with anti-cancer activity^[1].

IC₅₀ & Target^[1]

B-Raf

体外研究
(In Vitro)

The IC₅₀ values of PROTAC B-Raf degrader 1 (compound 2) towards MCF-7, MDA-MB-231, HepG2, LO2 and B16 cells are 2.7 μM, 21.21 μM, 18.70 μM, 41.11μM and 22.68 μM, respectively^[1].
PROTAC B-Raf degrader 1 (5 or 10 μM) can accelerate the degradation of B-Raf by recruiting ubiquitin-proteasome system, and further affects the expression of Mcl-1, a downstream protein of B-Raf^[1].
MCF-7 cells achieve an apoptosis rate of 76.70% (64.00% early apoptosis, 12.70% late apoptosis) after 24 h incubation of PROTAC B-Raf degrader 1 with the concentration of 20 μM^[1].
PROTAC B-Raf degrader 1 arrests cell cycle at the G2/M phase^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cytotoxicity Assay^[1]

Cell Line:	Human MCF-7 breast cancer cell line, MDA-MB-231 breast cancer cells, human HepG2 hepatoma cells, human normal LO2 liver cells, B16 cells.
Concentration:	0-200 μM.
Incubation Time:	72 hours.
Result:	The IC₅₀ values are 2.7 μM, 21.21 μM, 18.70 μM, 41.11μM and 22.68 μM in MCF-7, MDA-MB-231, HepG2, LO2 and B16 cells, respectively.

Western Blot Analysis^[1]

Cell Line:	Human MCF-7 breast cancer cell line.
Concentration:	5 or 10 μM.
Incubation Time:	24 hours.
Result:	Effectively induced the degradation of B-Raf and impacted the expression of Mcl-1.

Apoptosis Analysis^[1]

Cell Line:	Human MCF-7 breast cancer cell line.
Concentration:	2.7-20 μM.
Incubation Time:	24 hours.
Result:	Achieved an apoptosis rate of 76.70% (64.00% early apoptosis, 12.70% late apoptosis) after 24 h incubation with the concentration of 20 μM.

Cell Cycle Analysis^[1]

Cell Line:	Human MCF-7 breast cancer cell line.
Concentration:	20 μM.
Incubation Time:	24 hours.
Result:	1.94% cells were arrested at G1 phase, 8.20% at S phase, and 89.86% at G2/M phase.

分子量

763.77

Formula

C₃₆H₃₇N₅O₁₂S

CAS 号

2364367-27-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, stored under nitrogen

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

溶解性数据

In Vitro:

DMSO : 25 mg/mL (32.73 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.3093 mL	6.5465 mL	13.0929 mL
5 mM	0.2619 mL	1.3093 mL	2.6186 mL
10 mM	0.1309 mL	0.6546 mL	1.3093 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.5 mg/mL (3.27 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (3.27 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.5 mg/mL (3.27 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (3.27 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Chen H, et al. Pomalidomide hybrids act as proteolysis targeting chimeras: Synthesis, anticancer activity and B-Raf degradation. Bioorg Chem. 2019 Mar 19;87:191-199.

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Dual PARP EGFR ligand for PROTAC

发表于2026年1月1日由上海金畔生物科技有限公司

Dual PARP EGFR ligand for PROTAC

Dual PARP EGFR ligand for PROTAC 含靶蛋白 PARP 和 EGFR 的配体，以及募集 E3 连接酶（如 VHL、CRBN、MDM2 和 IAP）的 PROTAC linker。Dual PARP EGFR ligand for PROTAC 可用于合成 PROTAC DP-C-4，DP-C-4 是一种基于 CRBN 的双 PROTAC，用于同时降解 EGFR 和 PARP。

Dual PARP EGFR ligand for PROTAC Chemical Structure

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生物活性	Dual PARP EGFR ligand for PROTAC incorporates a ligand for PARP and EGFR , and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). Dual PARP EGFR ligand for PROTAC can be used in the synthesis of DP-C-4, which is CRBN-based dual PROTAC for simultaneous degradation of EGFR and PARP^[1].
分子量	1020.52
Formula	C₅₃H₅₆ClF₂N₉O₈
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献	[1]. Mengzhu Zheng, et al. Rational Design and Synthesis of Novel Dual PROTACs for Simultaneous Degradation of EGFR and PARP. J Med Chem. 2021 May 26.

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PROTAC Bcl-xL degrader-2

发表于2025年12月29日由上海金畔生物科技有限公司

PROTAC Bcl-xL degrader-2

PROTAC Bcl-xL degrader-2 是一种基于 von Hippel-Lindau 配体的 Bcl-xL (Bcl-2 家族成员) 降解剂，IC₅₀ 为 0.6 nM。

PROTAC Bcl-xL degrader-2 Chemical Structure

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生物活性

PROTAC Bcl-xL degrader-2 is a potent Bcl-xL (Bcl-2 family member) degrader based on von Hippel-Lindau ligand, with an IC₅₀ of 0.6 nM.

IC₅₀ & Target^[1]

Bcl-xL

0.6 nM (IC₅₀)

VHL

体外研究
(In Vitro)

PROTAC Bcl-xL degrader-2 (PROTAC 6; 0.1 nM-10 μM; 24 hours) treatment decreases the level of Bcl-xL protein in THP-1 cells^[1].
PROTAC Bcl-xL degrader-2 (PROTAC 6) inhibits caspase 3/7 activity in MOLT-4 cells with an IC₅₀ of 466 nM^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:	THP-1 cells
Concentration:	0.1 nM-10 μM
Incubation Time:	24 hours
Result:	Led to monotonic decreases in observed Bcl-xL protein.

分子量

1329.60

Formula

C₆₈H₈₀N₈O₁₄S₃

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

参考文献

[1]. Chun-Wa Chung, et al. Structural Insights into PROTAC-Mediated Degradation of Bcl-xL. ACS Chem Biol. 2020 Sep 18;15(9):2316-2323.

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Homo-PROTAC pVHL30 degrader 1

发表于2025年12月18日由上海金畔生物科技有限公司

Homo-PROTAC pVHL30 degrader 1 纯度: 99.83%

Homo-PROTAC pVHL30 degrader 1 是基于 PROTAC 的有效 pVHL30 降解剂。

Homo-PROTAC pVHL30 degrader 1 Chemical Structure

CAS No. : 2244684-49-7

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5 mg	￥3800	In-stock
10 mg	￥6400	In-stock
25 mg	￥12000	In-stock
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Homo-PROTAC pVHL30 degrader 1 相关产品

•相关化合物库:

Bioactive Compound Library Plus

生物活性

Homo-PROTAC pVHL30 degrader 1 is a potent pVHL30 degrader based on PROTAC^[1], consists of two ligands of von Hippel-Lindau.

IC₅₀ & Target

VHL

体外研究
(In Vitro)

Homo-PROTAC pVHL30 degrader 1 dimerizes von Hippel-Lindau (VHL) with high avidity in vitro and induces potent, rapid and proteasome-dependent self-degradation of VHL in different cell lines, in a highly isoform-selective fashion and without triggering a hypoxic response^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

1179.45

Formula

C₅₈H₈₂N₈O₁₄S₂

CAS 号

2244684-49-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, stored under nitrogen

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

溶解性数据

In Vitro:

DMSO : ≥ 150 mg/mL (127.18 mM)

* “≥” means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	0.8479 mL	4.2393 mL	8.4785 mL
5 mM	0.1696 mL	0.8479 mL	1.6957 mL
10 mM	0.0848 mL	0.4239 mL	0.8479 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.5 mg/mL (2.12 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (2.12 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (2.12 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (2.12 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.5 mg/mL (2.12 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (2.12 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Maniaci C, et al. Homo-PROTACs: bivalent small-molecule dimerizers of the VHL E3 ubiquitin ligase to induce self-degradation. Nat Commun. 2017 Oct 10;8(1):830.

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NH2-PEG3(Synonyms: PROTAC Linker 35)

发表于2025年12月12日由上海金畔生物科技有限公司

NH2-PEG3 (Synonyms: PROTAC Linker 35) 纯度: ≥98.0%

NH2-PEG3 (PROTAC Linker 35) 属于聚乙二醇 (PEG) 的 PROTAC linker。NH2-PEG3 (PROTAC Linker 35) 可用于合成 PROTAC (β-NF-JQ1)。

NH2-PEG3 Chemical Structure

CAS No. : 6338-55-2

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生物活性

NH2-PEG3 (PROTAC Linker 35) is a PROTAC linker, which belongs to a polyethylene glycol (PEG) linker. NH2-PEG3 (PROTAC Linker 35) can be used in the synthesis of the PROTAC (β-NF-JQ1)^[1].

IC₅₀ & Target

PEGs

分子量

149.19

Formula

C₆H₁₅NO₃

CAS 号

6338-55-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

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

溶解性数据

In Vitro:

DMSO : 100 mg/mL (670.29 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	6.7029 mL	33.5143 mL	67.0286 mL
5 mM	1.3406 mL	6.7029 mL	13.4057 mL
10 mM	0.6703 mL	3.3514 mL	6.7029 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.5 mg/mL (16.76 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (16.76 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
2.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.08 mg/mL (13.94 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (13.94 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
3.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.08 mg/mL (13.94 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (13.94 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Ohoka N,et al. Development of Small Molecule Chimeras That Recruit AhR E3 Ligase to Target Proteins. ACS Chem Biol. 2019 Oct 16.

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Methyltetrazine-acid

发表于2025年12月12日由上海金畔生物科技有限公司

Methyltetrazine-acid 纯度: 99.46%

Methyltetrazine-acid 是一种 PROTAC linker，属于 alkyl chain 类。可用于合成 PROTAC 分子。

Methyltetrazine-acid Chemical Structure

CAS No. : 1380500-88-8

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25 mg	￥2500	In-stock
100 mg	￥5000	In-stock
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生物活性

Methyltetrazine-acid is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs^[1].

IC₅₀ & Target

Alkyl-Chain

体外研究
(In Vitro)

PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

230.22

Formula

C₁₁H₁₀N₄O₂

CAS 号

1380500-88-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

溶解性数据

In Vitro:

DMSO : 100 mg/mL (434.37 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	4.3437 mL	21.7184 mL	43.4367 mL
5 mM	0.8687 mL	4.3437 mL	8.6873 mL
10 mM	0.4344 mL	2.1718 mL	4.3437 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.5 mg/mL (10.86 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (10.86 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (10.86 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (10.86 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. An S, et al. Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs. EBioMedicine. 2018 Oct;36:553-562

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PROTAC Bcl-xL degrader-3

发表于2025年12月12日由上海金畔生物科技有限公司

PROTAC Bcl-xL degrader-3

PROTAC Bcl-xL degrader-3 是一种有效的 PROTAC Bcl-xL 降解剂 (详细信息请参考 WO2020163823A2, compound 2)。

PROTAC Bcl-xL degrader-3 Chemical Structure

CAS No. : 2471970-60-0

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生物活性

PROTAC Bcl-xL degrader-3 is a potent ROTAC Bcl-xL degrader (WO2020163823A2, compound 44)^[1].

IC₅₀ & Target^[1]

Bcl-xL

VHL

分子量

1641.49

Formula

C₈₂H₁₀₅ClF₃N₁₁O₁₁S₄

CAS 号

2471970-60-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

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PROTAC BRD9 Degrader-4

发表于2025年12月12日由上海金畔生物科技有限公司

PROTAC BRD9 Degrader-4

PROTAC BRD9 Degrader-4是治疗癌症的BRD9双功能降解剂。

PROTAC BRD9 Degrader-4 Chemical Structure

CAS No. : 2633632-34-3

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生物活性	PROTAC BRD9 Degrader-4 is a BRD9 bifunctional degrader for treating cancer.
分子量	768.87
Formula	C₄₂H₄₉FN₆O₇
CAS 号	2633632-34-3
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献	[1]. Sabnis RW, et al. BRD9 Bifunctional Degraders for Treating Cancer. ACS Med. Chem. Lett. 2021 Nov 6.

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PROTAC ER Degrader-10

发表于2025年12月12日由上海金畔生物科技有限公司

PROTAC ER Degrader-10

PROTAC ER Degrader-10 是一种有效的 PROTAC ER 降解剂，可用于癌症研究。PROTAC ER Degrader-10 源自专利 WO2021133886，例 36。

PROTAC ER Degrader-10 Chemical Structure

CAS No. : 2504911-58-2

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500 mg		询价

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生物活性	PROTAC ER Degrader-10 is a potent PROTAC ER degrader and can be used for cancer research. PROTAC ER Degrader-10 is extracted from patent WO2021133886, example 36.
分子量	739.86
Formula	C₄₄H₄₅N₅O₆
CAS 号	2504911-58-2
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献	[1]. Jie Fan, et al. Combinations of estrogen receptor degraders and cyclin-dependent kinase inhibitors for treating cancer. Patent WO2021133886.

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PROTAC BRD9 Degrader-5

发表于2025年11月23日由上海金畔生物科技有限公司

PROTAC BRD9 Degrader-5

PROTAC BRD9 Degrader-5 是一种针对 BRD9 的靶向降解 PROTAC。

PROTAC BRD9 Degrader-5 Chemical Structure

CAS No. : 2704616-86-2

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生物活性	PROTAC BRD9 Degrader-5 is a PROTAC for targeted degradation of BRD9.
分子量	751.24
Formula	C₃₉H₄₂ClF₃N₆O₄
CAS 号	2704616-86-2
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献	[1]. Christopher G. Nasveschuk, et al. Compounds for targeted degradation of brd9. WO2021178920 A1.

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Bis-PEG5-acid(Synonyms: PROTAC Linker 36)

发表于2025年11月21日由上海金畔生物科技有限公司

Bis-PEG5-acid (Synonyms: PROTAC Linker 36)

Bis-PEG5-acid (PROTAC Linker 36) 属于聚乙二醇 (PEG) 的 PROTAC linker。Bis-PEG5-acid (PROTAC Linker 36) 可用于合成 CP5V。CP5V 是一种 PROTAC，专门降解 Cdc20。

Bis-PEG5-acid Chemical Structure

CAS No. : 439114-13-3

规格	价格	是否有货
250 mg	￥1000	In-stock
500 mg	￥1500	In-stock
1 g	￥2400	In-stock
5 g	￥7000	In-stock
10 g		询价
50 g		询价

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生物活性

Bis-PEG5-acid (PROTAC Linker 36) is a PROTAC linker, which belongs to a polyethylene glycol (PEG) linker. Bis-PEG5-acid (PROTAC Linker 36) can be used in the synthesis of the CP5V. CP5V is a PROTAC, and specifically degrades Cdc20^[1].

IC₅₀ & Target

PEGs

分子量

338.35

Formula

C₁₄H₂₆O₉

CAS 号

439114-13-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, stored under nitrogen

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

参考文献

[1]. Chi JJ, et al. A novel strategy to block mitotic progression for targeted therapy. EBioMedicine. 2019 Oct 25. pii: S2352-3964(19)30677-2.

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PROTAC CDK9 degrader-2

发表于2025年11月20日由上海金畔生物科技有限公司

PROTAC CDK9 degrader-2

PROTAC CDK9 degrader-2 是一种基于 PROTAC 技术，高效选择性的 CDK9 降解剂，在 MCF-7 细胞系中抑制 CDK9 的 IC₅₀ 值为 17 μM。PROTAC 由天然产物汉黄芩素 (Wogonin，CDK配体) 与Cereblon泛素 E3 连接酶 (CRBN) 通过 linker 连接而成。

PROTAC CDK9 degrader-2 Chemical Structure

CAS No. : 2435721-30-3

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生物活性

PROTAC CDK9 degrader-2 (compounds 11c) is a potent and selective CDK9 degrader based on PROTAC, with an IC₅₀ of 17 μM in MCF-7 cell lines. Natural product Wogonin (CDK ligand) binds ubiquitin E3 ligase Cereblon (CRBN) via a linker to form PROTAC^[1].

IC₅₀ & Target^[1]

CDK9

17 μM (IC₅₀, MCF-7 cells)

分子量

748.74

Formula

C₃₉H₃₆N₆O₁₀

CAS 号

2435721-30-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

参考文献

[1]. Bian J , et al. Discovery of Wogonin-based PROTACs against CDK9 and capable of achieving antitumor activity. Bioorg Chem. 2018 Dec;81:373-381.

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PROTAC BRD4-binding moiety 1

发表于2025年11月20日由上海金畔生物科技有限公司

PROTAC BRD4-binding moiety 1

PROTAC BRD4-binding moiety 1 是 BRD4 的配体。PROTAC BRD4-binding moiety 1 通过 linker 结合到 cereblon 配体上形成 PROTAC 以降解 BRD4 (HY-133136)。

PROTAC BRD4-binding moiety 1 Chemical Structure

CAS No. : 2101200-10-4

规格		是否有货
100 mg		询价
250 mg		询价
500 mg		询价

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生物活性

PROTAC BRD4-binding moiety 1 is a ligand for BRD4. PROTAC BRD4-binding moiety 1 binds to cereblon ligand via a linker to form PROTAC to degrade BRD4 (HY-133136)^[1].

IC₅₀ & Target

BRD4

体外研究
(In Vitro)

PROTAC BRD4 Degrader-2 is an efficacious PROTAC BRD4 degrader with an IC₅₀ of 14.2 nM against BRD4 BD1^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

371.43

Formula

C₂₃H₂₁N₃O₂

CAS 号

2101200-10-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

参考文献

[1]. Zhang F, et al. Discovery of a new class of PROTAC BRD4 degraders based on a dihydroquinazolinone derivative and lenalidomide/pomalidomide. Bioorg Med Chem. 2020 Jan 1;28(1):115228.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

whatman (沃特曼)

英国沃特曼 Millipore PALL中国代理商金畔官网

标签归档：protac

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