生物活性分子抑制剂UNC6852

发表于2024年4月6日由上海金畔生物科技有限公司

生物活性分子抑制剂特异性抑制剂激动剂化合物库重组蛋白 UNC6852 纯度: 98.68%

UNC6852是一种基于 PROTAC 技术的，选择性的 PRC2 降解剂，包含了一个 EED 配体和一个 von Hippel-Lindau 配体，对 EED 作用的 IC₅₀ 值为 247 nM。

UNC6852 Chemical Structure

CAS No. : 2688842-08-0

规格	价格	是否有货
5 mg	￥3000	询价
10 mg	￥5200	In-stock
25 mg	￥9800	In-stock
50 mg	￥15000	In-stock
100 mg		询价
200 mg		询价

* Please select Quantity before adding items.

UNC6852 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Epigenetics Compound Library
Histone Modification Research Compound Library
Anti-Cancer Compound Library
Reprogramming Compound Library
Anti-Blood Cancer Compound Library

生物活性

UNC6852 is a selective polycomb repressive complex 2 (PRC2) degrader based on PROTAC and contains an EED (embryonic ectoderm development) ligand and a von Hippel-Lindau ligand, with an IC₅₀ of 247 nM for EED^[1].

IC₅₀ & Target

IC50: 247 nM (EED)^[1]

体外研究
(In Vitro)

UNC6852 mediates PRC2 degradation^[1].
UNC6852 displays no cellular toxicity at concentrations up to 30 μM for HeLa Cells^[1].
UNC6852 (10 μM; 1-72 hours) results in a decrease in the levels of both EED and EZH2^[1].
UNC6852 facilitates PRC2 degradation via VHL recruitment^[1].
UNC6852 selectively degrades EED and EZH2^[1].
UNC6852 reduces H3K27me3 levels and DLBCL cell proliferation^[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 Proliferation Assay^[1]

Cell Line:	DLBCL Cells
Concentration:	3 μM
Incubation Time:	0 -10 days
Result:	Exhibited anti-proliferative effects.

Western Blot Analysis^[1]

Cell Line:	HeLa Cells
Concentration:	10 μM
Incubation Time:	1 hours, 4 hours, 8 hours, 10 hours, 16 hours, 20 hours, 24 hours, 48 hours, 72 hours
Result:	Resulted in a decrease in the levels of both EED and EZH2.

分子量

832.97

Formula

C₄₃H₄₈N₁₀O₆S

CAS 号

2688842-08-0

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 (120.05 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.2005 mL	6.0026 mL	12.0052 mL
5 mM	0.2401 mL	1.2005 mL	2.4010 mL
10 mM	0.1201 mL	0.6003 mL	1.2005 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 (6.00 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (6.00 mM，饱和度未知) 的澄清溶液。

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
2.

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

Solubility: ≥ 5 mg/mL (6.00 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (6.00 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 50.0 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: ≥ 5 mg/mL (6.00 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (6.00 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 50.0 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]. Potjewyd F, et al. Degradation of Polycomb Repressive Complex 2 with an EED-Targeted Bivalent Chemical Degrader. Cell Chem Biol. 2020 Jan 16;27(1):47-56.e15.

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

UNC0646

发表于2024年3月20日由上海金畔生物科技有限公司

UNC0646 纯度: 99.82%

UNC0646 是一种有效的选择性组蛋白甲基转移酶 G9a 抑制剂，其 IC₅₀ 为 6 nM。UNC0646 还是一种有效的 GLP 抑制剂 (IC₅₀ <15 nm)，对 G9a/GLP 的选择性比 SETD7，SUV39H2，SETD8 和 PRMT3 高。UNC0646 降低 MDA-MB-231 细胞中 H3K9me2 的水平，IC₅₀ 为 26 nM。

UNC0646 Chemical Structure

CAS No. : 1320288-17-2

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥1018	In-stock
5 mg	￥744	In-stock
10 mg	￥1050	In-stock
50 mg	￥3510	In-stock
100 mg		询价
200 mg		询价

* Please select Quantity before adding items.

UNC0646 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Epigenetics Compound Library
Histone Modification Research Compound Library
Anti-Cancer Compound Library
Reprogramming Compound Library
Anti-Blood Cancer Compound Library
Transcription Factor Targeted Library
Targeted Diversity Library

生物活性

UNC0646 is a potent and selective histone methyltransferase G9a inhibitor with an IC₅₀ of 6 nM. UNC0646 is also a potent GLP inhibitor (IC₅₀ <15 nm) and highly selective for G9a/GLP over SETD7, SUV39H2, SETD8 and PRMT3. UNC0646 reduces H3K9me2 levels in MDA-MB-231 cells with an IC₅₀ of 26 nM^[1].

IC₅₀ & Target

G9a

6 nM (IC₅₀)

GLP

<15 nM (IC₅₀)

体外研究
(In Vitro)

UNC0646 (Compound 6) has high cellular potency and excellent separation of functional potency versus cell toxicity in a variety of cell lines. UNC0646 is highly potent in reducing H3K9me2 levels and has low cell toxicity. UNC0646 reduces H3K9me2 levels with ICW IC₅₀ values of 26 nM, 10 nM, 12 nM, 14 nM, 68 nM, 86 nM and 10 nM in MDA-MB-231, MCF7, PC3, 22RV1, HCT116 wt, HCT 116 p53^-/- and IMR90 cell lines, respectively^[1].

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

分子量

621.90

Formula

C₃₆H₅₉N₇O₂

CAS 号

1320288-17-2

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 : 50 mg/mL (80.40 mM; ultrasonic and warming and adjust pH to 3 with HCl and heat to 80°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.6080 mL	8.0399 mL	16.0798 mL
5 mM	0.3216 mL	1.6080 mL	3.2160 mL
10 mM	0.1608 mL	0.8040 mL	1.6080 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: ≥ 4.55 mg/mL (7.32 mM); Clear solution

此方案可获得 ≥ 4.55 mg/mL (7.32 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 45.5 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 (4.02 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.02 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 (4.02 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.02 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 MCE 网站选购。

参考文献

[1]. Liu F, et al. Optimization of cellular activity of G9a inhibitors 7-aminoalkoxy-quinazolines. J Med Chem. 2011 Sep 8;54(17):6139-50.

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

UNC0646

发表于2024年3月20日由上海金畔生物科技有限公司

UNC0646 纯度: 99.82%

UNC0646 Chemical Structure

CAS No. : 1320288-17-2

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥1018	In-stock
5 mg	￥744	In-stock
10 mg	￥1050	In-stock
50 mg	￥3510	In-stock
100 mg		询价
200 mg		询价

* Please select Quantity before adding items.

UNC0646 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Epigenetics Compound Library
Histone Modification Research Compound Library
Anti-Cancer Compound Library
Reprogramming Compound Library
Anti-Blood Cancer Compound Library
Transcription Factor Targeted Library
Targeted Diversity Library

生物活性

IC₅₀ & Target

G9a

6 nM (IC₅₀)

GLP

<15 nM (IC₅₀)

体外研究
(In Vitro)

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

分子量

621.90

Formula

C₃₆H₅₉N₇O₂

CAS 号

1320288-17-2

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 : 50 mg/mL (80.40 mM; ultrasonic and warming and adjust pH to 3 with HCl and heat to 80°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.6080 mL	8.0399 mL	16.0798 mL
5 mM	0.3216 mL	1.6080 mL	3.2160 mL
10 mM	0.1608 mL	0.8040 mL	1.6080 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: ≥ 4.55 mg/mL (7.32 mM); Clear solution

此方案可获得 ≥ 4.55 mg/mL (7.32 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 45.5 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 (4.02 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.02 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 (4.02 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.02 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 MCE 网站选购。

参考文献

[1]. Liu F, et al. Optimization of cellular activity of G9a inhibitors 7-aminoalkoxy-quinazolines. J Med Chem. 2011 Sep 8;54(17):6139-50.

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

UNC1215

发表于2024年3月19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。

UNC1215 纯度: 98.47%

UNC1215 是选择性 L3MBTL3 甲基赖氨酸结构域的拮抗剂，IC₅₀ 为40 nM，K_d 为 120 nM。UNC1215 可用于恶性脑瘤的研究。

UNC1215 Chemical Structure

CAS No. : 1415800-43-9

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥867	In-stock
5 mg	￥744	In-stock
10 mg	￥1302	In-stock
50 mg	￥4780	In-stock
100 mg		询价
200 mg		询价

* Please select Quantity before adding items.

UNC1215 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Apoptosis Compound Library
Epigenetics Compound Library
Histone Modification Research Compound Library
Anti-Cancer Compound Library
Chemical Probe Library
Anti-Blood Cancer Compound Library
Targeted Diversity Library

生物活性

UNC1215 is a potent and selective inhibitor for the methyllysine (Kme) reading domain function of L3MBTL3 with a K_d value of 120 nM and an IC₅₀ of 40 nM. UNC1215 has the potential to treat malignant brain tumor.

IC₅₀ & Target

IC50: 40 nM (L3MBTL3).
Kd: 120 nM (L3MBTL3).

体外研究
(In Vitro)

UNC1215 binds L3MBTL3 with a _d of 120 nM, competitively displacing mono- or dimethyllysine-containing peptides, and is greater than 50-fold more potent toward L3MBTL3 than other members of the MBT family while also demonstrating selectivity against more than 200 other reader domains examined. X-ray crystallography identified a unique 2:2 polyvalent mode of interaction between UNC1215 and L3MBTL3. In cells, UNC1215 is nontoxic and directly binds L3MBTL3 via the Kme-binding pocket of the MBT domains. UNC1215 increases the cellular mobility of GFP-L3MBTL3 fusion proteins, and point mutants that disrupt the Kme-binding function of GFP-L3MBTL3 phenocopy the effects of UNC1215 on localization^[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

529.72

Formula

C₃₂H₄₃N₅O₂

CAS 号

1415800-43-9

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 : ≥ 270 mg/mL (509.70 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	1.8878 mL	9.4389 mL	18.8779 mL
5 mM	0.3776 mL	1.8878 mL	3.7756 mL
10 mM	0.1888 mL	0.9439 mL	1.8878 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: ≥ 0.83 mg/mL (1.57 mM); Clear solution

此方案可获得 ≥ 0.83 mg/mL (1.57 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 8.3 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: ≥ 0.83 mg/mL (1.57 mM); Clear solution

此方案可获得 ≥ 0.83 mg/mL (1.57 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 8.3 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: ≥ 0.83 mg/mL (1.57 mM); Clear solution

此方案可获得 ≥ 0.83 mg/mL (1.57 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 8.3 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]. James LI, Barsyte-Lovejoy D, Zhong N, et al. Discovery of a chemical probe for the L3MBTL3 methyllysine reader domain. Nat Chem Biol. 2013 Mar;9(3):184-91. doi: 10.1038/nchembio.1157.

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

UNC2025 hydrochloride

发表于2024年3月15日由上海金畔生物科技有限公司

UNC2025 hydrochloride 纯度: 99.41%

UNC2025 hydrochloride 是一种强效、ATP 竞争性，高口服活性的 Mer/Flt3 抑制剂，IC₅₀ 值分别为 0.74 nM 和 0.8 nM。UNC2025 hydrochloride 对 MERTK 的选择性是 Axl 的 45 倍(IC₅₀=122nM; K_i=13.3 nM)。UNC2025 hydrochloride 具有良好的 PK 特性，可用于急性白血病的研究。

UNC2025 hydrochloride Chemical Structure

CAS No. : 2070015-17-5

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥1129	In-stock
2 mg	￥600	In-stock
5 mg	￥1000	In-stock
10 mg	￥1700	In-stock
25 mg	￥2800	In-stock
50 mg	￥4800	In-stock
100 mg	￥8000	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

UNC2025 hydrochloride 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Kinase Inhibitor Library
Protein Tyrosine Kinase Compound Library
Anti-Cancer Compound Library
Orally Active Compound Library
Anti-Blood Cancer Compound Library

生物活性

UNC2025 hydrochloride is a potent, ATP-competitive, and highly orally active Mer/Flt3 inhibitor with IC₅₀ values of 0.74 nM and 0.8 nM, respectively. UNC2025 hydrochloride is >45-fold selectivity for MERTK relative to Axl (IC₅₀= 122 nM; K_i = 13.3 nM). UNC2025 hydrochloride exhibits an excellent PK properties, and can be used for the investigation of acute leukemia^[1].

IC₅₀ & Target

IC50: 0.74 nM (Mer); 0.8 nM (Flt3)^[1]

体外研究
(In Vitro)

UNC2025 is against FLT3, MER, AXL, TRKA, TRKC, QIK, TYRO3, SLK, NuaK1, KIT and Met with IC₅₀ values of 0.35 nM, 0.46 nM, 1.65 nM, 1.67 nM, 4.38 nM, 5.75 nM, 5.83 nM, 6.14 nM, 7.97 nM , 8.18 nM and 364 nM, respectively^[1].
UNC2025 (0-60 nM; 1 hour) mediates potent inhibition of Mer phosphorylation with an IC₅₀ of 2.7 nM in 697 B-ALL cells^[1].
UNC2025 (0-60 nM; 1 hour) results in decreased phosphorylation of Flt3 with an IC₅₀ of 14 nM in Flt3-ITD positive Molm-14 acute myeloid leukemia cells^[1].
UNC2025 (3 nM-3 μM; 1 hour) decreases p-MEK, p-AXL, p-TYRO3 expression as a concentration manner in 32D Cells^[1].
UNC2025 (14 nM–10 μM; 48 hours) inhibits MERTK signaling and colony-forming potential in a MERTK-expressing patient sample with a 20-fold difference in sensitivity of MERTK-expressing leukemia blasts relative to normal cord or marrow blood mononuclear cells^[2].
UNC2025 (25-300 nM; 1 hour) mediates potent and dose-dependent decreases in MERTK phosphorylation/activation in both cell lines and inhibition of MERTK correlated with decreased phosphorylation of previously reported MERTK-dependent signaling components STAT6, AKT, and ERK1/2^[2].

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.

Western Blot Analysis^[1]

Cell Line:	32D Cells
Concentration:	0 nM, 3 nM, 10 nM, 20 nM, 30 nM, 100 nM, 1000 nM, 3000 nM
Incubation Time:	1 hour
Result:	Inhibited p-MEK, p-AXL, p-TYRO3 expression.

Cell Proliferation Assay^[1]

Cell Line:	Mononuclear cells
Concentration:	14 nM–10 μM
Incubation Time:	48 hours
Result:	Showed IC₅₀ values ranged from 9.0 nM to >10 μM with a median IC₅₀ of 2.38 μM.

Western Blot Analysis^[2]

Cell Line:	Kasumi-1 AML and 697 B-ALL cells
Concentration:	25-300 nM
Incubation Time:	48 hours
Result:	Decresed p-MERTK, p-STAT6, p- AKT and p-ERK1/2 expression as a dose-dependent manner.

体内研究
(In Vivo)

UNC2025 (intravenous injection or oral adminstration; 3 mg/kg) exhibits an excellent PK properties: low clearance (9.2 mL/min kg), longer half-life (3.8 h), and high oral exposure (100%), it shows T_max, C_max, and AUClast 0.50 hour, 1.6 μM, and 9.2 h μM, respectively^[2].
UNC2025 (orally adminstration; 50 or 75 mg/kg; 34 and 70 days) mediates a statistically significant dose-dependent reduction in tumor burden relative to vehicle. mediates dose-dependent increases in median survival from 26 days after initiation of treatment in vehicle-treated mice, to 34 and 70 days in mice treated with 50 or 75 mg/kg UNC2025, respectively^[2].

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.

Animal Model:	NSG mice injected with 697 B-ALL cells^[2]
Dosage:	50 or 75 mg/kg
Administration:	Oral adminstration
Result:	Delayed the disease progression.

分子量

513.12

Formula

C₂₈H₄₁ClN₆O

CAS 号

2070015-17-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

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

溶解性数据

In Vitro:

H₂O : 55 mg/mL (107.19 mM; Need ultrasonic)

DMSO : 10 mg/mL (19.49 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9489 mL	9.7443 mL	19.4886 mL
5 mM	0.3898 mL	1.9489 mL	3.8977 mL
10 mM	0.1949 mL	0.9744 mL	1.9489 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 (sealed storage, away from moisture)。-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： PBS

Solubility: 100 mg/mL (194.89 mM); Clear solution; Need ultrasonic
2.

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

Solubility: ≥ 1 mg/mL (1.95 mM); Clear solution

此方案可获得 ≥ 1 mg/mL (1.95 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 10.0 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
3.

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

Solubility: ≥ 1 mg/mL (1.95 mM); Clear solution

此方案可获得 ≥ 1 mg/mL (1.95 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 10.0 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]. Zhang W, et al. UNC2025, a Potent and Orally Bioavailable MER/FLT3 Dual Inhibitor. J Med Chem. 2014 Aug 28;57(16):7031-41.

[2]. DeRyckere D, et al. UNC2025, a MERTK Small-Molecule Inhibitor, Is Therapeutically Effective Alone and in Combination with CL14377 in Leukemia Models.Clin Cancer Res. 2017 Mar 15;23(6):1481-1492.

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UNC 669

发表于2024年3月11日由上海金畔生物科技有限公司

UNC 669 纯度: 99.88%

UNC 669，甲基赖氨酸结合结构域的配体，是 L3MBTL1 和 L3MBTL3 的抑制剂，IC₅₀ 分别为 4.2 uM 和 3.1 uM。

UNC 669 Chemical Structure

CAS No. : 1314241-44-5

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥660	In-stock
10 mg	￥600	In-stock
50 mg	￥1350	In-stock
100 mg	￥2500	In-stock
500 mg	￥9900	In-stock
1 g		询价
5 g		询价

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UNC 669 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Epigenetics Compound Library
Histone Modification Research Compound Library
Anti-Cancer Compound Library
Reprogramming Compound Library
Anti-Blood Cancer Compound Library

生物活性

UNC 669, a ligand for a methyl-lysine binding domain, is a potent L3MBTL1 (IC₅₀=4.2 uM) and L3MBTL3 (3.1 uM) inhibitor^[1].

IC₅₀ & Target

IC50: 4.2 uM/3.1 uM (L3MBTL1/L3MBTL3)^[1]

体外研究
(In Vitro)

L3MBTL1, a paralogue of Drosophila tumor suppressor lethal(3)malignant brain tumor (l(3)mbt), binds histones in a methylation state-dependent manner and contributes to higher order chromatin structure and transcriptional repression. Similar to L3MBTL1, the closely related protein, L3MBTL3, also contains three MBT repeats and has been shown to play a role in meduloblastoma formation and normal hematopoiesis in humans^[1]^[2].

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

338.24

Formula

C₁₅H₂₀BrN₃O

CAS 号

1314241-44-5

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 : 50 mg/mL (147.82 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.9565 mL	14.7824 mL	29.5648 mL
5 mM	0.5913 mL	2.9565 mL	5.9130 mL
10 mM	0.2956 mL	1.4782 mL	2.9565 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 (7.39 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.39 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 (7.39 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.39 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 (7.39 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.39 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]. James LI, et al. Small-molecule ligands of methyl-lysine binding proteins: optimization of selectivity for L3MBTL3. J Med Chem. 2013 Sep 26;56(18):7358-71.

[2]. Trojer P, et al. L3MBTL1, a histone-methylation-dependent chromatin lock. Cell. 2007;129(5):915-928.

[3]. Baughman BM, et al. The L3MBTL3 Methyl-Lysine Reader Domain Functions As a Dimer [retracted in: ACS Chem Biol. 2018 Jan 19;13(1):281]. ACS Chem Biol. 2016;11(3):722-728.

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UNC926

发表于2024年3月5日由上海金畔生物科技有限公司

UNC926 纯度: 98.05%

UNC926 是一种 methyl-lysine (Kme) reader domain 抑制剂，可特异性抑制 L3MBTL1，其 IC₅₀ 为 3.9 μM。

UNC926 Chemical Structure

CAS No. : 1184136-10-4

规格	价格	是否有货
5 mg	￥590	In-stock
10 mg	￥980	In-stock
25 mg	￥1900	In-stock
50 mg	￥3900	In-stock
100 mg	￥5500	In-stock
200 mg		询价
500 mg		询价

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UNC926 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Epigenetics Compound Library
Histone Modification Research Compound Library
Anti-Cancer Compound Library
Reprogramming Compound Library
Anti-Blood Cancer Compound Library
Targeted Diversity Library

生物活性

UNC926 is a methyl-lysine (Kme) reader domain inhibitor that inhibits L3MBTL1 with an IC₅₀ of 3.9 μM^[1].

IC₅₀ & Target

IC50: 3.9 μM (L3MBTL1), 3.2 μM (L3MBTL3), 15.6 μM (L3MBTL4)^[1]

体外研究
(In Vitro)

UNC926 also exhibits a low micromolar affinity for the close homolog, L3MBTL3 ( IC₅₀ of 3.2 μM), with a decrease in affinity for the other MBT domains and no binding to CBX7^[1].
UNC926 (1-25 μM) inhibits binding of the 3xMBT domain to H4K20me1.UNC926 inhibits the association of L3MBTL13xMBT with the appropriate histonepeptides in a dose-dependent manner. UNC926 does not have an effect on the binding of 53BP1 to H4K20me1, demonstrating specificity of UNC926 for L3MBTL1 over 53BP1^[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

337.25

Formula

C₁₆H₂₁BrN₂O

CAS 号

1184136-10-4

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 : ≥ 155 mg/mL (459.60 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	2.9652 mL	14.8258 mL	29.6516 mL
5 mM	0.5930 mL	2.9652 mL	5.9303 mL
10 mM	0.2965 mL	1.4826 mL	2.9652 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 (7.41 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.41 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 (7.41 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.41 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 (7.41 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.41 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]. Herold JM, et al. Structure–activity relationships of methyl-lysine reader antagonists. MedChemComm. 2012;3(45):45–51.

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UNC1079

发表于2024年2月26日由上海金畔生物科技有限公司

UNC1079 纯度: ≥98.0%

UNC1079是UNC1021的哌啶类似物，结构相似，但具有较低的有效抑制剂用。

UNC1079 Chemical Structure

CAS No. : 1418741-86-2

规格	价格	是否有货
5 mg	￥1300	In-stock
10 mg	￥2200	In-stock
25 mg	￥5000	In-stock
50 mg	￥8500	In-stock
100 mg	￥14500	In-stock
200 mg		询价
500 mg		询价

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UNC1079 相关产品

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生物活性

UNC1079 is the piperidine analog of UNC1021, as a structurally similar but significantly less potent inhibitor for use as a negative control in cellular studies. Target: L3MBTL3 The low anticipated affinity of UNC1079 was confirmed, as it demonstrated an activity versus L3MBTL3 of > 10 μM by AlphaScreen, which is >1000-fold weaker than UNC1215. UNC1079 also displays weak binding by ITC.

分子量

466.66

Formula

C₂₈H₄₂N₄O₂

CAS 号

1418741-86-2

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 : 2.22 mg/mL (4.76 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1429 mL	10.7144 mL	21.4289 mL
5 mM	—	—	—
10 mM	—	—	—

参考文献

[1]. James LI, et al. Discovery of a chemical probe for the L3MBTL3 methyllysine reader domain. Nat Chem Biol. 2013 Mar;9(3):184-91.

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UNC569

发表于2024年2月20日由上海金畔生物科技有限公司

UNC569 纯度: 98.64%

UNC569 是一种有效、可逆、ATP 竞争性且具有口服活性的 Mer 激酶抑制剂，IC₅₀ 为 2.9 nM，K_i 为 4.3 nM。UNC569 还抑制 Axl 和 Tyro3，IC₅₀ 分别为 37 nM 和 48 nM。UNC569 可用于急性淋巴细胞白血病 (ALL) 和非典型畸胎瘤/横纹肌瘤的研究。

UNC569 Chemical Structure

CAS No. : 1350547-65-7

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
5 mg	￥1100	In-stock
10 mg	￥1800	In-stock
25 mg	￥4000	In-stock
50 mg	￥6500	In-stock
100 mg		询价
200 mg		询价

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UNC569 相关产品

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Bioactive Compound Library Plus
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Protein Tyrosine Kinase Compound Library
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Anti-Blood Cancer Compound Library
Targeted Diversity Library

生物活性

UNC569 is a potent, reversible, ATP-competitive and orally active Mer kinase inhibitor with an IC₅₀ of 2.9 nM and a K_i of 4.3 nM. UNC569 also inhibits Axl and Tyro3 with IC₅₀s of 37 nM and 48 nM, respectively. UNC569 can be used for acute lymphoblastic leukemia (ALL) and atypical teratoid/rhabdoid tumors research^[1]^[2]

IC₅₀ & Target

IC50: 2.9 nM (Mer), 37 nM (Axl), 48 nM (Tyro3)^[1] Ki: 4.3 nM (Mer)^[1]

体外研究
(In Vitro)

UNC569 (24 hours) induces apoptosis in ALL cell lines, and increases the levels of cleaved Caspase 3 and cleaved PARP^[2].
UNC569 (1 µM; 1.5 hours) treatment effectively inhibit the activation of Mer and downstream signaling, including the PI3K/AKT and MAPK/ERK pathways^[2].
UNC569 (1 hour) inhibits Mer phosphorylation levels with IC50 values of 141 nM and 193 nM in human B-ALL (acute lymphoblastic leukemia) 697 and Jurkat cell lines, respectively^[1]^[2].

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.

Apoptosis Analysis^[2]

Cell Line:	697 and Jurkat cells
Concentration:	0.4 µM, 0.8 µM, 1 µM, 1.2 µM, 1.4 µM, 1.6 µM, 1.8 µM, 2 µM
Incubation Time:	24 hours
Result:	Induced apoptosis in ALL cell lines.

Western Blot Analysis^[2]

Cell Line:	697 and Jurkat cells
Concentration:	1 µM
Incubation Time:	1.5 hours
Result:	Inhibited Mer activation and downstream signaling through ERK1/2 and AKT.

体内研究
(In Vivo)

The in vivo pharmacokinetic properties of UNC569 (3 mg/kg) are also assessed in mice via both intravenous (IV) and oral (PO) administration. UNC569 has low systemic clearance (19.5 mL/min/kg), high volume of distribution (V_ss of 5.83 L/kg), and good oral bioavailability (57%)^[1].
Leukemic zebrafish are treated continuously for 2 weeks by immersion in 4 µM UNC569. the result shows that UNC569 induces more than 50% reduction in tumor burden compared with vehicle- and mock-treated fish^[2].

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

396.50

Formula

C₂₂H₂₉FN₆

CAS 号

1350547-65-7

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 : 31.25 mg/mL (78.81 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.5221 mL	12.6103 mL	25.2207 mL
5 mM	0.5044 mL	2.5221 mL	5.0441 mL
10 mM	0.2522 mL	1.2610 mL	2.5221 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 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (6.31 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.31 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]. Jing Liu, et al. Discovery of Novel Small Molecule Mer Kinase Inhibitors for the Treatment of Pediatric Acute Lymphoblastic Leukemia. ACS Med Chem Lett. 2012 Feb 9;3(2):129-134.

[2]. Sandra Christoph, et al. UNC569, a novel small-molecule mer inhibitor with efficacy against acute lymphoblastic leukemia in vitro and in vivo. Mol Cancer Ther. 2013 Nov;12(11):2367-77.

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UNC4976

发表于2024年1月24日由上海金畔生物科技有限公司

UNC4976

UNC4976 是一种 CBX7 染色质结构域与核酸结合的正变构调节剂 (PAM) 拟肽。UNC4976 拮抗 H3K27me3 特异性募集 CBX7 至靶基因，同时增加与 DNA 和 RNA 的非特异性结合。

UNC4976 Chemical Structure

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生物活性	UNC4976 is a positive allosteric modulator (PAM) peptidomimetic of CBX7 chromodomain binding to nucleic acids. UNC4976 simultaneously antagonizes H3K27me3-specific recruitment of CBX7 to target genes while increasing non-specific binding to DNA and RNA^[1].
分子量	847.09
Formula	C₄₇H₇₀N₆O₈
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]. Lamb KN, et al. Discovery and Characterization of a Cellular Potent Positive Allosteric Modulator of the Polycomb Repressive Complex 1 Chromodomain, CBX7. Cell Chem Biol. 2019 Aug 14.

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UNC4976

发表于2024年1月24日由上海金畔生物科技有限公司

UNC4976

UNC4976 Chemical Structure

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	UNC4976 is a positive allosteric modulator (PAM) peptidomimetic of CBX7 chromodomain binding to nucleic acids. UNC4976 simultaneously antagonizes H3K27me3-specific recruitment of CBX7 to target genes while increasing non-specific binding to DNA and RNA^[1].
分子量	847.09
Formula	C₄₇H₇₀N₆O₈
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]. Lamb KN, et al. Discovery and Characterization of a Cellular Potent Positive Allosteric Modulator of the Polycomb Repressive Complex 1 Chromodomain, CBX7. Cell Chem Biol. 2019 Aug 14.

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

UNC4976

发表于2024年1月24日由上海金畔生物科技有限公司

UNC4976

UNC4976 Chemical Structure

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

* Please select Quantity before adding items.

生物活性	UNC4976 is a positive allosteric modulator (PAM) peptidomimetic of CBX7 chromodomain binding to nucleic acids. UNC4976 simultaneously antagonizes H3K27me3-specific recruitment of CBX7 to target genes while increasing non-specific binding to DNA and RNA^[1].
分子量	847.09
Formula	C₄₇H₇₀N₆O₈
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]. Lamb KN, et al. Discovery and Characterization of a Cellular Potent Positive Allosteric Modulator of the Polycomb Repressive Complex 1 Chromodomain, CBX7. Cell Chem Biol. 2019 Aug 14.

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UNC2399

发表于2024年1月23日由上海金畔生物科技有限公司

UNC2399

UNC2399，一种生物素化的 UNC1999，是选择性的 EZH2 降解剂，对 EZH2 具有很高的体外效力，IC₅₀ 值为 17 nM。

UNC2399 Chemical Structure

CAS No. : 2412791-72-9

规格		是否有货
1 mg		询价

* Please select Quantity before adding items.

生物活性

UNC2399, a biotinylated UNC1999, is a selective EZH2 degrader, maintaining high in vitro potency for EZH2, with an IC₅₀ of 17 nM^[1]^[2].

IC₅₀ & Target^[1]

EZH2

17 nM (IC₅₀)

体外研究
(In Vitro)

UNC2399 (1-1000 nM) displays high in vitro potency (IC₅₀=17±2 nM) in the EZH2 radioactive biochemical assay^[1].
UNC2399 (100 μM) enriches EZH2 from HEK293T cell lysates^[1].

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

分子量

927.17

Formula

C₄₈H₆₆N₁₀O₇S

CAS 号

2412791-72-9

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]. Konze KD, et, al. An orally bioavailable chemical probe of the Lysine Methyltransferases EZH2 and EZH1. ACS Chem Biol. 2013; 8(6): 1324-34.

[2]. Ma A, et, al. Discovery of a first-in-class EZH2 selective degrader. Nat Chem Biol. 2020 Feb;16(2):214-222.

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UNC2399

发表于2024年1月22日由上海金畔生物科技有限公司

UNC2399

UNC2399，一种生物素化的 UNC1999，是选择性的 EZH2 降解剂，对 EZH2 具有很高的体外效力，IC₅₀ 值为 17 nM。

UNC2399 Chemical Structure

CAS No. : 2412791-72-9

规格		是否有货
1 mg		询价

* Please select Quantity before adding items.

生物活性

UNC2399, a biotinylated UNC1999, is a selective EZH2 degrader, maintaining high in vitro potency for EZH2, with an IC₅₀ of 17 nM^[1]^[2].

IC₅₀ & Target^[1]

EZH2

17 nM (IC₅₀)

体外研究
(In Vitro)

UNC2399 (1-1000 nM) displays high in vitro potency (IC₅₀=17±2 nM) in the EZH2 radioactive biochemical assay^[1].
UNC2399 (100 μM) enriches EZH2 from HEK293T cell lysates^[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

927.17

Formula

C₄₈H₆₆N₁₀O₇S

CAS 号

2412791-72-9

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]. Konze KD, et, al. An orally bioavailable chemical probe of the Lysine Methyltransferases EZH2 and EZH1. ACS Chem Biol. 2013; 8(6): 1324-34.

[2]. Ma A, et, al. Discovery of a first-in-class EZH2 selective degrader. Nat Chem Biol. 2020 Feb;16(2):214-222.

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

UNC2399

发表于2024年1月22日由上海金畔生物科技有限公司

UNC2399

UNC2399，一种生物素化的 UNC1999，是选择性的 EZH2 降解剂，对 EZH2 具有很高的体外效力，IC₅₀ 值为 17 nM。

UNC2399 Chemical Structure

CAS No. : 2412791-72-9

规格		是否有货
1 mg		询价

* Please select Quantity before adding items.

生物活性

UNC2399, a biotinylated UNC1999, is a selective EZH2 degrader, maintaining high in vitro potency for EZH2, with an IC₅₀ of 17 nM^[1]^[2].

IC₅₀ & Target^[1]

EZH2

17 nM (IC₅₀)

体外研究
(In Vitro)

UNC2399 (1-1000 nM) displays high in vitro potency (IC₅₀=17±2 nM) in the EZH2 radioactive biochemical assay^[1].
UNC2399 (100 μM) enriches EZH2 from HEK293T cell lysates^[1].

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

分子量

927.17

Formula

C₄₈H₆₆N₁₀O₇S

CAS 号

2412791-72-9

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]. Konze KD, et, al. An orally bioavailable chemical probe of the Lysine Methyltransferases EZH2 and EZH1. ACS Chem Biol. 2013; 8(6): 1324-34.

[2]. Ma A, et, al. Discovery of a first-in-class EZH2 selective degrader. Nat Chem Biol. 2020 Feb;16(2):214-222.

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

UNC2400

发表于2024年1月20日由上海金畔生物科技有限公司

UNC2400

UNC2400 是UNC1999 的一个类似物，其活性比 UNC1999 小1000 倍以上，可作为 UNC1999 的阴性对照。

UNC2400 Chemical Structure

CAS No. : 1433200-49-7

规格		是否有货
5 mg		询价

* Please select Quantity before adding items.

生物活性	UNC2400 is a close analog of UNC1999 with >1,000-fold lower potency than UNC1999 as a negative control for cell-based studies^[1]^[2].
分子量	597.79
Formula	C₃₅H₄₇N₇O₂
CAS 号	1433200-49-7
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]. Kyle D Konze, et al. An orally bioavailable chemical probe of the Lysine Methyltransferases EZH2 and EZH1. ACS Chem Biol. 2013;8(6):1324-34. [2]. Bowen Xu, et al. Selective inhibition of EZH2 and EZH1 enzymatic activity by a small molecule suppresses MLL-rearranged leukemia. Blood. 2015 Jan 8;125(2):346-57.

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

UNC2400

发表于2024年1月20日由上海金畔生物科技有限公司

UNC2400

UNC2400 是UNC1999 的一个类似物，其活性比 UNC1999 小1000 倍以上，可作为 UNC1999 的阴性对照。

UNC2400 Chemical Structure

CAS No. : 1433200-49-7

规格		是否有货
5 mg		询价

* Please select Quantity before adding items.

生物活性	UNC2400 is a close analog of UNC1999 with >1,000-fold lower potency than UNC1999 as a negative control for cell-based studies^[1]^[2].
分子量	597.79
Formula	C₃₅H₄₇N₇O₂
CAS 号	1433200-49-7
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]. Kyle D Konze, et al. An orally bioavailable chemical probe of the Lysine Methyltransferases EZH2 and EZH1. ACS Chem Biol. 2013;8(6):1324-34. [2]. Bowen Xu, et al. Selective inhibition of EZH2 and EZH1 enzymatic activity by a small molecule suppresses MLL-rearranged leukemia. Blood. 2015 Jan 8;125(2):346-57.

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

UNC2400

发表于2024年1月20日由上海金畔生物科技有限公司

UNC2400

UNC2400 是UNC1999 的一个类似物，其活性比 UNC1999 小1000 倍以上，可作为 UNC1999 的阴性对照。

UNC2400 Chemical Structure

CAS No. : 1433200-49-7

规格		是否有货
5 mg		询价

* Please select Quantity before adding items.

生物活性	UNC2400 is a close analog of UNC1999 with >1,000-fold lower potency than UNC1999 as a negative control for cell-based studies^[1]^[2].
分子量	597.79
Formula	C₃₅H₄₇N₇O₂
CAS 号	1433200-49-7
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]. Kyle D Konze, et al. An orally bioavailable chemical probe of the Lysine Methyltransferases EZH2 and EZH1. ACS Chem Biol. 2013;8(6):1324-34. [2]. Bowen Xu, et al. Selective inhibition of EZH2 and EZH1 enzymatic activity by a small molecule suppresses MLL-rearranged leukemia. Blood. 2015 Jan 8;125(2):346-57.

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

UNC4203

发表于2023年12月29日由上海金畔生物科技有限公司

UNC4203

UNC4203 是有效的、具有口服活性的、高度选择性的 MERTK 抑制剂，其对 MERTK、AXL、TYRO3 和 FLT3 的 IC₅₀ 值分别为 1.2 nM、140 nM、42 nM 和 90 nM。

UNC4203 Chemical Structure

CAS No. : 1818234-19-3

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	UNC4203 is a potent, orally available and highly selective MERTK inhibitor, with IC₅₀s of 1.2 nM, 140 nM, 42 nM and 90 nM for MERTK, AXL, TYRO3 and FLT3, respectively^[1].
体内研究 (In Vivo)	Mice are treated with UNC4203 (compound 24) at a dose of 10 mg/kg administered via oral (po) or iv routes. Under the condition, UNC4203 (compound 24) has 58% oral bioavailability with a 7.8 h half-life, 1.7 L/kg volume of distribution, and 36 mL/min/kg clearance^[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量	504.71
Formula	C₃₀H₄₄N₆O
CAS 号	1818234-19-3
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]. Hongchao Zheng, et al. UNC5293, a potent, orally available and highly MERTK-selective inhibitor. Eur J Med Chem. 2021 Aug 5;220:113534.

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UNC4203

发表于2023年12月29日由上海金畔生物科技有限公司

UNC4203

UNC4203 是有效的、具有口服活性的、高度选择性的 MERTK 抑制剂，其对 MERTK、AXL、TYRO3 和 FLT3 的 IC₅₀ 值分别为 1.2 nM、140 nM、42 nM 和 90 nM。

UNC4203 Chemical Structure

CAS No. : 1818234-19-3

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

* Please select Quantity before adding items.

生物活性	UNC4203 is a potent, orally available and highly selective MERTK inhibitor, with IC₅₀s of 1.2 nM, 140 nM, 42 nM and 90 nM for MERTK, AXL, TYRO3 and FLT3, respectively^[1].
体内研究 (In Vivo)	Mice are treated with UNC4203 (compound 24) at a dose of 10 mg/kg administered via oral (po) or iv routes. Under the condition, UNC4203 (compound 24) has 58% oral bioavailability with a 7.8 h half-life, 1.7 L/kg volume of distribution, and 36 mL/min/kg clearance^[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	504.71
Formula	C₃₀H₄₄N₆O
CAS 号	1818234-19-3
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]. Hongchao Zheng, et al. UNC5293, a potent, orally available and highly MERTK-selective inhibitor. Eur J Med Chem. 2021 Aug 5;220:113534.

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