Ras
Ras产品
目录号 | 产品描述 | 文献引用 | 实验数据 |
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S1314 |
Zoledronic AcidZoledronic acid (ZA, Zoledronate, CGP-4244, GP42446A, ZOL 446, Zometa, Zomera, Aclasta, Reclast), 破骨细胞抑制剂,通过抑制甲羟戊酸途径诱导破骨细胞凋亡,并防止小GTP结合蛋白,如Ras 和 Rho的异戊二烯化。Zoledronic acid (ZA) 还可诱导自噬。 |
![]() ![]() Isolation of cd T cells. PBMCs were cultured in the presence of 400 nM ZA and 200 IU/ml IL-2 over 10 days. cd T cells were isolated by negative MACS isolation. Flow cytometric analysis revealed co-expression of CD3 and TCRcd on over 99% of cells of the flow through fraction (A). The T cells expressed the TCRVd2 chain (B) and the CD56 protein (C).
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S2797 |
LonafarnibLonafarnib (SCH66336) 是一种口服生物有效的FPTase抑制剂,作用于H-ras,K-ras-4B和N-ras,无细胞试验中IC50分别为1.9 nM, 5.2 nM和2.8 nM。Phase 3。 |
![]() ![]() Huh-7/hNTCP cells were infected with in vitro generated HDV in the presence or absence of MyrB (50 nM) or lonafarnib (200 nM). After 5 days cells were labeled with HDAg#280, secondary AF488 and stained with DAPI. A representative of four independent experiments is shown.
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S7332 |
K-Ras(G12C) inhibitor 9K-Ras(G12C) inhibitor 9 是致癌的K-Ras(G12C)的变构抑制剂。 |
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S7684 |
SalirasibSalirasib (Farnesylthiosalicylic acid, FTS)是一种有效的竞争性prenylated protein methyltransferase (PPMTase)抑制剂, Ki为2.6 μM,其抑制Ras甲基化。Salirasib 具有抗肿瘤的活性并可诱导凋亡。Phase 2。 |
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S8830 |
Sotorasib (AMG510)Sotorasib (AMG510) 是有效的KRAS G12C共价抑制剂,具有潜在的抗肿瘤活性。该AMG510是手性化合物。 |
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S6905New |
MCP110MCP110 是一种 Ras/Raf-1 相互作用的抑制剂。MCP110 可破坏激活的Ras与Raf的相互作用,具有治疗人类肿瘤的潜力。 |
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S8831New |
MRTX-1257MRTX-1257 是一种有效的、选择性的、不可逆的、共价的和口服活性的 KRAS G12C 的抑制剂,可在H358细胞中抑制KRAS依赖性的ERK磷酸化,对应的IC50值为900 pM。 |
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S8916New |
BI-3406BI-3406 (compound I-6) 是一种有效的、选择性和口服活性的抑制剂,可抑制 KRAS 和 Son of Sevenless 1 (SOS1) 之间的相互作用,其IC50值为6 nM。BI-3406 可减少 GTP-loaded KRAS 的形成,并抑制MAPK信号通路。BI-3406 具有抗肿瘤的活性。 |
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S0323New |
Antineoplaston A10Antineoplaston A10 是人体中天然存在的物质,可以潜在地用于治疗神经胶质瘤,淋巴瘤,星形细胞瘤和乳腺癌。Antineoplaston A10 的主要活性成分(Phenylacetylglutamine, PG)抑制 RAS 并促进其凋亡。 |
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S0023 |
K-Ras-IN-1K-Ras-IN-1 (MDK-3017)可通过结合apo-Ras晶体结构中被Tyr-71占据的疏水口袋中的K-Ras来抑制 K-Ras。 |
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S7224 |
DeltarasinDeltarasin是一种小分子抑制剂,抑制KRAS-PDEδ相互作用,其结合到纯PDEδ的Kd值为38 nM。 |
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S8826 |
BAY-293BAY-293可选择性抑制KRAS-SOS1相互作用,IC50为21 nM。 |
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S7330 |
6H056H05是一个致癌K-Ras(G12C)的选择性、变构抑制剂。 |
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S7331 |
K-Ras(G12C) inhibitor 12K-Ras(G12C) inhibitor 12是致癌K-Ras(G12C)的变构抑制剂。 |
![]() ![]() (A) Proliferation of Calu-1 cells after SAHA and K-ras inhibitor (K-ras C12) treatment. Calu-1 cells, containing an activating G12C K-ras mutation, were treated with SAHA (2.5 mM) and K-ras C12 (10 mM) for 24 h and analyzed as in Figure Figure1A.1A. (B) Immunoblotting of Calu-1 cells treated with inhibitors. Cells were treated with inhibitors as indicated for 24 hrs. Cell lysates were collected and immunoblotted with antibodies indicated.
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S8303 |
Kobe0065Kobe0065是H-Ras-cRaf1相互作用的抑制剂,能有效抑制H-Ras·GTP与c-Raf-1 RBD的结合,Ki值为46±13 μM。 |
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S7333 |
K-Ras(G12C) inhibitor 6K-Ras(G12C) inhibitor 6 是一种变构的,选择性的致瘤性K-Ras(G12C)抑制剂。 |
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S7607 |
BQU57BQU57,RBC8的衍生物,是一种相对于GTPases Ras 和 RhoA的选择性GTPase Ral 抑制剂。 |
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S8707 |
ARS-1620ARS-1620是一种有效的、具有口服活性的KRASG12C共价抑制剂,在体内可产生迅速而持续地结合(占用)靶点,诱导肿瘤消退。 |
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S6527 |
Kobe2602Kobe2602是选择性Ras抑制剂,抑制H-Ras GTP与c-Raf-1结合,Ki值为149 μM。 |
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S5279 |
Fendiline hydrochlorideFendiline hydrochloride is the hydrochloride salt form of Fendiline, which is an L-type calcium channel blocker and also a specific inhibitor of K-Ras plasma membrane targeting with no detectable effect on the localization of H- and N-Ras. |
||
S8884 |
Adagrasib (MRTX849)Adagrasib (MRTX849) 是一种有效的,选择性的和共价的KRAS G12C抑制剂,具有良好的药物样特性,可选择性地修饰GDP结合的KRAS G12C中的突变半胱氨酸12并抑制KRAS依赖性信号传导。 |
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S8499 |
KRpep-2dKRpep-2d是选择性的K-Ras(G12D)抑制性环肽,相较于WT K-Ras和K-Ras(G12C),对K-Ras(G12D)选择性更高,IC50为1.6 nM。 |
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S8156 |
ARS-853 (ARS853)ARS-853 是一种具有选择性的KRAS(G12C)共价结合抑制剂,通过结合GDP-肿瘤蛋白并阻止其激活,抑制突变型KRAS所驱动的信号通路。ARS-853 还可诱导凋亡。 |
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S8955 |
Sotorasib (AMG510) racemateSotorasib (AMG510) racemate 是AMG-510的外消旋体。AMG-510是一种有效的 KRAS G12C 共价抑制剂,具有潜在的抗肿瘤活性。 |
||
S5244 |
Zoledronic acid monohydrateZoledronic acid (Zoledronate, CGP-4244) monohydrate 是 Zoledronic acid (唑来膦酸) 的一水合物,是有效的破骨细胞抑制剂,可通过抑制甲戊二羟酸途径的酶、阻止小GTP结合蛋白如Ras和Rho的异戊二烯化来诱导破骨细胞凋亡。 |
||
S0458New |
KY1220KY1220 通过靶向 Wnt/β-catenin 通路,使得 β-catenin 和 Ras 的稳定性被破坏,其在HEK293 reporter细胞中的IC50值为2.1 μM。 |
目录号 | 产品描述 | 文献引用 | 实验数据 |
---|---|---|---|
S1314 |
Zoledronic AcidZoledronic acid (ZA, Zoledronate, CGP-4244, GP42446A, ZOL 446, Zometa, Zomera, Aclasta, Reclast), 破骨细胞抑制剂,通过抑制甲羟戊酸途径诱导破骨细胞凋亡,并防止小GTP结合蛋白,如Ras 和 Rho的异戊二烯化。Zoledronic acid (ZA) 还可诱导自噬。 |
![]() ![]() Isolation of cd T cells. PBMCs were cultured in the presence of 400 nM ZA and 200 IU/ml IL-2 over 10 days. cd T cells were isolated by negative MACS isolation. Flow cytometric analysis revealed co-expression of CD3 and TCRcd on over 99% of cells of the flow through fraction (A). The T cells expressed the TCRVd2 chain (B) and the CD56 protein (C).
|
|
S2797 |
LonafarnibLonafarnib (SCH66336) 是一种口服生物有效的FPTase抑制剂,作用于H-ras,K-ras-4B和N-ras,无细胞试验中IC50分别为1.9 nM, 5.2 nM和2.8 nM。Phase 3。 |
![]() ![]() Huh-7/hNTCP cells were infected with in vitro generated HDV in the presence or absence of MyrB (50 nM) or lonafarnib (200 nM). After 5 days cells were labeled with HDAg#280, secondary AF488 and stained with DAPI. A representative of four independent experiments is shown.
|
|
S7332 |
K-Ras(G12C) inhibitor 9K-Ras(G12C) inhibitor 9 是致癌的K-Ras(G12C)的变构抑制剂。 |
||
S7684 |
SalirasibSalirasib (Farnesylthiosalicylic acid, FTS)是一种有效的竞争性prenylated protein methyltransferase (PPMTase)抑制剂, Ki为2.6 μM,其抑制Ras甲基化。Salirasib 具有抗肿瘤的活性并可诱导凋亡。Phase 2。 |
||
S8830 |
Sotorasib (AMG510)Sotorasib (AMG510) 是有效的KRAS G12C共价抑制剂,具有潜在的抗肿瘤活性。该AMG510是手性化合物。 |
||
S6905New |
MCP110MCP110 是一种 Ras/Raf-1 相互作用的抑制剂。MCP110 可破坏激活的Ras与Raf的相互作用,具有治疗人类肿瘤的潜力。 |
||
S8831New |
MRTX-1257MRTX-1257 是一种有效的、选择性的、不可逆的、共价的和口服活性的 KRAS G12C 的抑制剂,可在H358细胞中抑制KRAS依赖性的ERK磷酸化,对应的IC50值为900 pM。 |
||
S8916New |
BI-3406BI-3406 (compound I-6) 是一种有效的、选择性和口服活性的抑制剂,可抑制 KRAS 和 Son of Sevenless 1 (SOS1) 之间的相互作用,其IC50值为6 nM。BI-3406 可减少 GTP-loaded KRAS 的形成,并抑制MAPK信号通路。BI-3406 具有抗肿瘤的活性。 |
||
S0323New |
Antineoplaston A10Antineoplaston A10 是人体中天然存在的物质,可以潜在地用于治疗神经胶质瘤,淋巴瘤,星形细胞瘤和乳腺癌。Antineoplaston A10 的主要活性成分(Phenylacetylglutamine, PG)抑制 RAS 并促进其凋亡。 |
||
S0023 |
K-Ras-IN-1K-Ras-IN-1 (MDK-3017)可通过结合apo-Ras晶体结构中被Tyr-71占据的疏水口袋中的K-Ras来抑制 K-Ras。 |
||
S7224 |
DeltarasinDeltarasin是一种小分子抑制剂,抑制KRAS-PDEδ相互作用,其结合到纯PDEδ的Kd值为38 nM。 |
||
S8826 |
BAY-293BAY-293可选择性抑制KRAS-SOS1相互作用,IC50为21 nM。 |
||
S7330 |
6H056H05是一个致癌K-Ras(G12C)的选择性、变构抑制剂。 |
||
S7331 |
K-Ras(G12C) inhibitor 12K-Ras(G12C) inhibitor 12是致癌K-Ras(G12C)的变构抑制剂。 |
![]() ![]() (A) Proliferation of Calu-1 cells after SAHA and K-ras inhibitor (K-ras C12) treatment. Calu-1 cells, containing an activating G12C K-ras mutation, were treated with SAHA (2.5 mM) and K-ras C12 (10 mM) for 24 h and analyzed as in Figure Figure1A.1A. (B) Immunoblotting of Calu-1 cells treated with inhibitors. Cells were treated with inhibitors as indicated for 24 hrs. Cell lysates were collected and immunoblotted with antibodies indicated.
|
|
S8303 |
Kobe0065Kobe0065是H-Ras-cRaf1相互作用的抑制剂,能有效抑制H-Ras·GTP与c-Raf-1 RBD的结合,Ki值为46±13 μM。 |
||
S7333 |
K-Ras(G12C) inhibitor 6K-Ras(G12C) inhibitor 6 是一种变构的,选择性的致瘤性K-Ras(G12C)抑制剂。 |
||
S7607 |
BQU57BQU57,RBC8的衍生物,是一种相对于GTPases Ras 和 RhoA的选择性GTPase Ral 抑制剂。 |
||
S8707 |
ARS-1620ARS-1620是一种有效的、具有口服活性的KRASG12C共价抑制剂,在体内可产生迅速而持续地结合(占用)靶点,诱导肿瘤消退。 |
||
S6527 |
Kobe2602Kobe2602是选择性Ras抑制剂,抑制H-Ras GTP与c-Raf-1结合,Ki值为149 μM。 |
||
S5279 |
Fendiline hydrochlorideFendiline hydrochloride is the hydrochloride salt form of Fendiline, which is an L-type calcium channel blocker and also a specific inhibitor of K-Ras plasma membrane targeting with no detectable effect on the localization of H- and N-Ras. |
||
S8884 |
Adagrasib (MRTX849)Adagrasib (MRTX849) 是一种有效的,选择性的和共价的KRAS G12C抑制剂,具有良好的药物样特性,可选择性地修饰GDP结合的KRAS G12C中的突变半胱氨酸12并抑制KRAS依赖性信号传导。 |
||
S8499 |
KRpep-2dKRpep-2d是选择性的K-Ras(G12D)抑制性环肽,相较于WT K-Ras和K-Ras(G12C),对K-Ras(G12D)选择性更高,IC50为1.6 nM。 |
||
S8156 |
ARS-853 (ARS853)ARS-853 是一种具有选择性的KRAS(G12C)共价结合抑制剂,通过结合GDP-肿瘤蛋白并阻止其激活,抑制突变型KRAS所驱动的信号通路。ARS-853 还可诱导凋亡。 |
||
S8955 |
Sotorasib (AMG510) racemateSotorasib (AMG510) racemate 是AMG-510的外消旋体。AMG-510是一种有效的 KRAS G12C 共价抑制剂,具有潜在的抗肿瘤活性。 |
||
S5244 |
Zoledronic acid monohydrateZoledronic acid (Zoledronate, CGP-4244) monohydrate 是 Zoledronic acid (唑来膦酸) 的一水合物,是有效的破骨细胞抑制剂,可通过抑制甲戊二羟酸途径的酶、阻止小GTP结合蛋白如Ras和Rho的异戊二烯化来诱导破骨细胞凋亡。 |
目录号 | 产品描述 | 文献引用 | 实验数据 |
---|---|---|---|
S0458New |
KY1220KY1220 通过靶向 Wnt/β-catenin 通路,使得 β-catenin 和 Ras 的稳定性被破坏,其在HEK293 reporter细胞中的IC50值为2.1 μM。 |