Ras
シグナル伝達経路
研究分野
阻害剤の選択性比較
| カタログ番号 | 製品カタログ | 溶解度(25°C) | ||
|---|---|---|---|---|
| 水 | DMSO | アルコール | ||
| S1314 | Zoledronic Acid | <1 mg/mL | 0.004 mg/mL | ''''<1 mg/mL |
| S2797 | Lonafarnib | <1 mg/mL | 127 mg/mL | ''127 mg/mL |
| S7332 | K-Ras(G12C) inhibitor 9 | <1 mg/mL | 53 mg/mL | '<1 mg/mL |
| S7684 | Salirasib | ' mg/mL | ||
| S8830 | Sotorasib (AMG510) | <1 mg/mL | 100 mg/mL | '''100 mg/mL |
| S6905 | MCP110 | <1 mg/mL | 100 mg/mL | '''100 mg/mL |
| S8916 | BI-3406 | <1 mg/mL | 92 mg/mL | '''''92 mg/mL |
| S8959 | BI-2852 | ' mg/mL | ||
| S0780 | Oncrasin-1 | ' mg/mL | ||
| S0023 | K-Ras-IN-1 | <1 mg/mL | 41 mg/mL | '''''41 mg/mL |
| S8955 | Sotorasib (AMG510) racemate | ' mg/mL | ||
| S8884 | MRTX849 | <1 mg/mL | 100 mg/mL | '50 mg/mL |
| S7224 | Deltarasin | <1 mg/mL | 100 mg/mL | '100 mg/mL |
| S8826 | BAY-293 | <1 mg/mL | 90 mg/mL | '90 mg/mL |
| S7330 | 6H05 | 100 mg/mL | 100 mg/mL | '100 mg/mL |
| S7331 | K-Ras(G12C) inhibitor 12 | <1 mg/mL | 27 mg/mL | '<1 mg/mL |
| S8303 | Kobe0065 | <1 mg/mL | 89 mg/mL | '13 mg/mL |
| S7333 | K-Ras(G12C) inhibitor 6 | <1 mg/mL | 81 mg/mL | '30 mg/mL |
| S7607 | BQU57 | <1 mg/mL | 66 mg/mL | '20 mg/mL |
| S8707 | ARS-1620 | <1 mg/mL | 86 mg/mL | '60 mg/mL |
| S6527 | Kobe2602 | <1 mg/mL | 84 mg/mL | '40 mg/mL |
| S5279 | Fendiline hydrochloride | -1 mg/mL | 70 mg/mL | '-1 mg/mL |
| S8499 | KRpep-2d | 100 mg/mL | -1 mg/mL | '-1 mg/mL |
| S8156 | ARS-853 (ARS853) | <1 mg/mL | 86 mg/mL | '''1 mg/mL |
| S5244 | Zoledronic acid monohydrate | <1 mg/mL | 0.01 mg/mL | '''''''<1 mg/mL |
| S0458 | KY1220 | <1 mg/mL | 63 mg/mL | ''''<1 mg/mL |
Ras製品
| 製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|
| S1314 |
Zoledronic AcidZoledronic acid (ZA, Zoledronate, CGP-4244), a potent osteoclast inhibitor, induces apoptosis in osteoclasts by inhibiting enzymes of the mevalonate pathway and preventing the isoprenylation of small GTP-binding proteins such as Ras and Rho. Zoledronic acid (ZA) also induces autophagy. |
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) is an orally bioavailable FPTase inhibitor for H-ras, K-ras-4B and N-ras with IC50 of 1.9 nM, 5.2 nM and 2.8 nM in cell-free assays, respectively. 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 is an allosteric inhibitor of oncogenic K-Ras(G12C). |
||
| S7684 |
SalirasibSalirasib is a potent competitive prenylated protein methyltransferase (PPMTase) inhibitor with Ki of 2.6 μM, which inhibits Ras methylation. Salirasib exerts antitumor effects and induces autophagy. Salirasib exerts antitumor effects and induces autophagy. Phase 2. |
||
| S8830 |
Sotorasib (AMG510)Sotorasib (AMG510) is a potent KRAS G12C covalent inhibitor with potential antineoplastic activity.This AMG510 is a chiral compound. |
||
| S6905新 |
MCP110MCP110 is an inhibitor of Ras/Raf-1 interaction. MCP110 disrupts the interaction of activated Ras with Raf and is potential for the treatment of human tumors. |
||
| S8916新 |
BI-3406BI-3406 is a potent, orally active and selective inhibitor of the interaction between KRAS and Son of Sevenless 1 (SOS1) with IC50 of 6 nM. BI-3406 reduces the formation of GTP-loaded KRAS, and inhibits MAPK pathway signaling with anticancer activities. |
||
| S8959新 |
BI-2852BI-2852 is a potent KRAS inhibitor for the switch I/II pocket (SI/II-pocket) by structure-based drug design with nanomolar affinity. BI-2852 blocks GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells. |
||
| S0780新 |
Oncrasin-1Oncrasin-1 is a potent and effective inhibitor with anticancer activity. Oncrasin-1 kills various human lung cancer cells with K-Ras mutations at low or submicromolar concentrations. Oncrasin-1 drives abnormal aggregation of PKCι in nucleus of sensitive cells but not in resistant cells. |
||
| S0023新 |
K-Ras-IN-1K-Ras-IN-1 inhibits K-Ras by binding to K-Ras in a hydrophobic pocket that is occupied by Tyr-71 in the apo-Ras crystal structure. |
||
| S8955新 |
Sotorasib (AMG510) racemateSotorasib (AMG510) racemate is a racemic of AMG-510 which is a potent KRAS G12C covalent inhibitor with potential antineoplastic activity. |
||
| S8884新 |
MRTX849MRTX849 is a potent, selective, and covalent KRAS G12C inhibitor that exhibits favorable drug-like properties, selectively modifies mutant cysteine 12 in GDP-bound KRAS G12C and inhibits KRAS-dependent signaling. |
||
| S7224 |
DeltarasinDeltarasin is a small molecular inhibitor of KRAS-PDEδ interaction with Kd of 38 nM for binding to purified PDEδ. |
||
| S8826 |
BAY-293BAY-293 selectively inhibits the KRAS-SOS1 interaction with an IC50 of 21 nM. |
||
| S7330 |
6H056H05 is a selective, and allosteric inhibitor of oncogenic K-Ras(G12C). |
||
| S7331 |
K-Ras(G12C) inhibitor 12K-Ras(G12C) inhibitor 12 is an allosteric inhibitor of oncogenic K-Ras(G12C). |
-inhibitor-12-S733101W0420171213.gif)
-inhibitor-12-S733101W0420171213.gif)
(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 is H-Ras-cRaf1 interaction inhibitor, exhibiting potent activity to competitively inhibit the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki value of 46 ± 13 μM. |
||
| S7333 |
K-Ras(G12C) inhibitor 6K-Ras(G12C) inhibitor 6 is an allosteric, and selective inhibitor of oncogenic K-Ras(G12C). |
||
| S7607 |
BQU57BQU57, a derivative of RBC8, is a selective GTPase Ral inhibitor relative to the GTPases Ras and RhoA. |
||
| S8707 |
ARS-1620ARS-1620 is a potent, orally bioavailable covalent inhibitor of KRASG12C) and could achieve rapid and sustained in vivo target occupancy to induce tumor regression. |
||
| S6527 |
Kobe2602Kobe2602 is a selective Ras inhibitor that blocks H-Ras GTP binding to c-Raf-1 (Ki = 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. |
||
| S8499 |
KRpep-2dKRpep-2d is a K-Ras(G12D) selective inhibitory cyclic peptide with selectivity against wild-type (WT) K-Ras and the K-Ras(G12C) mutant. The IC50 value is 1.6 nM. |
||
| S8156 |
ARS-853 (ARS853)ARS-853 is a selective, covalent KRAS(G12C) inhibitor that inhibits mutant KRAS-driven signaling by binding to the GDP-bound oncoprotein and preventing activation. ARS-853 also induces apoptosis. |
||
| S5244 |
Zoledronic acid monohydrateZoledronic acid (Zoledronate, CGP-4244) monohydrate, a nitrogen-containing bisphosphonate, is a potent osteoclast inhibitor which induces apoptosis in osteoclasts by inhibiting enzymes of the mevalonate pathway and preventing the isoprenylation of small GTP-binding proteins such as Ras and Rho. |
||
| S0458新 |
KY1220KY1220 is a small molecule that destabilizes both β-catenin and Ras, via targeting the Wnt/β-catenin pathway with IC50 of 2.1 μM in HEK293 reporter cells. |
| 製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|
| S1314 |
Zoledronic AcidZoledronic acid (ZA, Zoledronate, CGP-4244), a potent osteoclast inhibitor, induces apoptosis in osteoclasts by inhibiting enzymes of the mevalonate pathway and preventing the isoprenylation of small GTP-binding proteins such as Ras and Rho. Zoledronic acid (ZA) also induces autophagy. |
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) is an orally bioavailable FPTase inhibitor for H-ras, K-ras-4B and N-ras with IC50 of 1.9 nM, 5.2 nM and 2.8 nM in cell-free assays, respectively. 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 is an allosteric inhibitor of oncogenic K-Ras(G12C). |
||
| S7684 |
SalirasibSalirasib is a potent competitive prenylated protein methyltransferase (PPMTase) inhibitor with Ki of 2.6 μM, which inhibits Ras methylation. Salirasib exerts antitumor effects and induces autophagy. Salirasib exerts antitumor effects and induces autophagy. Phase 2. |
||
| S8830 |
Sotorasib (AMG510)Sotorasib (AMG510) is a potent KRAS G12C covalent inhibitor with potential antineoplastic activity.This AMG510 is a chiral compound. |
||
| S6905新 |
MCP110MCP110 is an inhibitor of Ras/Raf-1 interaction. MCP110 disrupts the interaction of activated Ras with Raf and is potential for the treatment of human tumors. |
||
| S8916新 |
BI-3406BI-3406 is a potent, orally active and selective inhibitor of the interaction between KRAS and Son of Sevenless 1 (SOS1) with IC50 of 6 nM. BI-3406 reduces the formation of GTP-loaded KRAS, and inhibits MAPK pathway signaling with anticancer activities. |
||
| S8959新 |
BI-2852BI-2852 is a potent KRAS inhibitor for the switch I/II pocket (SI/II-pocket) by structure-based drug design with nanomolar affinity. BI-2852 blocks GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells. |
||
| S0780新 |
Oncrasin-1Oncrasin-1 is a potent and effective inhibitor with anticancer activity. Oncrasin-1 kills various human lung cancer cells with K-Ras mutations at low or submicromolar concentrations. Oncrasin-1 drives abnormal aggregation of PKCι in nucleus of sensitive cells but not in resistant cells. |
||
| S0023新 |
K-Ras-IN-1K-Ras-IN-1 inhibits K-Ras by binding to K-Ras in a hydrophobic pocket that is occupied by Tyr-71 in the apo-Ras crystal structure. |
||
| S8955新 |
Sotorasib (AMG510) racemateSotorasib (AMG510) racemate is a racemic of AMG-510 which is a potent KRAS G12C covalent inhibitor with potential antineoplastic activity. |
||
| S8884新 |
MRTX849MRTX849 is a potent, selective, and covalent KRAS G12C inhibitor that exhibits favorable drug-like properties, selectively modifies mutant cysteine 12 in GDP-bound KRAS G12C and inhibits KRAS-dependent signaling. |
||
| S7224 |
DeltarasinDeltarasin is a small molecular inhibitor of KRAS-PDEδ interaction with Kd of 38 nM for binding to purified PDEδ. |
||
| S8826 |
BAY-293BAY-293 selectively inhibits the KRAS-SOS1 interaction with an IC50 of 21 nM. |
||
| S7330 |
6H056H05 is a selective, and allosteric inhibitor of oncogenic K-Ras(G12C). |
||
| S7331 |
K-Ras(G12C) inhibitor 12K-Ras(G12C) inhibitor 12 is an allosteric inhibitor of oncogenic K-Ras(G12C). |
-inhibitor-12-S733101W0420171213.gif)
-inhibitor-12-S733101W0420171213.gif)
(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 is H-Ras-cRaf1 interaction inhibitor, exhibiting potent activity to competitively inhibit the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki value of 46 ± 13 μM. |
||
| S7333 |
K-Ras(G12C) inhibitor 6K-Ras(G12C) inhibitor 6 is an allosteric, and selective inhibitor of oncogenic K-Ras(G12C). |
||
| S7607 |
BQU57BQU57, a derivative of RBC8, is a selective GTPase Ral inhibitor relative to the GTPases Ras and RhoA. |
||
| S8707 |
ARS-1620ARS-1620 is a potent, orally bioavailable covalent inhibitor of KRASG12C) and could achieve rapid and sustained in vivo target occupancy to induce tumor regression. |
||
| S6527 |
Kobe2602Kobe2602 is a selective Ras inhibitor that blocks H-Ras GTP binding to c-Raf-1 (Ki = 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. |
||
| S8499 |
KRpep-2dKRpep-2d is a K-Ras(G12D) selective inhibitory cyclic peptide with selectivity against wild-type (WT) K-Ras and the K-Ras(G12C) mutant. The IC50 value is 1.6 nM. |
||
| S8156 |
ARS-853 (ARS853)ARS-853 is a selective, covalent KRAS(G12C) inhibitor that inhibits mutant KRAS-driven signaling by binding to the GDP-bound oncoprotein and preventing activation. ARS-853 also induces apoptosis. |
||
| S5244 |
Zoledronic acid monohydrateZoledronic acid (Zoledronate, CGP-4244) monohydrate, a nitrogen-containing bisphosphonate, is a potent osteoclast inhibitor which induces apoptosis in osteoclasts by inhibiting enzymes of the mevalonate pathway and preventing the isoprenylation of small GTP-binding proteins such as Ras and Rho. |
| 製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|
| S0458新 |
KY1220KY1220 is a small molecule that destabilizes both β-catenin and Ras, via targeting the Wnt/β-catenin pathway with IC50 of 2.1 μM in HEK293 reporter cells. |
