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 (ZOL 446) | <1 mg/mL | 0.004 mg/mL | ''<1 mg/mL |
| S2797 | Lonafarnib (SCH66336) | <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 | ||
| E0135 | CID-1067700 | <1 mg/mL | 78 mg/mL | '''<1 mg/mL |
| S8959 | BI-2852 | <1 mg/mL | 100 mg/mL | ''''23 mg/mL |
| S8830 | Sotorasib (AMG510) | <1 mg/mL | 100 mg/mL | '100 mg/mL |
| S0023 | K-Ras-IN-1 | <1 mg/mL | 41 mg/mL | '41 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 |
| S6905 | MCP110 | <1 mg/mL | 100 mg/mL | 100 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 |
| S0323 | Antineoplaston A10 | <1 mg/mL | 49 mg/mL | '''<1 mg/mL |
| S5279 | Fendiline hydrochloride | -1 mg/mL | 70 mg/mL | -1 mg/mL |
| S8884 | Adagrasib (MRTX849) | <1 mg/mL | 100 mg/mL | '50 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 |
| S8916 | BI-3406 | <1 mg/mL | 92 mg/mL | ''92 mg/mL |
| S8955 | Sotorasib (AMG510) racemate | <1 mg/mL | 100 mg/mL | 100 mg/mL |
| S8831 | MRTX-1257 | <1 mg/mL | 100 mg/mL | ''30 mg/mL |
| S5244 | Zoledronic acid monohydrate | <1 mg/mL | 0.01 mg/mL | <1 mg/mL |
| S6996 | LC-2 | <1 mg/mL | 100 mg/mL | ''<1 mg/mL |
| S0458 | KY1220 | <1 mg/mL | 63 mg/mL | <1 mg/mL |
亜型選択性的な製品
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 acid (ZOL 446)Zoledronic acid (ZOL 446, ZA, Zoledronate, CGP-4244, GP42446A, Zometa, Zomera, Aclasta, Reclast), 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 |
Lonafarnib (SCH66336)Lonafarnib (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 (Farnesylthiosalicylic acid, FTS) 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. |
||
| E1051新 |
MRTX1133MRTX1133 is a highly selective inhibitor of mutant KRAS G12D and can reversibly binds to the activated and inactivated KRAS G12D mutants and inhibit their activity. The specificity of MRTX1133 to KRAS G12D is more than 1000 times that of wild-type KRAS. |
||
| E0135新 |
CID-1067700CID-1067700 (ML282) is a pan-GTPase inhibitor with a ki of 12.89 nM for Rab7wt. |
||
| S8959新 |
BI-2852BI-2852 is a potent inhibitor of KRAS that binds with nanomolar affinity to a pocket between switch I and II on RAS. BI-2852 blocks all GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in the low micromolar range in KRAS mutant cells. |
||
| S8830 |
Sotorasib (AMG510)Sotorasib (AMG510) is a potent KRAS G12C covalent inhibitor with potential antineoplastic activity.This AMG510 is a chiral compound. |
||
| S0023 |
K-Ras-IN-1K-Ras-IN-1 (MDK-3017) inhibits K-Ras by binding to K-Ras in a hydrophobic pocket that is occupied by Tyr-71 in the apo-Ras crystal structure. |
||
| 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. |
||
| S6905 |
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. |
||
| 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). |
||
| S0323 |
Antineoplaston A10Antineoplaston A10 is a naturally occurring substance in the human body that that can be potentially used for the treatment of glioma, lymphoma, astrocytoma and breast cancer. The main ingredient active of antineoplaston A10 (Phenylacetylglutamine, PG) inhibits RAS and promotes apoptosis. |
||
| 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) 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. |
||
| 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. |
||
| S8916 |
BI-3406BI-3406 (compound I-13) is a potent, selective and orally active inhibitor of the interaction between KRAS and Son of Sevenless 1 (SOS1) with IC50 of 5 nM. BI-3406 reduces the formation of GTP-loaded KRAS, and inhibits MAPK pathway signaling. BI-3406 exhibits anti-tumor activities. |
||
| S8955 |
Sotorasib (AMG510) racemateSotorasib (AMG510) racemate is a racemic of AMG-510 which is a potent KRAS G12C covalent inhibitor with potential antineoplastic activity. |
||
| S8831 |
MRTX-1257MRTX-1257 is a potent, selective, irreversible, covalent and orally active inhibitor of KRAS G12C with IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells. |
||
| 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. |
||
| S6996新 |
LC-2LC-2 is a first PROTAC capable of degrading endogenous KRASG12C with DC50s between 0.25 μM and 0.76 μM. LC-2 covalently binds KRASG12C with a MRTX849 warhead and recruits the E3 ligase VHL, inducing rapid and sustained KRASG12C degradation leading to suppression of MAPK signaling. |
||
| S0458 |
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 acid (ZOL 446)Zoledronic acid (ZOL 446, ZA, Zoledronate, CGP-4244, GP42446A, Zometa, Zomera, Aclasta, Reclast), 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 |
Lonafarnib (SCH66336)Lonafarnib (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 (Farnesylthiosalicylic acid, FTS) 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. |
||
| E1051新 |
MRTX1133MRTX1133 is a highly selective inhibitor of mutant KRAS G12D and can reversibly binds to the activated and inactivated KRAS G12D mutants and inhibit their activity. The specificity of MRTX1133 to KRAS G12D is more than 1000 times that of wild-type KRAS. |
||
| E0135新 |
CID-1067700CID-1067700 (ML282) is a pan-GTPase inhibitor with a ki of 12.89 nM for Rab7wt. |
||
| S8959新 |
BI-2852BI-2852 is a potent inhibitor of KRAS that binds with nanomolar affinity to a pocket between switch I and II on RAS. BI-2852 blocks all GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in the low micromolar range in KRAS mutant cells. |
||
| S8830 |
Sotorasib (AMG510)Sotorasib (AMG510) is a potent KRAS G12C covalent inhibitor with potential antineoplastic activity.This AMG510 is a chiral compound. |
||
| S0023 |
K-Ras-IN-1K-Ras-IN-1 (MDK-3017) inhibits K-Ras by binding to K-Ras in a hydrophobic pocket that is occupied by Tyr-71 in the apo-Ras crystal structure. |
||
| 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. |
||
| S6905 |
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. |
||
| 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). |
||
| S0323 |
Antineoplaston A10Antineoplaston A10 is a naturally occurring substance in the human body that that can be potentially used for the treatment of glioma, lymphoma, astrocytoma and breast cancer. The main ingredient active of antineoplaston A10 (Phenylacetylglutamine, PG) inhibits RAS and promotes apoptosis. |
||
| 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) 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. |
||
| 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. |
||
| S8916 |
BI-3406BI-3406 (compound I-13) is a potent, selective and orally active inhibitor of the interaction between KRAS and Son of Sevenless 1 (SOS1) with IC50 of 5 nM. BI-3406 reduces the formation of GTP-loaded KRAS, and inhibits MAPK pathway signaling. BI-3406 exhibits anti-tumor activities. |
||
| S8955 |
Sotorasib (AMG510) racemateSotorasib (AMG510) racemate is a racemic of AMG-510 which is a potent KRAS G12C covalent inhibitor with potential antineoplastic activity. |
||
| S8831 |
MRTX-1257MRTX-1257 is a potent, selective, irreversible, covalent and orally active inhibitor of KRAS G12C with IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells. |
||
| 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 |
|---|---|---|---|
| S6996新 |
LC-2LC-2 is a first PROTAC capable of degrading endogenous KRASG12C with DC50s between 0.25 μM and 0.76 μM. LC-2 covalently binds KRASG12C with a MRTX849 warhead and recruits the E3 ligase VHL, inducing rapid and sustained KRASG12C degradation leading to suppression of MAPK signaling. |
||
| S0458 |
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. |
