MS21, a novel degrader of AKT, selectively inhibits the growth of PI3K/PTEN pathway-mutant cancers with wild-type KRAS and BRAF.
分子量
1107.84
Formula
C58H79ClN12O6S
CAS 号
2376137-05-0
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]. Xu J, et al. AKT Degradation Selectively Inhibits the Growth of PI3K/PTEN Pathway-Mutant Cancers with Wild-Type KRAS and BRAF by Destabilizing Aurora Kinase B. Cancer Discov. 2021 Jul 23.
MS21, a novel degrader of AKT, selectively inhibits the growth of PI3K/PTEN pathway-mutant cancers with wild-type KRAS and BRAF.
分子量
1107.84
Formula
C58H79ClN12O6S
CAS 号
2376137-05-0
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]. Xu J, et al. AKT Degradation Selectively Inhibits the Growth of PI3K/PTEN Pathway-Mutant Cancers with Wild-Type KRAS and BRAF by Destabilizing Aurora Kinase B. Cancer Discov. 2021 Jul 23.
MS21, a novel degrader of AKT, selectively inhibits the growth of PI3K/PTEN pathway-mutant cancers with wild-type KRAS and BRAF.
分子量
1107.84
Formula
C58H79ClN12O6S
CAS 号
2376137-05-0
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]. Xu J, et al. AKT Degradation Selectively Inhibits the Growth of PI3K/PTEN Pathway-Mutant Cancers with Wild-Type KRAS and BRAF by Destabilizing Aurora Kinase B. Cancer Discov. 2021 Jul 23.
MS-PPOH is a potent and selective cytochrome P450 (CYP) epoxygenase inhibitor[1]. MS-PPOH inhibits CYP2C8 and CYP2C9 with IC50s of 15 and 11 µM, respectively[2].
体外研究 (In Vitro)
MS-PPOH blocks cellular EET synthesis. MS-PPOH inhibits tonic (basal) cell invasion and migration and reduces the 11,12-EET (1.0 μM)-induced cell motility[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay[1]
Cell Line:
PC-3 cells
Concentration:
2.0 and 10.0 μM
Incubation Time:
24 hours
Result:
Inhibited tonic (basal) cell invasion and migration.
体内研究 (In Vivo)
MS-PPOH (20 mg/kg/day, i.v.) for 6 days significantly reduced renal levels of epoxyeicosatrienoic acids (EETs) in Dahl salt-resistant rats on 2% NaCl drinking solution[3].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Six-week-old male stroke-prone spontaneously hypertensive rats (SHRSP)[3]
Dosage:
20 mg/kg/day
Administration:
Intravenously
Result:
Treatment had negligible effects on systolic blood pressure (SBP) in saline-drinking SHRSP after 1 week, 160 vs. 167 mmHg, or 2 weeks of treatment, 171 vs. 175 mmHg, for vehicle vs. MS-PPOH, respectively.
分子量
323.41
Formula
C16H21NO4S
CAS 号
206052-02-0
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]. Kasem Nithipatikom, et al. Inhibition of carcinoma cell motility by epoxyeicosatrienoic acid (EET) antagonists. Cancer Sci. 2010 Dec;101(12):2629-36.
[2]. Jun Yang, et al. Cytochrome P450 2C24: Expression, Tissue Distribution, High-Throughput Assay, and Pharmacological Inhibition. Acta Pharm Sin B. 2012 Apr;2(2):137-145.
[3]. Jing Li, et al. Pharmacological manipulation of arachidonic acid-epoxygenase results in divergent effects on renal damage. Front Pharmacol. 2014 Aug 15;5:187.
MS-PPOH is a potent and selective cytochrome P450 (CYP) epoxygenase inhibitor[1]. MS-PPOH inhibits CYP2C8 and CYP2C9 with IC50s of 15 and 11 µM, respectively[2].
体外研究 (In Vitro)
MS-PPOH blocks cellular EET synthesis. MS-PPOH inhibits tonic (basal) cell invasion and migration and reduces the 11,12-EET (1.0 μM)-induced cell motility[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay[1]
Cell Line:
PC-3 cells
Concentration:
2.0 and 10.0 μM
Incubation Time:
24 hours
Result:
Inhibited tonic (basal) cell invasion and migration.
体内研究 (In Vivo)
MS-PPOH (20 mg/kg/day, i.v.) for 6 days significantly reduced renal levels of epoxyeicosatrienoic acids (EETs) in Dahl salt-resistant rats on 2% NaCl drinking solution[3].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Six-week-old male stroke-prone spontaneously hypertensive rats (SHRSP)[3]
Dosage:
20 mg/kg/day
Administration:
Intravenously
Result:
Treatment had negligible effects on systolic blood pressure (SBP) in saline-drinking SHRSP after 1 week, 160 vs. 167 mmHg, or 2 weeks of treatment, 171 vs. 175 mmHg, for vehicle vs. MS-PPOH, respectively.
分子量
323.41
Formula
C16H21NO4S
CAS 号
206052-02-0
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]. Kasem Nithipatikom, et al. Inhibition of carcinoma cell motility by epoxyeicosatrienoic acid (EET) antagonists. Cancer Sci. 2010 Dec;101(12):2629-36.
[2]. Jun Yang, et al. Cytochrome P450 2C24: Expression, Tissue Distribution, High-Throughput Assay, and Pharmacological Inhibition. Acta Pharm Sin B. 2012 Apr;2(2):137-145.
[3]. Jing Li, et al. Pharmacological manipulation of arachidonic acid-epoxygenase results in divergent effects on renal damage. Front Pharmacol. 2014 Aug 15;5:187.
MS-PPOH is a potent and selective cytochrome P450 (CYP) epoxygenase inhibitor[1]. MS-PPOH inhibits CYP2C8 and CYP2C9 with IC50s of 15 and 11 µM, respectively[2].
体外研究 (In Vitro)
MS-PPOH blocks cellular EET synthesis. MS-PPOH inhibits tonic (basal) cell invasion and migration and reduces the 11,12-EET (1.0 μM)-induced cell motility[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 Viability Assay[1]
Cell Line:
PC-3 cells
Concentration:
2.0 and 10.0 μM
Incubation Time:
24 hours
Result:
Inhibited tonic (basal) cell invasion and migration.
体内研究 (In Vivo)
MS-PPOH (20 mg/kg/day, i.v.) for 6 days significantly reduced renal levels of epoxyeicosatrienoic acids (EETs) in Dahl salt-resistant rats on 2% NaCl drinking solution[3].
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:
Six-week-old male stroke-prone spontaneously hypertensive rats (SHRSP)[3]
Dosage:
20 mg/kg/day
Administration:
Intravenously
Result:
Treatment had negligible effects on systolic blood pressure (SBP) in saline-drinking SHRSP after 1 week, 160 vs. 167 mmHg, or 2 weeks of treatment, 171 vs. 175 mmHg, for vehicle vs. MS-PPOH, respectively.
分子量
323.41
Formula
C16H21NO4S
CAS 号
206052-02-0
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]. Kasem Nithipatikom, et al. Inhibition of carcinoma cell motility by epoxyeicosatrienoic acid (EET) antagonists. Cancer Sci. 2010 Dec;101(12):2629-36.
[2]. Jun Yang, et al. Cytochrome P450 2C24: Expression, Tissue Distribution, High-Throughput Assay, and Pharmacological Inhibition. Acta Pharm Sin B. 2012 Apr;2(2):137-145.
[3]. Jing Li, et al. Pharmacological manipulation of arachidonic acid-epoxygenase results in divergent effects on renal damage. Front Pharmacol. 2014 Aug 15;5:187.
MS33 is a potent WDR5 degrader, with Kds of 870 nM and 120 nM for VCB and WDR5, respectively. MS33 induces WDR5 degradation in an E3 ligase VHL, and proteasome-dependent manner. MS33 can be used for the research of acute myeloid leukemia[1][2][3].
IC50 & Target[1]
VHL
WDR5
120 nM (Kd)
VCB
870 nM (Kd)
体外研究 (In Vitro)
MS33 (0.05-5 μM; 18 h) induces WDR5 degradation in a concentration-dependent manner in MV4;11 cells[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:
MV4;11 cells
Concentration:
0.05, 0.1, 0.5, 1, 5 μM
Incubation Time:
1, 2, 4, 8, 16, 24 hours
Result:
Concentration- and time-dependently induced WDR5 degradation. The DC50 of MS33 was 260 nM, and the maximum degradation of 71%.
分子量
1208.48
Formula
C64H84F3N11O7S
CAS 号
2407449-11-8
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]. Yu X, et, al. A selective WDR5 degrader inhibits acute myeloid leukemia in patient-derived mouse models. Sci Transl Med. 2021 Sep 29;13(613):eabj1578.
MS33 is a potent WDR5 degrader, with Kds of 870 nM and 120 nM for VCB and WDR5, respectively. MS33 induces WDR5 degradation in an E3 ligase VHL, and proteasome-dependent manner. MS33 can be used for the research of acute myeloid leukemia[1][2][3].
IC50 & Target[1]
VHL
WDR5
120 nM (Kd)
VCB
870 nM (Kd)
体外研究 (In Vitro)
MS33 (0.05-5 μM; 18 h) induces WDR5 degradation in a concentration-dependent manner in MV4;11 cells[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:
MV4;11 cells
Concentration:
0.05, 0.1, 0.5, 1, 5 μM
Incubation Time:
1, 2, 4, 8, 16, 24 hours
Result:
Concentration- and time-dependently induced WDR5 degradation. The DC50 of MS33 was 260 nM, and the maximum degradation of 71%.
分子量
1208.48
Formula
C64H84F3N11O7S
CAS 号
2407449-11-8
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]. Yu X, et, al. A selective WDR5 degrader inhibits acute myeloid leukemia in patient-derived mouse models. Sci Transl Med. 2021 Sep 29;13(613):eabj1578.
MS33 is a potent WDR5 degrader, with Kds of 870 nM and 120 nM for VCB and WDR5, respectively. MS33 induces WDR5 degradation in an E3 ligase VHL, and proteasome-dependent manner. MS33 can be used for the research of acute myeloid leukemia[1][2][3].
IC50 & Target[1]
VHL
WDR5
120 nM (Kd)
VCB
870 nM (Kd)
体外研究 (In Vitro)
MS33 (0.05-5 μM; 18 h) induces WDR5 degradation in a concentration-dependent manner in MV4;11 cells[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.
Western Blot Analysis[1]
Cell Line:
MV4;11 cells
Concentration:
0.05, 0.1, 0.5, 1, 5 μM
Incubation Time:
1, 2, 4, 8, 16, 24 hours
Result:
Concentration- and time-dependently induced WDR5 degradation. The DC50 of MS33 was 260 nM, and the maximum degradation of 71%.
分子量
1208.48
Formula
C64H84F3N11O7S
CAS 号
2407449-11-8
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]. Yu X, et, al. A selective WDR5 degrader inhibits acute myeloid leukemia in patient-derived mouse models. Sci Transl Med. 2021 Sep 29;13(613):eabj1578.
MS37452 is a potent inhibitor of CBX7 chromodomain binding to H3K27me3, with a Kd of 27.7 μM. MS37452 can derepress transcription of polycomb repressive complex target gene p16/CDKN2A by displacing CBX7 binding to the INK4A/ARF locus in prostate cancer cells[1].
IC50 & Target
CBX7[1]
体外研究 (In Vitro)
MS37452 (125-500 μM; 12 hours) significantly increases INK4A/ARF transcript levels up to 25% and 60% for 250 μM and 500 μM, respectively, as compared to the DMSO control[1]. MS37452 (250 μM; 2 hours) treats human PC3 prostate cancer cells for 2 hours reducing CBX7 occupancy across the INK4A/ARF locus[1]. MS37452 (200 µM; 5 days) combined with doxorubicin results in consistently decreased cell viability compared to DMSO treated and single drug treatment[2]. MS37452 (200 µM; 5 days), which is a CBX7 chromodomain inhibitor (CBX7i), in combination with doxorubicin is a novel therapeutic strategy[2].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
RT-PCR[1]
Cell Line:
PC3 cells
Concentration:
125-500 μM
Incubation Time:
12 hours
Result:
Up-regulated INK4A/ARF expression up to 25% and 60% for 250 μM and 500 μM, respectively.
Identified several combinations that resulted in consistently decreased cell viability compared to DMSO treated and single drug treatment: SAHA/TMZ and MS37452/doxorubicin.
分子量
398.45
Formula
C22H26N2O5
CAS 号
423748-02-1
运输条件
Room temperature in continental US; may vary elsewhere.
MS37452 is a potent inhibitor of CBX7 chromodomain binding to H3K27me3, with a Kd of 27.7 μM. MS37452 can derepress transcription of polycomb repressive complex target gene p16/CDKN2A by displacing CBX7 binding to the INK4A/ARF locus in prostate cancer cells[1].
IC50 & Target
CBX7[1]
体外研究 (In Vitro)
MS37452 (125-500 μM; 12 hours) significantly increases INK4A/ARF transcript levels up to 25% and 60% for 250 μM and 500 μM, respectively, as compared to the DMSO control[1]. MS37452 (250 μM; 2 hours) treats human PC3 prostate cancer cells for 2 hours reducing CBX7 occupancy across the INK4A/ARF locus[1]. MS37452 (200 µM; 5 days) combined with doxorubicin results in consistently decreased cell viability compared to DMSO treated and single drug treatment[2]. MS37452 (200 µM; 5 days), which is a CBX7 chromodomain inhibitor (CBX7i), in combination with doxorubicin is a novel therapeutic strategy[2].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
RT-PCR[1]
Cell Line:
PC3 cells
Concentration:
125-500 μM
Incubation Time:
12 hours
Result:
Up-regulated INK4A/ARF expression up to 25% and 60% for 250 μM and 500 μM, respectively.
Identified several combinations that resulted in consistently decreased cell viability compared to DMSO treated and single drug treatment: SAHA/TMZ and MS37452/doxorubicin.
分子量
398.45
Formula
C22H26N2O5
CAS 号
423748-02-1
运输条件
Room temperature in continental US; may vary elsewhere.
MS37452 is a potent inhibitor of CBX7 chromodomain binding to H3K27me3, with a Kd of 27.7 μM. MS37452 can derepress transcription of polycomb repressive complex target gene p16/CDKN2A by displacing CBX7 binding to the INK4A/ARF locus in prostate cancer cells[1].
IC50 & Target
CBX7[1]
体外研究 (In Vitro)
MS37452 (125-500 μM; 12 hours) significantly increases INK4A/ARF transcript levels up to 25% and 60% for 250 μM and 500 μM, respectively, as compared to the DMSO control[1]. MS37452 (250 μM; 2 hours) treats human PC3 prostate cancer cells for 2 hours reducing CBX7 occupancy across the INK4A/ARF locus[1]. MS37452 (200 µM; 5 days) combined with doxorubicin results in consistently decreased cell viability compared to DMSO treated and single drug treatment[2]. MS37452 (200 µM; 5 days), which is a CBX7 chromodomain inhibitor (CBX7i), in combination with doxorubicin is a novel therapeutic strategy[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.
RT-PCR[1]
Cell Line:
PC3 cells
Concentration:
125-500 μM
Incubation Time:
12 hours
Result:
Up-regulated INK4A/ARF expression up to 25% and 60% for 250 μM and 500 μM, respectively.
Identified several combinations that resulted in consistently decreased cell viability compared to DMSO treated and single drug treatment: SAHA/TMZ and MS37452/doxorubicin.
分子量
398.45
Formula
C22H26N2O5
CAS 号
423748-02-1
运输条件
Room temperature in continental US; may vary elsewhere.
MS-PEG4-t-butyl ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
IC50 & Target
PEGs
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].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
356.43
Formula
C14H28O8S
CAS 号
1024602-74-1
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]. 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
MS-PEG4-t-butyl ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
IC50 & Target
PEGs
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].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
356.43
Formula
C14H28O8S
CAS 号
1024602-74-1
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]. 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