Mdm2

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)
DMSO アルコール
S2678 NSC 207895 <1 mg/mL 0.4 mg/mL <1 mg/mL
S8059 Nutlin-3a <1 mg/mL 100 mg/mL '100 mg/mL
S7030 RG-7112 <1 mg/mL 100 mg/mL 100 mg/mL
S7875 NVP-CGM097 <1 mg/mL 65 mg/mL ''65 mg/mL
S8403 MX69 <1 mg/mL 95 mg/mL 41 mg/mL
S8606 HDM201 (Siremadlin) <1 mg/mL 100 mg/mL 3 mg/mL
S7205 Idasanutlin (RG-7388) <1 mg/mL 100 mg/mL 8 mg/mL
S0167 RO8994 <1 mg/mL 100 mg/mL ''13 mg/mL
S3604 Triptolide (PG490) <1 mg/mL 72 mg/mL <1 mg/mL
S0901 SP141 <1 mg/mL 65 mg/mL 65 mg/mL
S2341 (-)-Parthenolide <1 mg/mL 49 mg/mL 49 mg/mL
S1061 Nutlin-3 <1 mg/mL 100 mg/mL 30 mg/mL
S8065 Nutlin-3b <1 mg/mL 100 mg/mL 100 mg/mL
S7649 MI-773 (SAR405838) <1 mg/mL 100 mg/mL 31 mg/mL
S7489 YH239-EE <1 mg/mL 100 mg/mL 18 mg/mL

亜型選択性的な製品

Mdm2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
S2678

NSC 207895

NSC 207895 (XI-006) suppresses MDMX with IC50 of 2.5 μM, leading to enhanced p53 stabilization/activation and DNA damage, and also regulates MDM2, an E3 ligase.

S8059

Nutlin-3a

Nutlin-3a ((-)-Nutlin-3), the active enantiomer of Nutlin-3, inhibits the p53/MDM2 interaction with IC50 of 90 nM in a cell-free assay. Nutlin-3a induces autophagy and apoptosis in a p53-dependent manner.

S7030

RG-7112

RG7112 (RO5045337) is an orally bioavailable and selective p53-MDM2 inhibitor with HTRF IC50 of 18 nM.

S7875

NVP-CGM097

NVP-CGM097 is a highly potent and selective MDM2 inhibitor. It binds to the p53 binding-site of the Mdm2 protein, disrupting the interaction between both proteins, leading to an activation of the p53 pathway.

S8403

MX69

MX69 is a MDM2/XIAP inhibitor, used for cancer treatment.

S8606

HDM201 (Siremadlin)

HDM201 (Siremadlin, NVP-HDM201) is a novel, highly potent and selective inhibitor of the p53-Mdm2 interaction with affinity constant for Mdm2 in the picomolar range and a selectivity ratio greater than 10000-fold vs Mdm4.

S7205

Idasanutlin (RG-7388)

Idasanutlin (RG-7388) is a potent and selective p53-MDM2 inhibitor with IC50 of 6 nM showing improved in vitro binding as well as cellular potency/selectivity.

S0167

RO8994

RO8994 is a potent and selective small-molecule MDM2 inhibitor with IC50 values of 5 nM in HTRF binding assays and 20 nM in MTT proliferation assays, respectively.

S3604

Triptolide (PG490)

Triptolide (PG490, NSC 163062) is a diterpene triepoxide, immunosuppresive agent extracted from the Chinese herb Tripterygium wilfordii. It functions as a NF-κB inhibitor with dual actions by disruption of p65/CBP interaction and by reduction of p65 protein. Triptolide (PG490) abrogates the transactivation function of heat shock transcription factor 1 (HSF1). Triptolide inhibits MDM2 and induces apoptosis through a p53-independent pathway.

S0901

SP141

SP141 is a new class of MDM2 inhibitor that promotes MDM2 auto-ubiquitination and degradation, and reduces levels of MDM2 in pancreatic cancer cell lines, as well as their proliferation and ability to form tumors in nude mice. SP141 inhibits human pancreatic cancer cell growth with IC50 values of less than 0.5 μM (0.38–0.50 μM) in a p53-independent manner.

S2341

(-)-Parthenolide

(-)-Parthenolide, an inhibitor of the Nuclear Factor-κB Pathway, specifically depletes HDAC1 protein without affecting other class I/II HDACs; Also promotes the ubiquitination of MDM2 and activates p53 cellular functions.

S1061

Nutlin-3

Nutlin-3 is a potent and selective Mdm2 (RING finger-dependent ubiquitin protein ligase for itself and p53) antagonist with IC50 of 90 nM in a cell-free assay; stabilizes p73 in p53-deficient cells.

S8065

Nutlin-3b

Nutlin-3b ((+)-Nutlin-3) is a p53/MDM2 antagonist or inhibitor with IC50 value of 13.6 μM, 150-fold less potent (+)-enantiomer of Nutlin-3 as in comparison with opposite (-)-enantiomer Nutlin-3a.

S7649

MI-773 (SAR405838)

MI-773 (SAR405838) is an orally available MDM2 antagonist with Ki of 0.88 nM. Phase 1.

S7489

YH239-EE

YH239-EE, the ethyl ester of YH239, is a potent p53-MDM2 antagonist and an apoptosis inducer.

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
S2678

NSC 207895

NSC 207895 (XI-006) suppresses MDMX with IC50 of 2.5 μM, leading to enhanced p53 stabilization/activation and DNA damage, and also regulates MDM2, an E3 ligase.

S8059

Nutlin-3a

Nutlin-3a ((-)-Nutlin-3), the active enantiomer of Nutlin-3, inhibits the p53/MDM2 interaction with IC50 of 90 nM in a cell-free assay. Nutlin-3a induces autophagy and apoptosis in a p53-dependent manner.

S7030

RG-7112

RG7112 (RO5045337) is an orally bioavailable and selective p53-MDM2 inhibitor with HTRF IC50 of 18 nM.

S7875

NVP-CGM097

NVP-CGM097 is a highly potent and selective MDM2 inhibitor. It binds to the p53 binding-site of the Mdm2 protein, disrupting the interaction between both proteins, leading to an activation of the p53 pathway.

S8403

MX69

MX69 is a MDM2/XIAP inhibitor, used for cancer treatment.

S8606

HDM201 (Siremadlin)

HDM201 (Siremadlin, NVP-HDM201) is a novel, highly potent and selective inhibitor of the p53-Mdm2 interaction with affinity constant for Mdm2 in the picomolar range and a selectivity ratio greater than 10000-fold vs Mdm4.

S7205

Idasanutlin (RG-7388)

Idasanutlin (RG-7388) is a potent and selective p53-MDM2 inhibitor with IC50 of 6 nM showing improved in vitro binding as well as cellular potency/selectivity.

S0167

RO8994

RO8994 is a potent and selective small-molecule MDM2 inhibitor with IC50 values of 5 nM in HTRF binding assays and 20 nM in MTT proliferation assays, respectively.

S3604

Triptolide (PG490)

Triptolide (PG490, NSC 163062) is a diterpene triepoxide, immunosuppresive agent extracted from the Chinese herb Tripterygium wilfordii. It functions as a NF-κB inhibitor with dual actions by disruption of p65/CBP interaction and by reduction of p65 protein. Triptolide (PG490) abrogates the transactivation function of heat shock transcription factor 1 (HSF1). Triptolide inhibits MDM2 and induces apoptosis through a p53-independent pathway.

S0901

SP141

SP141 is a new class of MDM2 inhibitor that promotes MDM2 auto-ubiquitination and degradation, and reduces levels of MDM2 in pancreatic cancer cell lines, as well as their proliferation and ability to form tumors in nude mice. SP141 inhibits human pancreatic cancer cell growth with IC50 values of less than 0.5 μM (0.38–0.50 μM) in a p53-independent manner.

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
S2341

(-)-Parthenolide

(-)-Parthenolide, an inhibitor of the Nuclear Factor-κB Pathway, specifically depletes HDAC1 protein without affecting other class I/II HDACs; Also promotes the ubiquitination of MDM2 and activates p53 cellular functions.

2021, 17(11):e1009890

2020, 10(22):9923-9936

2020, 295(11):3576-3589

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
S1061

Nutlin-3

Nutlin-3 is a potent and selective Mdm2 (RING finger-dependent ubiquitin protein ligase for itself and p53) antagonist with IC50 of 90 nM in a cell-free assay; stabilizes p73 in p53-deficient cells.

2022, 10.1038/s41587-021-01172-3

2022, 41(1):79

2022, 12(1):20

S8065

Nutlin-3b

Nutlin-3b ((+)-Nutlin-3) is a p53/MDM2 antagonist or inhibitor with IC50 value of 13.6 μM, 150-fold less potent (+)-enantiomer of Nutlin-3 as in comparison with opposite (-)-enantiomer Nutlin-3a.

2015, 36(24):3101-4

S7649

MI-773 (SAR405838)

MI-773 (SAR405838) is an orally available MDM2 antagonist with Ki of 0.88 nM. Phase 1.

2021, 36(5):109482

2021, 5(1):96

2020, 12(8):E2157

S7489

YH239-EE

YH239-EE, the ethyl ester of YH239, is a potent p53-MDM2 antagonist and an apoptosis inducer.

2018, 23(4):544-556