2. Protein Tyrosine Kinase/RTK Apoptosis
  3. BMX Kinase Apoptosis
  4. IHMT-15137

IHMT-15137 是一种 BMX 抑制剂，其 IC50 为 26.97 nM。IHMT-15137 可与 ATP 结合口袋内的 BMX Cys496 共价结合，抑制 BMX 在 Tyr566 位点的磷酸化，并破坏 BMX-ERK1/2-Cyclin D1/CDK4/6-E2F1 信号轴。IHMT-15137 可通过降低 Ser332/337 位点的磷酸化水平、增加泛素化作用以及经泛素-蛋白酶体途径降解的方式，降低 E2F1 蛋白的稳定性。IHMT-15137 可诱导细胞周期阻滞、细胞凋亡 (apoptosis) 和 DNA 损伤，并抑制细胞迁移与侵袭。IHMT-15137 可用于小细胞肺癌的研究。

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IHMT-15137

IHMT-15137 Chemical Structure

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IHMT-15137 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

IHMT-15137 is a BMX inhibitor with an IC50 of 26.97 nM. IHMT-15137 covalently binds to BMX Cys496 within the ATP-binding pocket, inhibits BMX phosphorylation at Tyr566, and disrupts the BMX-ERK1/2-Cyclin D1/CDK4/6-E2F1 signaling axis. IHMT-15137 reduces E2F1 protein stability via decreased Ser332/337 phosphorylation, increased ubiquitination, and ubiquitin-proteasome pathway degradation. IHMT-15137 induces cell cycle arrest, apoptosis, DNA damage, and suppresses cell migration and invasion. IHMT-15137 can be used for the research of small cell lung cancer[1].

体外研究
(In Vitro)

IHMT-15137 (3 μM；24-168 小时) 与 Cisplatin (HY-17394) (5-30 μM) 协同作用，可降低小细胞肺癌 (SCLC) 患者来源细胞 C23084 和 LUC22009 的活力，诱导 S 期细胞周期阻滞，抑制增殖，促进凋亡，增加 DNA 损伤，并破坏 BMX-ERK1/2-Cyclin D1-E2F1 信号轴[1]。
IHMT-15137 可增强 Cisplatin+Etoposide (HY-13629) 在 SCLC 患者来源细胞 C23084 和 LUC22009 中的细胞毒性与抗增殖作用[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

IHMT-15137 相关抗体:

Cell Cycle Analysis[1]

Cell Line: SCLC patient-derived cells C23084 and LUC22009
Concentration: 3 μM; 3 μM plus 5 μM Cisplatin
Incubation Time: 48 h
Result: Induced S-phase cell cycle arrest.

Cell Proliferation Assay[1]

Cell Line: SCLC patient-derived cells C23084 and LUC22009
Concentration: 3 μM; 3 μM plus 5 μM Cisplatin
Incubation Time: 14 days
Result: Suppressed cell proliferation compared with DMSO group.

Western Blot Analysis[1]

Cell Line: SCLC patient-derived cells C23084 and LUC22009
Concentration: 10 μM; 10 μM plus 30 μM Cisplatin
Incubation Time: 24 h
Result: Enhanced apoptosis (cleaved PARP and cleaved caspase-3) and significantly increased DNA damage (γ-H2AX) in the treated groups compared with the monotherapies.

Western Blot Analysis[1]

Cell Line: SCLC patient-derived cells C23084 and LUC22009
Concentration: 3 μM; 3 μM plus 30 μM Cisplatin
Incubation Time: 24 h
Result: Potentiated the effects of Cisplatin by modulating the ERK1/2-Cyclin D1/CDK4/6 signaling axis and promoting the degradation of E2F1.
体内研究
(In Vivo)

IHMT-15137 (100 mg/kg；腹腔注射) 联合 Cisplatin 和 Etoposide 可在 H69AR 小细胞肺癌 (SCLC) 异种移植模型中诱导 60.1% 的肿瘤生长抑制，增强细胞凋亡并抑制细胞增殖，且无显著毒性[1]。
IHMT-15137 (100 mg/kg；腹腔注射) 联合 Cisplatin 与 Etoposide 可在 H446DDPR 小细胞肺癌异种移植物中诱导 69.0%的肿瘤生长抑制，增强细胞凋亡并抑制细胞增殖，且无显著毒性[1]。
IHMT-15137 (100 mg/kg；腹腔注射) 联合 Cisplatin 与 Etoposide 可在 SCLC 患者来源异种移植物中诱导 59.8%的肿瘤生长抑制，增强细胞凋亡并抑制细胞增殖，且无显著毒性[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: NCG mice (female, 6 weeks old, subcutaneous xenograft model implanted with chemoresistant H69AR cells)[1]
Dosage: 100 mg/kg; 100 mg/kg plus 2 mg/kg Cisplatin plus 16 mg/kg Etoposide
Administration: i.p.
Result: Achieved 60.1% tumor growth inhibition (TGI).
Reduced final mean tumor weight to 0.96 g compared to vehicle control (2.46 g).
Suppressed chemotherapy-induced increases in tumor tissue levels of p-BMX (Tyr566), p-ERK1/2 (Thr202/Tyr204), Cyclin D1, p-E2F1 (Ser332), and p-E2F1 (Ser337).
Increased tumor apoptosis (TUNEL-positive cells) compared to monotherapies.
Reduced tumor proliferation (Ki-67-positive cells) compared to monotherapies.
Caused no significant body weight loss.
Animal Model: NCG mice (female, 6 weeks old, subcutaneous xenograft model implanted with chemoresistant H446DDPR cells)[1]
Dosage: 100 mg/kg; 100 mg/kg plus 2 mg/kg Cisplatin plus 16 mg/kg Etoposide
Administration: i.p.
Result: Achieved 69.0% tumor growth inhibition (TGI).
Reduced final mean tumor weight to 0.78 g compared to vehicle control (2.52 g).
Suppressed chemotherapy-induced increases in tumor tissue levels of p-BMX (Tyr566), p-ERK1/2 (Thr202/Tyr204), Cyclin D1, p-E2F1 (Ser332), and p-E2F1 (Ser337).
Increased tumor apoptosis (TUNEL-positive cells) compared to monotherapies.
Reduced tumor proliferation (Ki-67-positive cells) compared to monotherapies.
Caused no significant body weight loss.
Animal Model: NCG mice (female, 6 weeks old, subcutaneous patient-derived xenograft model implanted with PDC C23084 cells)[1]
Dosage: 100 mg/kg; 100 mg/kg plus 2 mg/kg Cisplatin plus 16 mg/kg Etoposide
Administration: i.p.
Result: Achieved 59.8% tumor growth inhibition (TGI).
Reduced final mean tumor weight to 0.39 g compared to vehicle control (0.97 g).
Suppressed chemotherapy-induced increases in tumor tissue levels of p-BMX (Tyr566), p-ERK1/2 (Thr202/Tyr204), Cyclin D1, p-E2F1 (Ser332), and p-E2F1 (Ser337).
Increased levels of cleaved PARP and cleaved caspase-3 (apoptosis markers).
Increased tumor apoptosis (TUNEL-positive cells) compared to monotherapies.
Reduced tumor proliferation (Ki-67-positive cells) compared to monotherapies.
Caused no significant body weight loss.
分子量

446.43

Formula

C21H21F3N6O2
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.
纯度 & 产品资料
参考文献

IHMT-15137 相关分类

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  • 稀释计算器

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

IHMT-15137IHMT15137IHMT 15137BMX KinaseApoptosisCyclin D1E2F1Tyr566small cell lung cancerBMXCys496SCLC patient-derived cellsCDK4/6H69AR SCLC xenograftsERK1/2Inhibitorinhibitorinhibit

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