2. JAK/STAT Signaling Apoptosis Cell Cycle/DNA Damage Epigenetics NF-κB
  3. Pim Caspase Apoptosis Necroptosis PARP NF-κB
  4. JP-11646

JP-11646 是一种泛 PIM 抑制剂，对 PIM2 的抑制效力显著增强 (IC50 = 0.5 nM)。JP-11646 的作用是可逆的，且不与 ATP 竞争。JP-11646 可导致 PIM1、PIM2 和 PIM3 mRNA。JP-11646 能有效抑制小细胞肺癌 (SCLC) 和肺大细胞神经内分泌癌 (LCNEC) 的细胞活力。JP-11646 可导致 p-4EBP-1 蛋白水平下降，同时增加 caspase-3 的裂解活性。JP-11646 可以诱导细胞凋亡 (apoptosis) 或坏死 (necroptosis)。JP-11646 还会导致 MYC 旁系同源基因的表达降低。JP-11646 可用于研究 SCLC、LCNEC、人类急性白血病 (AML)、多发性骨髓瘤 (MM) 和三阴性乳腺癌 (TNBC)。

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JP-11646

JP-11646 Chemical Structure

CAS No. : 1902983-63-4

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JP-11646 相关抗体

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PIM1 PIM2 PIM3

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

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PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

JP-11646 is a pan-PIM inhibitor with increased potency against PIM2 (IC50 = 0.5 nM). JP11646 is freely reversible and ATP non-competitive. JP-11646 results in a decrease of PIM1, 2, and 3 mRNA. JP-11646 can effectively inhibit cell viability in small cell lung cancer (SCLC) and large cell neuroendocrine carcinomas of the lung (LCNEC). JP-11646 can cause a decrease in p-4EBP-1 protein, increasing the cleavage of caspases while decreasing caspase-3. JP-11646 induces apoptosis or necroptosis in cells. JP-11646 leads to reductions in MYC paralogs. JP-11646 can be used for the study of SCLC, LCNEC, human acute leukemia (AML), multiple myeloma (MM), and triple-negative breast cancer (TNBC)[1][2][3][4][5].

IC50 & Target[1][2][3][4][5]

NF-κB

 

Caspase 3

 

PIM2

0.5 nM (IC50)

体外研究
(In Vitro)

JP11646 (0.005 至 10 μM，72 小时) 以浓度依赖的方式抑制所有测试的癌细胞系的增殖，包括头颈癌 FaDu 细胞系、卵巢癌 SK-OV-3 细胞系、乳腺癌 MDA-MB-231 和 BT549 细胞系、前列腺癌 PC-3 细胞系、肝癌 HepG2 细胞系、胰腺导管腺癌 MIAPaCa-2 和 PANC1 细胞系、结直肠癌 DLD-1 和 HT29 细胞系以及非小细胞肺癌 H1650、H661、H460 和 A549 细胞系[3]。
JP11646 (100-200 nM，24 小时) 选择性地下调 PIM2 蛋白的表达水平，但对 PIM1 和 PIM3 无影响，并诱导 MDA-MB-231 和 BT549 细胞中凋亡标志物 cleaved PARP 的表达[3]。
JP11646 (100-200 nM，48 小时) 显著提高 MDA-MB-231 和 BT549 细胞的凋亡率[3]。
JP11646 (20-200 nM，0-24 小时) 随时间推移逐渐降低 MM1.S 和 U266 细胞中 p4EBP1 (S65) 和 pBAD (S112) 的水平，以及这些蛋白的总水平。此外，抗凋亡因子 MCL1 的强效磷酸化形式 (Ser159/Thr163) 的水平也呈剂量依赖性降低[4]。
JP11646 (0-1 μM，72 小时) 对 MF 特征细胞系 MM1.S 表现出最强的抗增殖作用 (GI50 = 5 nM)[4]。
JP11646 (20-200 nM，24 小时) 可逆转重组 IL-6 (rIL-6) 诱导的 MM1.S 和 U266 细胞中 PIM2 的上调，而 IL-6 本身并不影响 PIM2 mRNA 水平[4]。
JP11646 (10-20 nM，48 小时) 可逆转 CD28 激活或 DC 共培养介导的化学保护作用；CTLA4-Ig 可增强 JP11646 的细胞毒性[4]。
JP11646 (20-200 nM，0-24 小时) 以剂量和时间依赖的方式抑制 MM1.S 和 RPMI8226 细胞中 CD28 诱导的 NF-κB 活性[4]。

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

JP-11646 相关抗体:

Western Blot Analysis[3]

Cell Line: MDA-MB-231 cells, BT549 cells
Concentration: 100 nM, 200 nM
Incubation Time: 24 h
Result: Downregulated the protein expression level of PIM2, but had no effect on PIM1 and PIM3, and induced the expression of the apoptosis marker cleaved PARP in MDA-MB-231 and BT549 cells.

Apoptosis Analysis[3]

Cell Line: MDA-MB-231 cells, BT549 cells
Concentration: 100 nM, 200 nM
Incubation Time: 48 h
Result: Significantly increased the apoptosis rate of MDA-MB-231 and BT549 cells.
体内研究
(In Vivo)

JP11646 (15 mg/kg，腹腔注射，每周两次，24-40 天) 在各种小鼠异种移植肿瘤体内模型中表现出广谱和强效的抗肿瘤活性，且未观察到明显的毒性作用[3]。
JP11646 (10-15 mg/kg，腹腔注射，每周 2 或 3 次，持续 48 天) 在多发性骨髓瘤异种移植小鼠模型中表现出强大的剂量依赖性抗肿瘤活性，并显著延长了荷瘤小鼠的中位生存期[4]。

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

Animal Model: Cell suspensions (1×106 of MDA‑MB‑231, 3×106 of MIAPaCa‑2, 2×106 of PANC‑1, 5×106 of HepG2, 5×106 of A549, 5×106 of HT29 and 5×106 of H1650) in a mixture of 50 µl PBS and 50 µl Matrigel were injected subcutaneously into the CB17 SCID mice (female, 6‑8 weeks‑old, weighing 18‑22 g) flanks, or in the case of MDA‑MB‑231 cells, into the abdomen mammary fat pads[3].
Dosage: 15 mg/kg
Administration: I.p., twice every week (MDA‑MB‑231, 24 days; HepG2, 23 days; MIAPaCa‑2, 29 days; PANC‑1, 40 days; A549, 29 days; H1650, 18 days; HT29, 12 days)
Result: Demonstrated significant tumor growth inhibition in five models: MDA-MB-231 (breast cancer), HepG2 (liver cancer), MIAPaCa-2 (pancreatic cancer), A549 (lung cancer), and H1650 (lung cancer).
Did not show significant efficacy in two models (PANC-1 pancreatic cancer and HT29 colorectal cancer).
No mice experienced weight loss exceeding 20% or other detectable serious side effects.
Animal Model: SCID/SCIDCBIgh.lblcrTac.Prkdcscid/Ros mice < 5 weeks of age were irradiated at 300 rads using a Mark II Cesium irradiator 24 hours before injecting them with MM1.S cells (5×106) subcutaneously under the skin on the left ventral flank[4].
Dosage: 10 mg/kg, 15 mg/kg
Administration: I.p., 2 or 3 times a week for 48 days
Result: The relative tumor volume in the 10 mg/kg and 15 mg/kg groups was reduced to 49% and 89% of that in the control group, respectively.
The 15 mg/kg group showed a tumor reduction of over 91%.
The median survival in the 10 mg/kg group was prolonged to 27 days.
The median survival in the 15 mg/kg group was significantly prolonged to 48 days.
During the two-week observation period after treatment cessation in the 15 mg/kg group, two of the three surviving mice did not show tumor regeneration.
分子量

459.56

Formula

C25H25N5O2S
CAS 号
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

JP-11646 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

JP-116461902983-63-4JP11646JP 11646PimCaspaseApoptosisNecroptosisPARPNF-κBPim kinasespoly ADP ribose polymerase Nuclear factor-κBNuclear factor-kappaBSmall Cell Lung Cancerlarge cell neuroendocrine carcinomas of the lungPIM2MYCp-4EBP-1caspase-3human acute leukemiaAMLtriple-negative breast cancer (TNBC)Inhibitorinhibitorinhibit

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