标签归档：抑制剂

JW480

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JW480 

JW480 是丝氨酸水解酶 KIAA1363 的有效选择性抑制剂。

JW480

JW480 Chemical Structure

CAS No. : 1354359-53-7

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生物活性

JW480 is a potent and selective inhibitor of a serine hydrolase enzyme KIAA1363[1].

分子量

333.42

Formula

C22H23NO2
CAS 号

1354359-53-7
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]. Chang JW, et al. A potent and selective inhibitor of KIAA1363/AADACL1 that impairs prostate cancer pathogenesis. Chem Biol. 2011 Apr 22;18(4):476-84.

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Butyrolactone I(Synonyms: Olomoucin)

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Butyrolactone I (Synonyms: Olomoucin)

Butyrolactone I 是 CDK1 的 ATP 竞争性抑制剂，是 A.terreus 的次级代谢产物。Butyrolactone I 在非小细胞肺癌、小细胞肺癌和前列腺癌细胞系中具有抗肿瘤作用。

Butyrolactone I(Synonyms: Olomoucin)

Butyrolactone I Chemical Structure

CAS No. : 87414-49-1

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生物活性

Butyrolactone I is an ATP-competitive inhibitor of CDK1 as a secondary metabolite from A. terreus[1]. Butyrolactone I has antitumor effects in non-small cell lung, small cell lung, and prostate cancer cell lines[2].

IC50 & Target

CDK1

 

分子量

424.44

Formula

C24H24O7
CAS 号

87414-49-1
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]. Nishio K, et al. Antitumor effects of butyrolactone I, a selective cdc2 kinase inhibitor, on human lung cancer cell lines. Anticancer Res. 1996 Nov-Dec;16(6B):3387-95. P

    [2]. Suzuki M, et al. Butyrolactone I induces cyclin B1 and causes G2/M arrest and skipping of mitosis in human prostate cell lines. Cancer Lett. 1999 Apr 26;138(1-2):121-30.

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Tyrosinase-IN-5

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Tyrosinase-IN-5 

Tyrosinase-IN-5 (compound 16c) 是一种有效的 tyrosinase 抑制剂，IC50 为 0.02 μM。Tyrosinase-IN-5 有效抑制黑色素生成，对细胞无明显毒性。

Tyrosinase-IN-5

Tyrosinase-IN-5 Chemical Structure

CAS No. : 2525175-90-8

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生物活性

Tyrosinase-IN-5 (compound 16c) is a potent inhibitor of tyrosinase with an IC50 of 0.02 μM. Tyrosinase-IN-5 efficiently suppresses the melanogenesis without significant toxicity on cells[1].

分子量

367.31

Formula

C18H13N3O6
CAS 号

2525175-90-8
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]. Ashooriha M, et al. Kojic acid-natural product conjugates as mushroom tyrosinase inhibitors. Eur J Med Chem. 2020;201:112480.

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Safingol(Synonyms: L-threo-dihydrosphingosine)

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Safingol (Synonyms: L-threo-dihydrosphingosine)

Safingol 是溶血磷脂 PKC (蛋白激酶 C) 的抑制剂。

Safingol(Synonyms: L-threo-dihydrosphingosine)

Safingol Chemical Structure

CAS No. : 15639-50-6

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生物活性

Safingol is a lyso-sphingolipid PKC (protein kinase C ) inhibitor[1].

分子量

301.51

Formula

C18H39NO2
CAS 号

15639-50-6
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]. Tsukamoto S, et al. Sphingosine Kinase-1 Protects Multiple Myeloma from Apoptosis Driven by Cancer-Specific Inhibition of RTKs. Mol Cancer Ther. 2015 Oct;14(10):2303-12.

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EGFR-IN-30

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EGFR-IN-30 

EGFR-IN-30 是一种有效的 EGFR 抑制剂，对 EGFR (WT)、EGFR (L858R/T790M/C797S) 的 IC50 分别为 1-10 nM、<1 nM。EGFR-IN-30 具有用于细胞增殖类疾病，类如肿瘤等研究的潜力。

EGFR-IN-30

EGFR-IN-30 Chemical Structure

CAS No. : 2726463-68-7

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生物活性

EGFR-IN-30 is a potent EGFR inhibitor with IC50s of 1-10 nM, <1 nm for egfr (wt), (l858r>[1].

IC50 & Target[1]

EGFR (WT)

1-10 nM (IC50)

EGFR (L858R/T790M/C797S)

<1 nM (IC50)

体外研究
(In Vitro)

EGFR-IN-30 (compound 27) inhibits A431 cell (IC50=100-1000 nM),Ba/F3_L858R/T790M/C797S cell (IC50<10 nm), ba>50<10 nm)[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

610.49

Formula

C28H33BrN7O2P
CAS 号

2726463-68-7
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]. Shansong Zheng, et al. Tricyclic compounds as EGFR inhibitors. WO2021208918A1.

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SHR902275

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SHR902275 

SHR902275 是一种有效、选择性和口服活性 RAF 抑制剂，靶向 RAS 突变癌症。 对于 cRAF、bRAFwt 和 bRAFV600E，SHR902275 对 cRAF, bRAFwt, bRAFV600E 的 IC50 分别为 1.6 nM、10 nM、5.7 nM。 SHR902275 显示细胞生长抑制作用，对 H358、A375、Calu6 和 SK-MEL2 细胞的 GI50 分别为 1.5 和 0.17 nM、0.4 nM 和 0.32 nM .

SHR902275

SHR902275 Chemical Structure

CAS No. : 2695506-82-0

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生物活性

SHR902275 is a potent, selective, and orally active RAF inhibitor targeting RAS mutant cancers. SHR902275 has IC50s of 1.6 nM, 10 nM, and 5.7 nM for cRAF, bRAFwt, and bRAFV600E, respectively. SHR902275 shows cell growth inhibition with GI50s of 1.5 and 0.17 nM, 0.4 nM and 0.32 nM for H358, A375, Calu6, and SK-MEL2 cells respectively[1].

IC50 & Target[1]

c-Raf

1.6 nM (IC50)

BRafV600E

5.7 nM (IC50)

BRAFWT

10 nM (IC50)

分子量

512.48

Formula

C26H23F3N4O4
CAS 号

2695506-82-0
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]. Zhao P, et al. Discovery of spiro amide SHR902275: A potent, selective, and efficacious RAF inhibitor targeting RAS mutant cancers. Eur J Med Chem. 2022;228:114040.

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Butyrolactone I(Synonyms: Olomoucin)

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Butyrolactone I (Synonyms: Olomoucin)

Butyrolactone I 是 CDK1 的 ATP 竞争性抑制剂，是 A.terreus 的次级代谢产物。Butyrolactone I 在非小细胞肺癌、小细胞肺癌和前列腺癌细胞系中具有抗肿瘤作用。

Butyrolactone I(Synonyms: Olomoucin)

Butyrolactone I Chemical Structure

CAS No. : 87414-49-1

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生物活性

Butyrolactone I is an ATP-competitive inhibitor of CDK1 as a secondary metabolite from A. terreus[1]. Butyrolactone I has antitumor effects in non-small cell lung, small cell lung, and prostate cancer cell lines[2].

IC50 & Target

CDK1

 

分子量

424.44

Formula

C24H24O7
CAS 号

87414-49-1
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]. Nishio K, et al. Antitumor effects of butyrolactone I, a selective cdc2 kinase inhibitor, on human lung cancer cell lines. Anticancer Res. 1996 Nov-Dec;16(6B):3387-95. P

    [2]. Suzuki M, et al. Butyrolactone I induces cyclin B1 and causes G2/M arrest and skipping of mitosis in human prostate cell lines. Cancer Lett. 1999 Apr 26;138(1-2):121-30.

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TMI-1(Synonyms: WAY-171318)

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TMI-1 (Synonyms: WAY-171318)

TMI-1 是去整合素金属酶 17 (ADAM17) 和其它基质金属蛋白酶 MMPs 的有效抑制剂。TMI-1 能有效抑制 LPS 诱导的人原代单核细胞和人全血中 TNF-α 的分泌。TMI-1 在三阴性 (TN) 和 ERBB2 过度表达的乳腺肿瘤细胞系中选择性诱导 Caspase 依赖的细胞凋亡。

TMI-1(Synonyms: WAY-171318)

TMI-1 Chemical Structure

CAS No. : 287403-39-8

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生物活性

TMI-1 is a potent inhibitor of disintegrin metalloenzyme 17 (ADAM17) and other MMPs. TMI-1 inhibits LPS-induced TNF-α secretion in human primary monocytes, and human whole blood[1]. TMI-1 selectively induces caspase-dependent apoptosis in triple negative (TN) and ERBB2-overexpressing breast tumor cell lines[2].

IC50 & Target

ADAM17

8.4 nM (IC50)

分子量

398.50

Formula

C17H22N2O5S2
CAS 号

287403-39-8
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]. Zhang Y, et al. Identification and characterization of 4-[[4-(2-butynyloxy)phenyl]sulfonyl]-N-hydroxy-2,2-dimethyl-(3S)thiomorpholinecarboxamide (TMI-1), a novel dual tumor necrosis factor-alpha-converting enzyme/matrix metalloprotease inhibitor for the treatment of rheumatoid arthritis. J Pharmacol Exp Ther. 2004 Apr;309(1):348-55.

    [2]. Mezil L, et al. Tumor selective cytotoxic action of a thiomorpholin hydroxamate inhibitor (TMI-1) in breast cancer. PLoS One. 2012;7(9):e43409.

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Dezapelisib(Synonyms: INCB040093)

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Dezapelisib (Synonyms: INCB040093)

Dezapelisib (NCB040093) 是一种有效的磷脂酰肌醇 3-激酶 δ (PI3Kδ) 抑制剂。Dezapelisib 是一种很有前景的研究策略，可用于治疗特定的 R/R B 细胞淋巴瘤。

Dezapelisib(Synonyms: INCB040093)

Dezapelisib Chemical Structure

CAS No. : 1262440-25-4

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生物活性

Dezapelisib (NCB040093) is a potent inhibitor of phosphatidylinositol 3-kinase δ (PI3Kδ). Dezapelisib is a promising research strategy for select R/R B-cell lymphomas[1].

分子量

421.45

Formula

C20H16FN7OS
CAS 号

1262440-25-4
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]. Phillips TJ, et al. Phase 1 study of the PI3Kδ inhibitor INCB040093 ± JAK1 inhibitor itacitinib in relapsed/refractory B-cell lymphoma. Blood. 2018;132(3):293-306.

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CDK1-IN-1

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CDK1-IN-1 

CDK1-IN-7是一种有效的 CDK1 抑制剂 (CDK1/CycB IC50=161.2 nM)，具有潜在的抗增殖活性以及对肿瘤组织有选择性。CDK1-IN-7 通过凋亡内在途径以 p53 依赖的方式诱导细胞凋亡 (Apoptosis)。CDK1-IN-7 是一种潜在的靶向抗肿瘤药物。

CDK1-IN-1

CDK1-IN-1 Chemical Structure

CAS No. : 2761858-59-5

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生物活性

CDK1-IN-7 is a potent CDK1 inhibitor (CDK1/CycB IC50=161.2 nM) with potential antiproliferative activity and selectivity for cancer tissues. CDK1-IN-7 induces apoptosis in p53 dependent manner through the intrinsic apoptotic pathway. CDK1-IN-7 is a potential targeted antitumor agent[1].

IC50 & Target

CDK1/cycB

161.2 nM (IC50)

体外研究
(In Vitro)

CDK1-IN-7 (compound 7a) (10 µM, 48 hours) has the high antiproliferative activity with a mean percentage of growth inhibition of 48.5 % over NCI cancer cell lines, and caused more than 40% growth inhibition in 36 cancer cell lines from different cancer subtypes[1].
CDK1-IN-7 (0.1-100 μM, 48 hours) has better selectivity for cancer cells over normal cell lines (IC50 of 17.7 and 6.28 μM in WI-38 and HCT-116 cells, respectively; SI=2.8)[1].
CDK1-IN-7 (17.7 μM in WI-38 and 6.28 μM in HCT-116; 48 hours) has a superior activity on cancerous cells than normal cells in inducing apoptosis and arresting the cell cycle at the G2/M phase[1].
CDK1-IN-7 (17.7 μM in WI-38 and 6.28 μM in HCT-116; 48 hours) can cause cell death mainly through apoptosis rather than necrosis and confirmed that its activity is more selective to cancerous cells than normal cells[1].
CDK1-IN-7 (6.28 μM; 48 hours) induce apoptosis in p53 dependent manner through the intrinsic apoptotic pathway in HCT-116 cells[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

Cell Line: 60 human cancer cell lines (LOX IMVI, IGROV1, A498, COLO205 et al.)[1]
Concentration: 10 µM
Incubation Time: 48 hours
Result: Had the high antiproliferative activity with a mean percentage of growth inhibition of 48.5 % over NCI cancer cell lines, and caused more than 40% growth inhibition in 36 cancer cell lines from different cancer subtypes.

Cell Cytotoxicity Assay

Cell Line: HCT-116 and WI-38 cells[1]
Concentration: 0.1-100 μM
Incubation Time: 48 hours
Result: Had better selectivity for cancer cells over normal cell lines (IC50 of 17.7 and 6.28 μM in WI-38 and HCT-116 cells, respectively; SI=2.8).

Cell Cycle Analysis

Cell Line: HCT-116 and WI-38 cells[1]
Concentration: 17.7 μM in WI-38 and 6.28 μM in HCT-116
Incubation Time: 48 hours
Result: Exerted a superior activity on cancerous cells than normal cells in inducing apoptosis and arresting the cell cycle at the G2/M phase.

分子量

465.50

Formula

C27H23N5O3
CAS 号

2761858-59-5
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]. Elgiushy HR, et al. Identification of a promising hit from a new series of pyrazolo[1,5-a]pyrimidine based compounds as a potential anticancer agent with potent CDK1 inhibitory and pro-apoptotic properties through a multistep in vitro assessment [published online ahead of print, 2022 Jan 29]. Bioorg Chem. 2022;120:105646.

    [2]. Gangadevi S, et al. Kobophenol A Inhibits Binding of Host ACE2 Receptor with Spike RBD Domain of SARS-CoV-2, a Lead Compound for Blocking COVID-19. J Phys Chem Lett. 2021;12(7):1793-1802.

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Carbonic anhydrase inhibitor 12

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Carbonic anhydrase inhibitor 12 

碳酸酐酶抑制剂12是一种有效的 CA II 抑制剂，对 CA I 也有抑制活性(CA II与CA I的 Kis分别为1.72 nM和271 nM)。碳酸酐酶抑制剂12对不同的肿瘤细胞系具有较强的抗癌活性。

Carbonic anhydrase inhibitor 12

Carbonic anhydrase inhibitor 12 Chemical Structure

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生物活性

Carbonic anhydrase inhibitor 12 is a potent CA II inhibitor, also has inhibitory activity in CA I (Kis of 1.72 and 271 nM in CA II and CA I, respectively). Carbonic anhydrase inhibitor 12 has potent anticancer activity against different cancer cell lines[1].

IC50 & Target

Ki: 1.72 nM (CA II), 271 nM (CA I)[1]
体外研究
(In Vitro)

Carbonic anhydrase inhibitor 12 (Compound 14h) (10 μM; 48 hours; single) has great influence on the specificity and the inhibitory potency against the different cancer cell lines[1].
Carbonic anhydrase inhibitor 12 (2.4 μM in MCF-7 and 2.5 μM MDA-MB-231; 48 hours) can arrest the cell cycle of MCF-7 and MDA-MB-231 cells at the G2/M phase[1].
Carbonic anhydrase inhibitor 12 (2.4 μM in MCF-7 and 2.5 μM MDA-MB-231; 48 hours) demonstrates an increase in the early apoptotic and late apoptotic phase in comparison to the control untreated cells[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

Cell Line: MCF-7, T47D, MDA-MB-231, COLO 205, HCT-116, HT29, SW-620, A549, SK-OV-3 and NCI-ADR-RES[1]
Concentration: 10 μM
Incubation Time: 48 hours
Result: Showed a mean growth inhibitory activity of 55.12% and a broad range of antiproliferative activity against most of the tested cancer cell lines.

Cell Cycle Analysis

Cell Line: MCF-7 and MDA-MB-231[1]
Concentration: 2.4 μM in MCF-7, 2.5 μM MDA-MB-231
Incubation Time: 48 hours
Result: Arrested the cell cycle of MCF-7 and MDA-MB-231 cells at the G2/M phase.

Apoptosis Analysis

Cell Line: MCF-7 and MDA-MB-231[1]
Concentration: 2.4 μM in MCF-7, 2.5 μM MDA-MB-231
Incubation Time: 48 hours
Result: Demonstrated an increase in the early apoptotic and late apoptotic phase in comparison to the control untreated cells.

分子量

640.53

Formula

C27H22BrN5O5S2
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]. Abdel-Mohsen HT, et al. Application of the dual-tail approach for the design and synthesis of novel Thiopyrimidine-Benzenesulfonamide hybrids as selective carbonic anhydrase inhibitors. Eur J Med Chem. 2022;228:114004.

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EGFR-IN-30

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EGFR-IN-30 

EGFR-IN-30 是一种有效的 EGFR 抑制剂，对 EGFR (WT)、EGFR (L858R/T790M/C797S) 的 IC50 分别为 1-10 nM、<1 nM。EGFR-IN-30 具有用于细胞增殖类疾病，类如肿瘤等研究的潜力。

EGFR-IN-30

EGFR-IN-30 Chemical Structure

CAS No. : 2726463-68-7

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生物活性

EGFR-IN-30 is a potent EGFR inhibitor with IC50s of 1-10 nM, <1 nm for egfr (wt), (l858r>[1].

IC50 & Target[1]

EGFR (WT)

1-10 nM (IC50)

EGFR (L858R/T790M/C797S)

<1 nM (IC50)

体外研究
(In Vitro)

EGFR-IN-30 (compound 27) inhibits A431 cell (IC50=100-1000 nM),Ba/F3_L858R/T790M/C797S cell (IC50<10 nm), ba>50<10 nm)[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

610.49

Formula

C28H33BrN7O2P
CAS 号

2726463-68-7
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]. Shansong Zheng, et al. Tricyclic compounds as EGFR inhibitors. WO2021208918A1.

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DHODH-IN-19

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DHODH-IN-19 

DHODH-IN-19 是一种有效的 DHODH 抑制剂。DHODH 存在于人类线粒体的内膜中，是一种含铁的黄素依赖性酶。DHODH-IN-19 抑制肿瘤生长。DHODH-IN-19具有研究癌症和炎症疾病的潜力 (摘自专利 WO2021238881A1，化合物 1)。

DHODH-IN-19

DHODH-IN-19 Chemical Structure

CAS No. : 2742675-85-8

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生物活性

DHODH-IN-19 is a potent inhibitor of DHODH. DHODH is present in the inner membrane of human mitochondria and is an iron-containing flavin-dependent enzyme. DHODH-IN-19 inhibits tumor growth. DHODH-IN-19 has the potential for the research of cancer and inflammation disease (extracted from patent WO2021238881A1, compound 1)[1].

分子量

521.84

Formula

C22H18ClF6N3O3
CAS 号

2742675-85-8
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]. Shuhui Chen, et al. Triazolones. Patent WO2021238881A1.

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TMI-1(Synonyms: WAY-171318)

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TMI-1 (Synonyms: WAY-171318)

TMI-1 是去整合素金属酶 17 (ADAM17) 和其它基质金属蛋白酶 MMPs 的有效抑制剂。TMI-1 能有效抑制 LPS 诱导的人原代单核细胞和人全血中 TNF-α 的分泌。TMI-1 在三阴性 (TN) 和 ERBB2 过度表达的乳腺肿瘤细胞系中选择性诱导 Caspase 依赖的细胞凋亡。

TMI-1(Synonyms: WAY-171318)

TMI-1 Chemical Structure

CAS No. : 287403-39-8

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生物活性

TMI-1 is a potent inhibitor of disintegrin metalloenzyme 17 (ADAM17) and other MMPs. TMI-1 inhibits LPS-induced TNF-α secretion in human primary monocytes, and human whole blood[1]. TMI-1 selectively induces caspase-dependent apoptosis in triple negative (TN) and ERBB2-overexpressing breast tumor cell lines[2].

IC50 & Target

ADAM17

8.4 nM (IC50)

分子量

398.50

Formula

C17H22N2O5S2
CAS 号

287403-39-8
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]. Zhang Y, et al. Identification and characterization of 4-[[4-(2-butynyloxy)phenyl]sulfonyl]-N-hydroxy-2,2-dimethyl-(3S)thiomorpholinecarboxamide (TMI-1), a novel dual tumor necrosis factor-alpha-converting enzyme/matrix metalloprotease inhibitor for the treatment of rheumatoid arthritis. J Pharmacol Exp Ther. 2004 Apr;309(1):348-55.

    [2]. Mezil L, et al. Tumor selective cytotoxic action of a thiomorpholin hydroxamate inhibitor (TMI-1) in breast cancer. PLoS One. 2012;7(9):e43409.

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SHR902275

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SHR902275 

SHR902275 是一种有效、选择性和口服活性 RAF 抑制剂，靶向 RAS 突变癌症。 对于 cRAF、bRAFwt 和 bRAFV600E，SHR902275 对 cRAF, bRAFwt, bRAFV600E 的 IC50 分别为 1.6 nM、10 nM、5.7 nM。 SHR902275 显示细胞生长抑制作用，对 H358、A375、Calu6 和 SK-MEL2 细胞的 GI50 分别为 1.5 和 0.17 nM、0.4 nM 和 0.32 nM .

SHR902275

SHR902275 Chemical Structure

CAS No. : 2695506-82-0

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生物活性

SHR902275 is a potent, selective, and orally active RAF inhibitor targeting RAS mutant cancers. SHR902275 has IC50s of 1.6 nM, 10 nM, and 5.7 nM for cRAF, bRAFwt, and bRAFV600E, respectively. SHR902275 shows cell growth inhibition with GI50s of 1.5 and 0.17 nM, 0.4 nM and 0.32 nM for H358, A375, Calu6, and SK-MEL2 cells respectively[1].

IC50 & Target[1]

c-Raf

1.6 nM (IC50)

BRafV600E

5.7 nM (IC50)

BRAFWT

10 nM (IC50)

分子量

512.48

Formula

C26H23F3N4O4
CAS 号

2695506-82-0
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]. Zhao P, et al. Discovery of spiro amide SHR902275: A potent, selective, and efficacious RAF inhibitor targeting RAS mutant cancers. Eur J Med Chem. 2022;228:114040.

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Corydamine(Synonyms: 刻叶紫堇胺)

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Corydamine (Synonyms: 刻叶紫堇胺)

Corydamine 是一种 3-芳基异喹啉生物碱, 一种有效的 DNA 拓扑异构酶 I/II (DNA topoisomerase I/II) 抑制剂。Corydamine 具有抗癌活性。

Corydamine(Synonyms: 刻叶紫堇胺)

Corydamine Chemical Structure

CAS No. : 49870-84-0

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生物活性

Corydamine, 3-arylisoquinoline alkaloid, is a potent DNA topoisomerase I/II inhibitor. Corydamine has anti-cancer activity[1].

IC50 & Target[1]

Topoisomerase I

 

Topoisomerase II

 

分子量

350.37

Formula

C20H18N2O4
CAS 号

49870-84-0
中文名称

刻叶紫堇胺
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]. Xuemei Deng, et al. Design, synthesis and anti-hepatocellular carcinoma activity of 3-arylisoquinoline alkaloids. Eur J Med Chem. 2022 Jan 15;228:113985.

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Dezapelisib(Synonyms: INCB040093)

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Dezapelisib (Synonyms: INCB040093)

Dezapelisib (NCB040093) 是一种有效的磷脂酰肌醇 3-激酶 δ (PI3Kδ) 抑制剂。Dezapelisib 是一种很有前景的研究策略，可用于治疗特定的 R/R B 细胞淋巴瘤。

Dezapelisib(Synonyms: INCB040093)

Dezapelisib Chemical Structure

CAS No. : 1262440-25-4

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生物活性

Dezapelisib (NCB040093) is a potent inhibitor of phosphatidylinositol 3-kinase δ (PI3Kδ). Dezapelisib is a promising research strategy for select R/R B-cell lymphomas[1].

分子量

421.45

Formula

C20H16FN7OS
CAS 号

1262440-25-4
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]. Phillips TJ, et al. Phase 1 study of the PI3Kδ inhibitor INCB040093 ± JAK1 inhibitor itacitinib in relapsed/refractory B-cell lymphoma. Blood. 2018;132(3):293-306.

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Tubulin polymerization-IN-7

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Tubulin polymerization-IN-7 

Tubulin aggregation-IN-7 (compound 5) 是一种有效的tubulin 聚合抑制剂。Tubulin aggregation-IN-7 具有研究癌症疾病的潜力。

Tubulin polymerization-IN-7

Tubulin polymerization-IN-7 Chemical Structure

CAS No. : 1394017-46-9

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生物活性

Tubulin polymerization-IN-7 (compound 5) is a potent inhibitor of tubulin polymerization. Tubulin polymerization-IN-7 has the potential for the research of cancer diseases[1].

分子量

544.58

Formula

C28H24N4O6S
CAS 号

1394017-46-9
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]. Chen L, et al. Concise synthesis and preliminary biological evaluation of new triazolylthioacetone derivatives bearing pyridine, pyrazine, and 3,4,5-trimethoxybenzyl fragment. Bioorg Med Chem Lett. 2022;66:128721.

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CDK1-IN-1

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CDK1-IN-1 

CDK1-IN-7是一种有效的 CDK1 抑制剂 (CDK1/CycB IC50=161.2 nM)，具有潜在的抗增殖活性以及对肿瘤组织有选择性。CDK1-IN-7 通过凋亡内在途径以 p53 依赖的方式诱导细胞凋亡 (Apoptosis)。CDK1-IN-7 是一种潜在的靶向抗肿瘤药物。

CDK1-IN-1

CDK1-IN-1 Chemical Structure

CAS No. : 2761858-59-5

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生物活性

CDK1-IN-7 is a potent CDK1 inhibitor (CDK1/CycB IC50=161.2 nM) with potential antiproliferative activity and selectivity for cancer tissues. CDK1-IN-7 induces apoptosis in p53 dependent manner through the intrinsic apoptotic pathway. CDK1-IN-7 is a potential targeted antitumor agent[1].

IC50 & Target

CDK1/cycB

161.2 nM (IC50)

体外研究
(In Vitro)

CDK1-IN-7 (compound 7a) (10 µM, 48 hours) has the high antiproliferative activity with a mean percentage of growth inhibition of 48.5 % over NCI cancer cell lines, and caused more than 40% growth inhibition in 36 cancer cell lines from different cancer subtypes[1].
CDK1-IN-7 (0.1-100 μM, 48 hours) has better selectivity for cancer cells over normal cell lines (IC50 of 17.7 and 6.28 μM in WI-38 and HCT-116 cells, respectively; SI=2.8)[1].
CDK1-IN-7 (17.7 μM in WI-38 and 6.28 μM in HCT-116; 48 hours) has a superior activity on cancerous cells than normal cells in inducing apoptosis and arresting the cell cycle at the G2/M phase[1].
CDK1-IN-7 (17.7 μM in WI-38 and 6.28 μM in HCT-116; 48 hours) can cause cell death mainly through apoptosis rather than necrosis and confirmed that its activity is more selective to cancerous cells than normal cells[1].
CDK1-IN-7 (6.28 μM; 48 hours) induce apoptosis in p53 dependent manner through the intrinsic apoptotic pathway in HCT-116 cells[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

Cell Line: 60 human cancer cell lines (LOX IMVI, IGROV1, A498, COLO205 et al.)[1]
Concentration: 10 µM
Incubation Time: 48 hours
Result: Had the high antiproliferative activity with a mean percentage of growth inhibition of 48.5 % over NCI cancer cell lines, and caused more than 40% growth inhibition in 36 cancer cell lines from different cancer subtypes.

Cell Cytotoxicity Assay

Cell Line: HCT-116 and WI-38 cells[1]
Concentration: 0.1-100 μM
Incubation Time: 48 hours
Result: Had better selectivity for cancer cells over normal cell lines (IC50 of 17.7 and 6.28 μM in WI-38 and HCT-116 cells, respectively; SI=2.8).

Cell Cycle Analysis

Cell Line: HCT-116 and WI-38 cells[1]
Concentration: 17.7 μM in WI-38 and 6.28 μM in HCT-116
Incubation Time: 48 hours
Result: Exerted a superior activity on cancerous cells than normal cells in inducing apoptosis and arresting the cell cycle at the G2/M phase.

分子量

465.50

Formula

C27H23N5O3
CAS 号

2761858-59-5
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]. Elgiushy HR, et al. Identification of a promising hit from a new series of pyrazolo[1,5-a]pyrimidine based compounds as a potential anticancer agent with potent CDK1 inhibitory and pro-apoptotic properties through a multistep in vitro assessment [published online ahead of print, 2022 Jan 29]. Bioorg Chem. 2022;120:105646.

    [2]. Gangadevi S, et al. Kobophenol A Inhibits Binding of Host ACE2 Receptor with Spike RBD Domain of SARS-CoV-2, a Lead Compound for Blocking COVID-19. J Phys Chem Lett. 2021;12(7):1793-1802.

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Carbonic anhydrase inhibitor 12

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Carbonic anhydrase inhibitor 12 

碳酸酐酶抑制剂12是一种有效的 CA II 抑制剂，对 CA I 也有抑制活性(CA II与CA I的 Kis分别为1.72 nM和271 nM)。碳酸酐酶抑制剂12对不同的肿瘤细胞系具有较强的抗癌活性。

Carbonic anhydrase inhibitor 12

Carbonic anhydrase inhibitor 12 Chemical Structure

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生物活性

Carbonic anhydrase inhibitor 12 is a potent CA II inhibitor, also has inhibitory activity in CA I (Kis of 1.72 and 271 nM in CA II and CA I, respectively). Carbonic anhydrase inhibitor 12 has potent anticancer activity against different cancer cell lines[1].

IC50 & Target

Ki: 1.72 nM (CA II), 271 nM (CA I)[1]
体外研究
(In Vitro)

Carbonic anhydrase inhibitor 12 (Compound 14h) (10 μM; 48 hours; single) has great influence on the specificity and the inhibitory potency against the different cancer cell lines[1].
Carbonic anhydrase inhibitor 12 (2.4 μM in MCF-7 and 2.5 μM MDA-MB-231; 48 hours) can arrest the cell cycle of MCF-7 and MDA-MB-231 cells at the G2/M phase[1].
Carbonic anhydrase inhibitor 12 (2.4 μM in MCF-7 and 2.5 μM MDA-MB-231; 48 hours) demonstrates an increase in the early apoptotic and late apoptotic phase in comparison to the control untreated cells[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

Cell Line: MCF-7, T47D, MDA-MB-231, COLO 205, HCT-116, HT29, SW-620, A549, SK-OV-3 and NCI-ADR-RES[1]
Concentration: 10 μM
Incubation Time: 48 hours
Result: Showed a mean growth inhibitory activity of 55.12% and a broad range of antiproliferative activity against most of the tested cancer cell lines.

Cell Cycle Analysis

Cell Line: MCF-7 and MDA-MB-231[1]
Concentration: 2.4 μM in MCF-7, 2.5 μM MDA-MB-231
Incubation Time: 48 hours
Result: Arrested the cell cycle of MCF-7 and MDA-MB-231 cells at the G2/M phase.

Apoptosis Analysis

Cell Line: MCF-7 and MDA-MB-231[1]
Concentration: 2.4 μM in MCF-7, 2.5 μM MDA-MB-231
Incubation Time: 48 hours
Result: Demonstrated an increase in the early apoptotic and late apoptotic phase in comparison to the control untreated cells.

分子量

640.53

Formula

C27H22BrN5O5S2
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]. Abdel-Mohsen HT, et al. Application of the dual-tail approach for the design and synthesis of novel Thiopyrimidine-Benzenesulfonamide hybrids as selective carbonic anhydrase inhibitors. Eur J Med Chem. 2022;228:114004.

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