Flavokawain B (Synonyms: Flavokavain B)

目錄號(hào): HY-N2132 純度: 99.99%: FAQs
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Flavokawain B (Flavokavain B) 是一種口服活性的查耳酮。Flavokawain B 可激活 caspase-9、-3 和 -8，切割 PARP。Flavokawain B 可下調(diào) Bcl-2，同時(shí)增加 Bax 水平。Flavokawain B 可抑制 NF-κB、PI3K/Akt 和 MAPK 信號(hào)通路。Flavokawain B 具有凋亡 (Apoptotic) 作用。Flavokawain B 可抑制 MMP-9 和促進(jìn) ROS 生成。Flavokawain B 可抑制多種腫瘤和炎癥。

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Flavokawain B Chemical Structure

CAS No. : 1775-97-9

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Customer Review

Other Forms of Flavokawain B:

Flavokawain B (Standard) 詢價(jià)

MCE 顧客使用本產(chǎn)品發(fā)表的 1 篇科研文獻(xiàn)

•Phytomedicine. 2023 Sep 7, 155074.

Flavokawain B 相關(guān)產(chǎn)品

•相關(guān)化合物庫(kù):

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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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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

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Akt Akt1 Akt2 Akt3

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p38 MAPK p38α p38β MAPK13 p38δ p38γ

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MMP-1 MMP-2 MMP-3 MMP-8 MMP-9 MMP-13 MMP-14 MMP-17 ADAM10 ADAM17 MMP-7 MMP-12 MMP-10 MMP ADAM8

生物活性
純度 & 產(chǎn)品資料
參考文獻(xiàn)

生物活性

Flavokawain B (Flavokavain B) is an orally active chalcone. Flavokawain B results in activation of caspase-9, -3 and -8, cleavage of PARP. Flavokawain B down-regulates Bcl-2 with concomitant increase in Bax level. Flavokawain B inhibits NF-κB, PI3K/Akt and MAPK signaling pathway. Flavokawain B exhibits Apoptotic effects. Flavokawain B inhibits MMP-9 and promotes ROS generation. Flavokawain B inhibits multiple tumors and inflammation^[1]^[2]^[3]^[4]^[5]^[6]^[7]^[8]^[9]^[10]^[11]^[12]^[13].

細(xì)胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A549	IC₅₀	> 20 μM Compound: 7	Inhibition of TNFalpha induced NF-kappaB activation in human A549 cells by luciferase reporter gene assay Inhibition of TNFalpha induced NF-kappaB activation in human A549 cells by luciferase reporter gene assay	[PMID: 19883086]
A549	IC₅₀	19.7 μM Compound: 21	Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by alamar blue assay Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by alamar blue assay	[PMID: 31673309]
A549	IC₅₀	8 μg/mL Compound: Flavokawain B	Inhibition of TNF-alpha-induced NF-kappaB expressed in human A549 cells treated 1 hr after TNFalpha challenge measured after 6 hrs by luciferase reporter gene assay Inhibition of TNF-alpha-induced NF-kappaB expressed in human A549 cells treated 1 hr after TNFalpha challenge measured after 6 hrs by luciferase reporter gene assay	[PMID: 19716299]
B16-F10	IC₅₀	7.7 μM Compound: 1a	Antimelanogenic activity in mouse B16F10 cells assessed as inhibition of melanin production after 4 days Antimelanogenic activity in mouse B16F10 cells assessed as inhibition of melanin production after 4 days	[PMID: 25597012]
Caco-2	IC₅₀	9.9 μM Compound: 2	Cytotoxicity against human Caco2 cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay Cytotoxicity against human Caco2 cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay	[PMID: 28214231]
Fibroblast	IC₅₀	> 20 μM Compound: 2	Cytotoxicity against human fibroblasts assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay Cytotoxicity against human fibroblasts assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay	[PMID: 28214231]
HaCaT	IC₅₀	13.6 μM Compound: 2	Cytotoxicity against human HaCaT cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay Cytotoxicity against human HaCaT cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay	[PMID: 28214231]
HCT-116	IC₅₀	> 20 μM Compound: 21	Cytotoxicity against human HCT116 cells assessed as reduction in cell viability incubated for 72 hrs by alamar blue assay Cytotoxicity against human HCT116 cells assessed as reduction in cell viability incubated for 72 hrs by alamar blue assay	[PMID: 31673309]
HCT-116	IC₅₀	7.5 μM Compound: 2	Cytotoxicity against human HCT116 cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay Cytotoxicity against human HCT116 cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay	[PMID: 28214231]
HeLa	IC₅₀	> 20 μM Compound: 21	Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by alamar blue assay Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by alamar blue assay	[PMID: 31673309]
Huh-7	IC₅₀	15.9 μM Compound: 2	Cytotoxicity against human HuH7 cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay Cytotoxicity against human HuH7 cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay	[PMID: 28214231]
MCF7	IC₅₀	15.5 μM Compound: 2	Cytotoxicity against human MCF7 assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay Cytotoxicity against human MCF7 assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay	[PMID: 28214231]
MDA-MB-231	IC₅₀	16.3 μM Compound: 2	Cytotoxicity against human MDA-MB-231 cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay Cytotoxicity against human MDA-MB-231 cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay	[PMID: 28214231]
MIA PaCa-2	IC₅₀	18.2 μM Compound: 21	Cytotoxicity against human MIAPaCa2 cells assessed as reduction in cell viability incubated for 72 hrs by alamar blue assay Cytotoxicity against human MIAPaCa2 cells assessed as reduction in cell viability incubated for 72 hrs by alamar blue assay	[PMID: 31673309]
NCI-H727	IC₅₀	11.3 μM Compound: 2	Cytotoxicity against human NCI-H727 cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay Cytotoxicity against human NCI-H727 cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay	[PMID: 28214231]
NIH3T3	IC₅₀	3.3 μM Compound: 2b	Inhibition of cobalt chloride-induced HIF-1 activation expressed in mouse NIH3T3 cells after 8 hrs by luciferase reporter gene assay Inhibition of cobalt chloride-induced HIF-1 activation expressed in mouse NIH3T3 cells after 8 hrs by luciferase reporter gene assay	[PMID: 21112783]
PC-3	IC₅₀	9.1 μM Compound: 2	Cytotoxicity against human PC3 cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay Cytotoxicity against human PC3 cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay	[PMID: 28214231]
RAW264.7	IC₅₀	26.5 μM Compound: FK B	Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay	[PMID: 32208222]
RAW264.7	IC₅₀	4.2 μM Compound: FK B	Inhibition of LPS-induced nitric oxide production in mouse RAW264.7 cells measured after 24 hrs by Griess reagent based assay Inhibition of LPS-induced nitric oxide production in mouse RAW264.7 cells measured after 24 hrs by Griess reagent based assay	[PMID: 32208222]
REH	IC₅₀	> 20 μM Compound: 21	Cytotoxicity against human REH cells assessed as reduction in cell viability incubated for 72 hrs by alamar blue assay Cytotoxicity against human REH cells assessed as reduction in cell viability incubated for 72 hrs by alamar blue assay	[PMID: 31673309]
RL	IC₅₀	8.2 μM Compound: 2	Cytotoxicity against human RL assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay Cytotoxicity against human RL assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay	[PMID: 28214231]
U-937	IC₅₀	> 20 μM Compound: 21	Cytotoxicity against human U937 cells assessed as reduction in cell viability incubated for 72 hrs by alamar blue assay Cytotoxicity against human U937 cells assessed as reduction in cell viability incubated for 72 hrs by alamar blue assay	[PMID: 31673309]

體外研究
(In Vitro)

Flavokawain B (1-5 μg/mL，18-24 h) 抑制人腦內(nèi)皮細(xì)胞 (HUVEC) 遷移和管形成^[1]。
Flavokawain B (1.25-20 μg/mL，18 h) 通過(guò)下調(diào) PI3K/Akt 軸誘導(dǎo)多種 B 細(xì)胞淋巴瘤細(xì)胞系增殖抑制和凋亡^[3]。
Flavokawain B (5-40 μM，1 h) 具有抗炎活性，可抑制 LPS 誘導(dǎo)的 RAW 264.7 細(xì)胞中 NO 和 PGE2 的產(chǎn)生^[4]。
Flavokawain B (17.6-70.4 μM，24 h) 導(dǎo)致 KB 細(xì)胞凋亡，表現(xiàn)為細(xì)胞活力喪失、形態(tài)學(xué)改變變化、基因組 DNA 碎片化和亞 G1 期積累^[5]。
Flavokawain B (2.5-7.5 μg/mL，24 h) 誘導(dǎo)滑膜肉瘤細(xì)胞系凋亡^[6]。
Flavokawain B (2.5-7.5 μg/mL，24 h) 通過(guò) G2/M 細(xì)胞周期停滯和凋亡抑制人骨肉瘤細(xì)胞 (143B 和 saos-2) 的生長(zhǎng)^[7]。
Flavokawain B (1.25-10 μg/mL，24 h) 通過(guò)細(xì)胞內(nèi) ROS 生成和 Akt/p38 MAPK 信號(hào)下調(diào)誘導(dǎo)人口腔癌 HSC-3 細(xì)胞凋亡通路^[8]。
Flavokawain B (2.5-5 μg/mL，24 h) 表現(xiàn)出強(qiáng)大的凋亡作用，并誘導(dǎo)子宮平滑肌肉瘤細(xì)胞系 SK-LMS-1 和 ECC-1 的 G2/M 停滯^[9]。

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

Cell Viability Assay^[3]

Cell Line:	SUDHL-4, OCI-Ly3, Raji, and Jeko-1
Concentration:	1.25, 2.5, 5, 10, 20 μg/mL
Incubation Time:	24 ?h, 48 h
Result:	Showed dose- and time-dependent inhibition of cell proliferation (SUDHL-4). Mildly affected cell (SUDHL-4) viability at a concentration of 1.25 μg/mL (24 h).

Apoptosis Analysis^[3]

Cell Line:	SUDHL-4, OCI-Ly3, Raji, and Jeko-1
Concentration:	2.5, 5, and 10 μg/mL
Incubation Time:	12 ?h, 24 h
Result:	Increased the number of cleaved PARP and caspase-3 fragments. Reduced the expression of BCL-XL (an anti-apoptotic member of the BCL-2 family). Induced the breakdown of MMP.

體內(nèi)研究
(In Vivo)

Flavokawain B (1-2.5 μg/mL，24 h) 抑制斑馬魚模型中的血管生成^[1]。
Flavokawain B (50-200 mg/kg，腹腔注射) 在 LPS 誘導(dǎo)的小鼠中表現(xiàn)出抗炎活性^[4]。
Flavokawain B (0.35-0.75 mg/kg，腹腔注射，每 2 天一次，27 天) 顯著抑制裸鼠體內(nèi)人類 KB 細(xì)胞衍生腫瘤異種移植瘤的生長(zhǎng)^[5]。
Flavokawain B (20-40 mg/kg，口服，7 天) 通過(guò)靶向 TLR2 抑制結(jié)腸炎小鼠中的 NF-κB 炎癥信號(hào)通路激活^[10]。
Flavokawain B (25 mg/kg，口服，每天一次，持續(xù)一周) 通過(guò)調(diào)節(jié) IKK/NF-κB 和 MAPK 信號(hào)通路，在小鼠中誘導(dǎo) GSH 敏感的氧化應(yīng)激^[11]。
Flavokawain B (10-20 mg/kg，例如，連續(xù) 3 天) 通過(guò)靶向髓系分化因子 2，緩解小鼠 LPS 誘導(dǎo)的急性肺損傷^[12]。
Flavokawain B (25 mg/kg，腹腔注射，每周兩次，持續(xù) 2 周) 與 Cisplatin (HY-17394)/Gemcitabine (HY-17026) 聯(lián)合使用，可顯著抑制異種移植小鼠 (SNU-478 細(xì)胞) 模型中的腫瘤生長(zhǎng)^[13]。

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

Animal Model:	Nude mice injected human KB cell^[5]
Dosage:	0.35, 0.75 mg/kg
Administration:	Intraperitoneal injection (i.p.), every 2 days, 27 days
Result:	Showed no loss of body weight. Showed time-dependent growth inhibition of tumor. Showed tumor cell inactivity or regression. Showed augmentation of apoptotic DNA fragmentation.

分子量

284.31

Formula

C₁₇H₁₆O₄

CAS 號(hào)

1775-97-9

性狀

固體

顏色

Light yellow to yellow

中文名稱

黃卡瓦胡椒素B

結(jié)構(gòu)分類

初始來(lái)源

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性數(shù)據(jù)

細(xì)胞實(shí)驗(yàn)：

DMSO 中的溶解度 : 5 mg/mL (17.59 mM; 超聲助溶 (<60°C); 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開封的 DMSO)

配制儲(chǔ)備液

濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg

1 mM	3.5173 mL	17.5864 mL	35.1729 mL
5 mM	0.7035 mL	3.5173 mL	7.0346 mL
10 mM	0.3517 mL	1.7586 mL	3.5173 mL

查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

摩爾計(jì)算器
稀釋計(jì)算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

濃度 _(start)

體積 _(start)

濃度 _(final)

體積 _(final)

動(dòng)物溶解方案計(jì)算器

請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只

由于實(shí)驗(yàn)過(guò)程有損耗，建議您多配一只動(dòng)物的量

計(jì)算結(jié)果

工作液所需濃度 : mg/mL

純度 & 產(chǎn)品資料

純度: 99.99%

選擇批次：

Data Sheet (632 KB) SDS (252 KB)

COA (285 KB) RP-HPLC (260 KB)

產(chǎn)品使用指南 (1538 KB)

參考文獻(xiàn)

[1]. Rossette MC, et al. The In Vitro and In Vivo Antiangiogenic Effects of Flavokawain B. Phytother Res. 2017 Oct;31(10):1607-1613. [Content Brief]

[2]. Li X, et al. Flavokawain B targets protein neddylation for enhancing the anti-prostate cancer effect of Bortezomib via Skp2 degradation. Cell Commun Signal. 2019 Mar 18;17(1):25. [Content Brief]

[3]. Zhao M, et al. The kava chalcone flavokawain B exerts inhibitory activity and synergizes with BCL-2 inhibition in malignant B-cell lymphoma. Phytomedicine. 2023 Nov;120:155074. [Content Brief]

[4]. Lin CT, et al. Anti-inflammatory activity of Flavokawain B from Alpinia pricei Hayata. J Agric Food Chem. 2009 Jul 22;57(14):6060-5. [Content Brief]

[5]. Lin E, et al. Flavokawain B inhibits growth of human squamous carcinoma cells: Involvement of apoptosis and cell cycle dysregulation in vitro and in vivo. J Nutr Biochem. 2012 Apr;23(4):368-78. [Content Brief]

[6]. Sakai T, et al. Flavokawain B, a kava chalcone, induces apoptosis in synovial sarcoma cell lines. J Orthop Res. 2012 Jul;30(7):1045-50. [Content Brief]

[7]. Ji T, et al. Flavokawain B, a kava chalcone, inhibits growth of human osteosarcoma cells through G2/M cell cycle arrest and apoptosis. Mol Cancer. 2013 Jun 10;12:55. [Content Brief]

[8]. Hseu YC, et al. The chalcone flavokawain B induces G2/M cell-cycle arrest and apoptosis in human oral carcinoma HSC-3 cells through the intracellular ROS generation and downregulation of the Akt/p38 MAPK signaling pathway. J Agric Food Chem. 2012 Mar 7;60(9):2385-97. [Content Brief]

[9]. Eskander RN, et al. Flavokawain B, a novel, naturally occurring chalcone, exhibits robust apoptotic effects and induces G2/M arrest of a uterine leiomyosarcoma cell line. J Obstet Gynaecol Res. 2012 Aug;38(8):1086-94. [Content Brief]

[10]. Chen Y, et al. Flavokawain B inhibits NF-κB inflammatory signaling pathway activation in inflammatory bowel disease by targeting TLR2. Toxicol Appl Pharmacol. 2024 May;486:116922. [Content Brief]

[11]. Zhou P, et al. Flavokawain B, the hepatotoxic constituent from kava root, induces GSH-sensitive oxidative stress through modulation of IKK/NF-kappaB and MAPK signaling pathways. FASEB J. 2010 Dec;24(12):4722-32. [Content Brief]

[12]. Luo W, et al. Flavokawain B alleviates LPS-induced acute lung injury via targeting myeloid differentiation factor 2. Acta Pharmacol Sin. 2022 Jul;43(7):1758-1768. [Content Brief]

[13]. Son JH, et al. Flavokawain B Inhibits Growth of Cholangiocarcinoma Cells by Suppressing the Akt Pathway. In Vivo. 2023 May-Jun;37(3):1077-1084. [Content Brief]

Flavokawain B 相關(guān)分類

完整儲(chǔ)備液配制表

可選溶劑	濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.5173 mL	17.5864 mL	35.1729 mL	87.9322 mL
	5 mM	0.7035 mL	3.5173 mL	7.0346 mL	17.5864 mL
	10 mM	0.3517 mL	1.7586 mL	3.5173 mL	8.7932 mL
	15 mM	0.2345 mL	1.1724 mL	2.3449 mL	5.8621 mL

Help & FAQs

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.

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Flavokawain B (Synonyms: Flavokavain B)

Customer Review

Other Forms of Flavokawain B:

Flavokawain B 相關(guān)抗體

MCE 顧客使用本產(chǎn)品發(fā)表的 1 篇科研文獻(xiàn)

Flavokawain B 相關(guān)產(chǎn)品

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參考文獻(xiàn)

Flavokawain B 相關(guān)抗體:

摩爾計(jì)算器

稀釋計(jì)算器

Flavokawain B 相關(guān)分類

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