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16

抑制剂 & 化合物

3

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
TP1724L	PUMA BH3 acetate PUMA BH3 acetate(PUMA BH3 Free base)	BCL	Apoptosis
	PUMA BH3 acetate (PUMA BH3 Free base) 是一种 p53 凋亡阳性调节因子 (PUMA) BH3 结构域多肽，可作为 Bak 的直接激活剂，Kd 为 26 nM。
TP1724	PUMA BH3
	PUMA BH3 is a p53 upregulated modulator of apoptosis (PUMA) BH3 domain peptide, acts as a direct activator of Bak, with a Kd of 26 nM.This is a PUMA BH3 domain peptide. PUMA proteins bind Bcl-2, localize to the mitochondria, and induce cytochrome C releas
TP1712	PUMA BH3 (TFA)
	PUMA BH3 (TFA) is a p53 upregulated modulator of apoptosis (PUMA) BH3 domain peptide, acts as a direct activator of Bak, with a Kd of 26 nM.
T75980	PUMA BH3 TFA
	PUMA BH3 (TFA) 是一种 p53 正向凋亡调控因子 (PUMA) BH3 结构域多肽，作为Bak 的直接激活剂，Kd 值为 26 nM。
T83751	PUMA BH3 (human) TFA
	PUMA BH3是一个由p53上调凋亡调节器(PUMA)的BH3域组成的肽，并激活促凋亡蛋白Bak。PUMA BH3与Bak结合（在HEPES和CHAPS缓冲液中的Kds分别为290和26 nM），诱导Bak同源寡聚化和Bak介导的膜透性增加。
TQ0108	MK-6892	GPR	Endocrinology/Hormones; GPCR/G Protein
	MK-6892 是烟酸受体GPR109A 选择性激动剂。它作用于人 GPR109A 的Ki=4 nM，EC50=16 nM。
T15432	GSK256073	GPR; Others	Endocrinology/Hormones; GPCR/G Protein; Others
	GSK256073 是一种口服有活性的GPR109A 选择性激动剂，也是一种持久的人HCA2激动剂(pEC50:7.5) 。它能够减少脂降解，而显著改善葡萄糖稳态，对 2 型糖尿病和血脂异常具有潜在的研究价值。
T36083	DS-7423	PI3K; mTOR	PI3K/Akt/mTOR signaling
	DS-7423 是PI3K 和mTOR 的有效抑制剂，抑制PI3Kα 和 mTOR 的IC50分别为15.6 nM 和 34.9 nM。DS-7423表现出抗癌活性。
T19700	IBC 293 IBC293,1-异丙基-1H-1,2,3-苯并噻唑-5-羧酸,IBC-293	GPR	Endocrinology/Hormones; GPCR/G Protein
	IBC 293 对 GPR109B 的选择性高于烟酸受体 GPR109A。 IBC 293 是 GPR109B 的高选择性激动剂，GPR109B 是一种在脂肪细胞中表达的人类孤儿 G 蛋白偶联受体。
T0794	Mepenzolate Bromide Colibantil,Cantil,溴美喷酯,Cantilaque	AChR	Neuroscience
	Mepenzolate Bromide (Colibantil) 是一种可口服的毒蕈碱受体拮抗剂，对hM2R 和hM3R 的Ki 分别为 0.68 和 2.6 nM。它是GPR109A 抑制剂，可用于抑制与肠易激综合征相关的胃肠道过度运动。
T16682	Pumaprazole BY-841,普马拉唑	Proton pump	Membrane transporter/Ion channel
	Pumaprazole (BY-841) 是一种有效的、可逆的质子泵拮抗剂。
T71691	Pumafentrine BY 343	PDE	Metabolism
	Pumafentrine（BY 343）是 PDE3/PDE4双重抑制剂，可降低小鼠实验性结肠炎的临床评分和 TNF 表达。
T69218	PUMAi HCl
	PUMAi is an inhibitor of p53 up-regulated modulator of apoptosis (PUMA), a BH3-only Bcl-2 family member, mitigating acetaminophen (APAP)-induced hepatocyte necrosis and liver injury.
T16030	Mcl1-IN-8	Others	Others
	Mcl1-IN-8 is an Mcl-1-PUMA interface inhibitor (Ki: 0.3 μM). In cancer cells, Mcl1-IN-8 shows dual activity on reducing PUMA-dependent apoptosis while deactivating Mcl-1-mediated anti-apoptosis.
T73000	SIRT2-IN-11
	SIRT2-IN-11 (AEM1) 是选择性的SIRT2抑制剂，IC50值为 18.5 μM。SIRT2-IN-11 以 p53 依赖的诱导细胞凋亡，激活CDKN1A，PUMA 和NOXA 的表达，并且促进 p53 的乙酰化。SIRT2-IN-11 可用于 p53 相关的癌症研究。
T70008	Bomedemstat ditosylate
	Bomedemstat, also known as IMG-7289, is a lysine-specific histone demethylase 1 (LSD1) inhibitor with antineoplastic activity. Bomedemstat may be useful in the treatment of acute myeloid leukaemia, myelodysplastic syndrome, and Myelofibrosis. IMG-7289 selectively inhibited proliferation and induced apoptosis of JAK2 V617F cells by concomitantly increasing expression and methylation of p53, and, independently, the pro-apoptotic factor PUMA and by decreasing the levels of its antiapoptotic antago...

化合物

PUMA BH3 acetate

Cat.No: TP1724L

Synonym: PUMA BH3 acetate(PUMA BH3 Free base)

Target: BCL

Cat.No: TP1724

PUMA BH3 (TFA)

Cat.No: TP1712

Cat.No: T75980

PUMA BH3 (human) TFA

Cat.No: T83751

Cat.No: TQ0108

Target: GPR

Cat.No: T15432

Target: GPR, Others

Cat.No: T36083

Target: PI3K, mTOR

Cat.No: T19700

Synonym: IBC293,1-异丙基-1H-1,2,3-苯并噻唑-5-羧酸,IBC-293

Target: GPR

Mepenzolate Bromide

Cat.No: T0794

Synonym: Colibantil,Cantil,溴美喷酯,Cantilaque

Target: AChR

Cat.No: T16682

Synonym: BY-841,普马拉唑

Target: Proton pump

Cat.No: T71691

Synonym: BY 343

Target: PDE

Cat.No: T69218

Cat.No: T16030

Target: Others

Cat.No: T73000

Bomedemstat ditosylate

Cat.No: T70008

Cat. No.	Product Name	Target	Signaling Pathways
T12095	Monomethyl fumarate	GPR; Drug Metabolite	Endocrinology/Hormones; GPCR/G Protein; Metabolism
	Monomethyl fumarate 是 Dimethyl fumarate 的活性代谢产物。Monomethyl fumarate 是一种 GPR109A 激动剂。Monomethyl fumarate 是一种 GPR109A 激动剂具有用于多种神经保护途径和其他视网膜疾病模型的潜力。
T5668	Triacetylresveratrol 乙酰化白藜芦醇,三乙酰基白藜芦醇,Acetyl-trans-resveratrol	BCL; NF-κB; STAT	Apoptosis; JAK/STAT signaling; NF-κB; Stem Cells
	Triacetylresveratrol (Acetyl-trans-resveratrol) 是 Resveratrol 的乙酰化类似物，可降低 STAT3和 NF-κB 磷酸化，具有抗癌作用。
TMA1743	Ergosterol peroxide	ERK; VEGFR; p38 MAPK; Wnt/beta-catenin; Akt; JAK; CDK; JNK; STAT; Antifection	Angiogenesis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Cytoskeletal Signaling; JAK/STAT signaling; MAPK; Microbiology/Virology; PI3K/Akt/mTOR signaling; Stem Cells; Tyrosine Kinase/Adaptors
	Ergosterol peroxide is an inhibitor of osteoclast differentiation, which has antiviral, trypanocidal, antitumor, and antiangiogenic actions, it can stimulate Foxo3a activity by inhibiting pAKT and c-Myc and activating pro-apoptotic protein Puma and Bax to

天然产物

Monomethyl fumarate

Cat.No: T12095

Target: GPR, Drug Metabolite

Triacetylresveratrol

Cat.No: T5668

Synonym: 乙酰化白藜芦醇,三乙酰基白藜芦醇,Acetyl-trans-resveratrol

Target: BCL, NF-κB, STAT

Ergosterol peroxide

Cat.No: TMA1743

Target: ERK, VEGFR, p38 MAPK, Wnt/beta-catenin, Akt, JAK, CDK, JNK, STAT, Antifection

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