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Search Results for " allosteric "

Targets Recommended: Serine/threonin kinase

602

抑制剂 & 化合物

12

天然产物

2

化合物库

9

重组蛋白

3

同位素标记化合物

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Cat. No.	Product Name
L1120	AMPK靶向分子库		80 compounds
	80 个靶向AMPK 的分子集合，可用于高通量和高内涵筛选；
L2550	谷氨酰胺代谢化合物库		565 compounds
	565 种谷氨酰胺代谢相关的分子，可以用于高通量和高内涵筛选；

化合物库

AMPK靶向分子库

Cat.No: L1120

Compounds: 80

谷氨酰胺代谢化合物库

Cat.No: L2550

Compounds: 565

Cat. No.	Product Name	Target	Signaling Pathways
T5456	WNK-IN-11 Allosteric WNK Kinase Inhibitor	Serine/threonin kinase	Cell Cycle/Checkpoint; Metabolism
	WNK-IN-11 (Allosteric WNK Kinase Inhibitor) 是(WNK)激酶的变构抑制剂，能够抑制 WNK1 (IC50:4 nM) 。
T61562	CB1R Allosteric modulator 3	cAMP; Cannabinoid Receptor	GPCR/G Protein
	CB1R Allosteric modulator 3 是一种有效的 CB1R 调制剂。CB1R Allosteric modulator 3 抑制 cAMP 和 β-Arrestin ，可用于研究肥胖和尼古丁成瘾。
T62016	CB1R Allosteric modulator 1	Others	Others
	CB1R Allosteric modulator 1 (compound 11) 是有效的 CB1R 变构调节剂。CB1R Allosteric modulator 1 显示出对 CB1Rs 正构配体 (NAM) 功能活性的负面影响。
T61371	CB1R Allosteric modulator 4	Others	Others
	CB1R Allosteric modulator 4 is an effective and positive modulator of cannabinoid type-1 (CB1R), exhibiting significant biological activity. This compound inhibits the production of cAMP and demonstrates strong β-arrestin-2 recruitment [1].
T61276	CB1R Allosteric modulator 2	Others	Others
	CB1R Allosteric modulator 2 (compound 18) is a potent allosteric modulator of the CB1R receptor. It exhibits negative modulation of the functional activity of orthosteric ligands (NAM) at CB1Rs, as demonstrated in previous studies [1].
T64096	Integrase-LEDGF/p75 allosteric inhibitor 1	Others	Others
	Integrase-LEDGF/p75 allosteric inhibitor 1 是一种口服具有活力的 integrase-LEDGF/p75 (IN-LEDGF/p75) 变构抑制剂。Integrase-LEDGF/p75 allosteric inhibitor 1 能够抑制 HIV-1 DNA 整合，表现出抗病毒作用，能够作用于 HIV-1重组分子克隆 NL432 (EC50: 3.9 nM)。
T3464	PHCCC (-) PHCCC	GluR	Neuroscience
	PHCCC ((-) PHCCC) 是 I 组代谢型谷氨酸受体拮抗剂和 mGluR4 的正变构调节剂。它对 mGluR2 和 mGluR8 也有很强的拮抗作用，具有抗帕金森病作用。
T22641	CDPPB	GluR	Neuroscience
	CDPPB 是选择性和脑渗透性的代谢型谷氨酸受体亚型5 (mGluR5) 阳性变构的调节剂，在表达人类 mGluR5 的中国仓鼠卵巢细胞中的 EC50值为 27 nM。它为开发抗精神病药提供了一种可能性。
T8868	4BP-TQS	AChR	Neuroscience
	4BP-TQS 是 α7nAChR 变构激动剂。它利用变构跨膜位点激活 nAChRs。
T21781	A-286982	Integrin	Cytoskeletal Signaling
	A 286982是高效的LFA-1/ICAM-1相互作用变构抑制剂，在LFA-1/ICAM-1结合和LFA-1介导的细胞粘附实验中，其IC50分别为44和35 nM。
T9466	RTICBM-189	Others	Others
	RTICBM-189 是可透过血脑屏障的大麻素 1 型受体变构调节剂，在 Ca2+动员试验中pIC50为 7.54，对 hCB1和 mCB1的 pIC50分别为 5.29 和 6.25。
T4573	Cyclothiazide	GluR	Neuroscience
	Cyclothiazide 是AMPA 受体的正变构调节剂，可快速抑制 AMPA 受体脱敏，并缓慢增强 AMPA 电流。它可以阻断天然和异源表达的AMPA 受体脱敏。
T22711	DCB 3,3'-dichlorobenzaldazine	Others; GluR	Neuroscience; Others
	DCB (3,3'-dichlorobenzaldazine) 是 mGluR5 的变构配体，显示出 3,3'-二甲氧基苯扎嗪 (DMeOB) 的负调节作用。 DCB 在 3,3'-二氟苯扎嗪 (DFB) 的帮助下阻断 mGluR 的正变构调节。
T21747	VU0483605	GluR	Neuroscience
	VU0483605 是一种有效的特异性 mGluR1 正变构调节剂，对人和大鼠的 EC50 分别为 390 和 356 nM。
T22703	CYM-5520 CYM 5520	S1P Receptor; LPL Receptor	GPCR/G Protein
	CYM-5520 是一种选择性的变构鞘氨醇 1-磷酸受体 2 (S1PR2) 激动剂，EC50为 480 nM。它可以在 S1PR2 受体中与 S1P 结合，可用于骨质疏松症研究。
T9884	EN523	Others	Others
	EN523 靶向 K48 泛素特异性去泛素酶 OTUB1 中的非催化变构半胱氨酸 C23。
T23515	VU-29 VU 29	GluR	Neuroscience
	VU-29 是代谢型谷氨酸 5(mGlu5)受体的正变构调节剂，对 rmGluR5 的 EC50为 9 nM，Ki 为 244 nM。相对于其他亚型，它对 mGluR5 具有选择性，对 rmGluR1/rmGluR2和 hmGluR4的 EC50分别为557 nM/1.5 μM 和 154 nM。
T8642	4-CMTB	GPR	Endocrinology/Hormones; GPCR/G Protein
	4-CMTB 是选择性的游离脂肪酸受体 2(FFA2/GPR43)的激动剂以及正变构调节剂 (pEC50=6.38)。
T12103	MR-L2	PDE	Metabolism
	MR-L2 是可逆的、非竞争性的长型异构体磷酸二酯酶 -4激活剂，可以激活代表性的 PDE4 长型异构体 (PDE4A4、PDE4B1、PDE4C3、PDE4D5)。它可抑制 PGE2- 诱导的 MDCK 细胞囊肿形成，其EC50=1.2 µM。
T9699	TAK-615	LPA Receptor	GPCR/G Protein
	TAK-615常用于研究肺纤维化，是一种LPA1受体的负变构调节剂。
T9238	KI-7	Adenosine Receptor	GPCR/G Protein; Neuroscience
	KI-7 是一种A2B 腺苷受体阳性变构调节剂。它增强选择性 A2B 腺苷受体激动剂 BAY 60-6583 和腺苷诱导的 cAMP 积累，EC50分别为 2390 nM 和 2550 nM。它也增强非选择性 A2B 腺苷受体激动剂 NECA 诱导的 cAMP 积累，EC50为 445.8 nM。
T36670	JNJ-67856633	MALT	Immunology/Inflammation
	JNJ-67856633 是口服有效的、选择性的、变构性的 MALT1 protease 抑制剂。在某些情况下，JNJ-67856633可以导致肿瘤停滞。
T28069	ML380 ML 380,ML-380	AChR	Neuroscience
	ML380 是一种高效的中枢神经系统渗透剂 M5 正变构调节剂，对人和大鼠 M5 的 EC50值分别为 190 和 610 nM。它对 M1 和 M3 mAChR 亚型具有中等选择性，可增加 Ach 对 M5 mAChR 的亲和力。
T26869	BMS-986122 BMS 986122	Opioid Receptor	Endocrinology/Hormones; GPCR/G Protein; Neuroscience
	BMS-986122 (BMS 986122) 是选择性 μ 阿片受体正变构调节剂，可增加 β-抑制蛋白募集、腺苷酸环化酶抑制和 G 蛋白活化的作用，还增强 DAMGO 介导的 [35S]GTPγS 在小鼠脑膜中的结合。
T22027	AH-7614 AH 7614	GPR	Endocrinology/Hormones; GPCR/G Protein
	AH-7614 (AH 7614) 是一种选择性的游离脂肪酸受体 4(FFA4/GPR120) 拮抗剂，对人和大小鼠 FFA4 的pIC50值分别为 7.1、8.1 和 8.1。它能够阻断多不饱和 ω-6 脂肪酸亚油酸和 FFA4 激动剂的作用。
T0830	Bithionol 硫双二氯酚,Actamer,硫氯酚	cAMP; Parasite	GPCR/G Protein; Microbiology/Virology
	Bithionol (Actamer) 是一种抗寄生虫药物，对若干癌细胞有抑制作用。
T9694	Emraclidine CVL-231	AChR	Neuroscience
	Emraclidine (CVL-231) 是一种毒蕈碱 M4 受体阳性变构调节剂，可用于神经系统疾病研究。
T23513	VU10010 VU 10010	AChR	Neuroscience
	VU10010 (VU 10010) 是一种高度选择性的M4mAChR 变构增强剂，EC50为 400 nM。它与 M4mAChR 的变构位点结合，增强与 G 蛋白偶联，增加对乙酰胆碱的亲和力，还会增加卡巴胆碱引起的兴奋性传导抑制。
T29137	VU0453595 VU 0453595,VU-0453595	AChR	Neuroscience
	VU0453595 是有效的、高选择性的、全身活性的M1正变构调节剂 (PAM, EC50=2140 nM)，在精神分裂症方面有研究价值。
T8497	SX-682	CXCR	Autophagy; GPCR/G Protein; Immunology/Inflammation
	SX-682 是口服有效的 CXCR1和 CXCR2变构抑制剂，可以阻断肿瘤髓系抑制细胞募集并增强 T 细胞活化和抗肿瘤免疫，具有治疗去势抵抗性前列腺癌的潜力。
T8776	FEMA 4774 S9632	Others	Others
	FEMA 4774 (S9632) 是 T1R2/T1R3 的正变构调节剂。 FEMA 4774 在感官评价测试中表现出明显增强蔗糖的甜度。
T13176	TNO155 Batoprotafib	Phosphatase	Metabolism
	TNO155 是具有口服活性野生型SHP2的选择性变构抑制剂 (IC50= 0.011 µM)。它有研究 RTK 依赖性恶性肿瘤（尤其是晚期实体瘤）的潜力。
T14127	Adenosine A1 receptor activator T62	Adenosine Receptor	GPCR/G Protein; Neuroscience
	Adenosine A1 receptor activator T62 是腺苷 A1 受体的变构增强剂，有镇痛作用。
T7776	ADH-503 GB1275	Complement System	Immunology/Inflammation
	ADH-503 (GB1275) 是一种可口服的变构CD11b 激动剂，可以导致与肿瘤相关的巨噬细胞重新极化，可减轻骨髓细胞的免疫抑制，并增强树突状细胞的反应。
T10826	CK-666	HIV Protease; Microtubule Associated	Cytoskeletal Signaling; Microbiology/Virology; Proteases/Proteasome
	CK-666 是一种肌动蛋白相关蛋白 Arp2/3 复合物的细胞渗透性抑制剂。它与 Arp2/3 复合物结合，稳定复合物的非活性状态，阻止 Arp2 和 Arp3 亚基进入活化的丝状短节距构象。
T15050	Danicamtiv MYK-491,SAR 440181	Myosin	Cytoskeletal Signaling
	Danicamtiv (MYK-491) 是一种正性肌力药物，也是一种心肌肌球蛋白的选择性变构激活剂，可增加心脏收缩功能并保持机械效率。
T8421	TED-347	YAP	Stem Cells
	TED-347 是不可逆的、共价的 YAP-TEAD 蛋白质-蛋白质相互作用变构抑制剂，对 TEAD4•Yap1 蛋白质-蛋白质相互作用的 EC50为 5.9 μM。它与 TEAD4 中央口袋内的 Cys-367 特异性共价结合(Ki:10.3 μM)。它可以抑制 TEAD 的转录活性，并且具有抗肿瘤作用。
T26396	6-Hydroxy-DOPA 6-羟基-DL-多巴,6-Hydroxy-DL-DOPA	DNA/RNA Synthesis	Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	6-Hydroxy-DOPA 是 RAD52 的变构抑制剂，可用于癌症研究。它在体外抑制 BRCA 缺陷癌细胞的增殖，也抑制 APE1。
T22282	Brr2-IN-3 Brr2 Inhibitor 9,Brr2 Inhibitor C9	Others	Others
	Brr2-IN-3 (Brr2 Inhibitor C9) 是选择性 Brr2解旋酶变构抑制剂。它呈剂量依赖性地抑制解旋酶(IC50:1.3 μM)。
T9072	Tuxobertinib BDTX-189	EGFR; HER; BTK; RIP kinase	Angiogenesis; Apoptosis; JAK/STAT signaling; NF-κB; Tyrosine Kinase/Adaptors
	Tuxobertinib (BDTX-189) 是一种高效可口服的选择性 EGFR 和 HER2变构突变抑制剂，具有抗癌活性。它对 EGFR、HER2、BLK 和 RIPK2 的 KD 值分别为 0.2、0.76、13 和 1.2 nM。
T1817	GNF-2 GNF2	SARS-CoV; Bcr-Abl	Angiogenesis; Cytoskeletal Signaling; Microbiology/Virology; Tyrosine Kinase/Adaptors
	GNF-2 是一种高选择性的非 ATP 竞争性 Bcr-Abl 抑制剂。它抑制 Ba/F3.p210 增殖，IC50为 138 nM。
T21935L	AMN082 free base AMN082	GluR	Neuroscience
	AMN082 free base 是 mGluR7选择性激动剂，口服有活性，能够透过血脑屏障，可通过跨膜区的变构位点直接激活受体信号。在表达 mGluR7 的转染哺乳动物细胞上，它能够有效抑制 cAMP 积累并刺激 GTPγS 结合。它能够选择性针对 mGluR 的其他亚型及选择性离子型谷氨酸受体。具有抗抑郁活性。
T2463	ML141 CID-2950007	Apoptosis; CDK; Ras	Apoptosis; Cell Cycle/Checkpoint; GPCR/G Protein; MAPK
	ML141 (CID-2950007) 是一种高效变构，选择性可逆的 Cdc42 GTPase 非竞争性抑制剂，IC50值为200 nM。它抑制 Cdc42 野生型和 Cdc42 Q61L 突变体。
T23524	W-84 dibromide HDMPPA	AChR	Neuroscience
	W-84 dibromide (HDMPPA) 是 M2胆碱受体的强变构调节剂，是一种非竞争性毒蕈碱乙酰胆碱受体拮抗剂，具有变构效应。它联合阿托品时，可有效地防止有机磷中毒。它阻碍 [3H]N-甲基东莨菪碱解离，能稳定胆碱能拮抗剂-受体复合物。
T8872	(Rac)-JBJ-04-125-02 JBJ-04-125-02	EGFR	Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	(Rac)-JBJ-04-125-02 (JBJ-04-125-02) 是 JBJ-04-125-02 的消旋体，是选择性突变，可口服的 EGFR 变构抑制剂，对EGFRL858R/T790M 的IC50为 0.26 nM。
T4190	Ticlopidine PCR 5332,Ticlid,噻氯匹定	ATPase; Adiponectin receptor	GPCR/G Protein; Membrane transporter/Ion channel
	Ticlopidine (PCR 5332) 是抗血栓前药。它是CYP2C19人肝细胞色素的抑制剂，抑制 CYP2C9 及 CYP3A4。他是变构CD39的非竞争性抑制剂，能够阻断 NTPDase 同工酶，对NTPDase2和NTPDase3的IC50分别为 170 µM 和 149 µM。
T23469	TQS 4-Naphthalen-1-yl-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-8-sulfonamide	AChR	Neuroscience
	TQS (4-Naphthalen-1-yl-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-8-sulfonamide) 是 α7 烟碱乙酰胆碱受体正变构调节剂，可用于神经炎性疼痛的研究。
T7706	LY-404187 N-[2-(4'-氰基联苯-4-基)丙基]-2-丙烷磺酰胺	GluR; iGluR	Membrane transporter/Ion channel; Neuroscience
	LY404187 是一种选择性的、有效的，中枢活性的AMPA 受体的正变构调节剂，作用于GluR1i，GluR2i，GluR2o，GluR3i 和GluR4i 的EC50值分别为 5.65、0.15、1.44、1.66 和 0.21 µM。它用于许多精神疾病和神经退行性疾病的研究潜力。
T23008L	MMPIP hydrochloride MMPIP hydrochloride (479077-02-6 Free base)	GluR	Neuroscience
	MMPIP hydrochloride 是变构 mGluR7 的选择性拮抗剂。 MMPIP hydrochloride 可用于研究 mGluR7 对中枢神经系统功能的作用。
T1884	CX516 Ampakine CX516,BDP 12,Ampalex,安帕来斯	GluR; iGluR	Membrane transporter/Ion channel; Neuroscience
	CX516 (Ampalex) 是AMPA 受体正向调节剂，可用于研究阿尔茨海默病，精神分裂等。

化合物

Cat.No: T5456

Synonym: Allosteric WNK Kinase Inhibitor

Target: Serine/threonin kinase

CB1R Allosteric modulator 3

Cat.No: T61562

Target: cAMP, Cannabinoid Receptor

CB1R Allosteric modulator 1

Cat.No: T62016

Target: Others

CB1R Allosteric modulator 4

Cat.No: T61371

Target: Others

CB1R Allosteric modulator 2

Cat.No: T61276

Target: Others

Integrase-LEDGF/p75 allosteric inhibitor 1

Cat.No: T64096

Target: Others

Cat.No: T3464

Synonym: (-) PHCCC

Target: GluR

Cat.No: T22641

Target: GluR

Cat.No: T8868

Target: AChR

Cat.No: T21781

Target: Integrin

Cat.No: T9466

Target: Others

Cat.No: T4573

Target: GluR

Cat.No: T22711

Synonym: 3,3'-dichlorobenzaldazine

Target: Others, GluR

Cat.No: T21747

Target: GluR

Cat.No: T22703

Synonym: CYM 5520

Target: S1P Receptor, LPL Receptor

Cat.No: T9884

Target: Others

Cat.No: T23515

Synonym: VU 29

Target: GluR

Cat.No: T8642

Target: GPR

Cat.No: T12103

Target: PDE

Cat.No: T9699

Target: LPA Receptor

Cat.No: T9238

Target: Adenosine Receptor

Cat.No: T36670

Target: MALT

Cat.No: T28069

Synonym: ML 380,ML-380

Target: AChR

Cat.No: T26869

Synonym: BMS 986122

Target: Opioid Receptor

Cat.No: T22027

Synonym: AH 7614

Target: GPR

Cat.No: T0830

Synonym: 硫双二氯酚,Actamer,硫氯酚

Target: cAMP, Parasite

Cat.No: T9694

Synonym: CVL-231

Target: AChR

Cat.No: T23513

Synonym: VU 10010

Target: AChR

Cat.No: T29137

Synonym: VU 0453595,VU-0453595

Target: AChR

Cat.No: T8497

Target: CXCR

Cat.No: T8776

Synonym: S9632

Target: Others

Cat.No: T13176

Synonym: Batoprotafib

Target: Phosphatase

Adenosine A1 receptor activator T62

Cat.No: T14127

Target: Adenosine Receptor

Cat.No: T7776

Synonym: GB1275

Target: Complement System

Cat.No: T10826

Target: HIV Protease, Microtubule Associated

Cat.No: T15050

Synonym: MYK-491,SAR 440181

Target: Myosin

Cat.No: T8421

Target: YAP

Cat.No: T26396

Synonym: 6-羟基-DL-多巴,6-Hydroxy-DL-DOPA

Target: DNA/RNA Synthesis

Cat.No: T22282

Synonym: Brr2 Inhibitor 9,Brr2 Inhibitor C9

Target: Others

Cat.No: T9072

Synonym: BDTX-189

Target: EGFR, HER, BTK, RIP kinase

Cat.No: T1817

Synonym: GNF2

Target: SARS-CoV, Bcr-Abl

AMN082 free base

Cat.No: T21935L

Synonym: AMN082

Target: GluR

Cat.No: T2463

Synonym: CID-2950007

Target: Apoptosis, CDK, Ras

Cat.No: T23524

Synonym: HDMPPA

Target: AChR

(Rac)-JBJ-04-125-02

Cat.No: T8872

Synonym: JBJ-04-125-02

Target: EGFR

Cat.No: T4190

Synonym: PCR 5332,Ticlid,噻氯匹定

Target: ATPase, Adiponectin receptor

Cat.No: T23469

Synonym: 4-Naphthalen-1-yl-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-8-sulfonamide

Target: AChR

Cat.No: T7706

Synonym: N-[2-(4'-氰基联苯-4-基)丙基]-2-丙烷磺酰胺

Target: GluR, iGluR

MMPIP hydrochloride

Cat.No: T23008L

Synonym: MMPIP hydrochloride (479077-02-6 Free base)

Target: GluR

Cat.No: T1884

Synonym: Ampakine CX516,BDP 12,Ampalex,安帕来斯

Target: GluR, iGluR

Cat. No.	Product Name	Target	Signaling Pathways
T4S0878	Prunetin 樱黄素,Prunusetin	ERK; Dehydrogenase; NF-κB	MAPK; Metabolism; NF-κB
	Prunetin (Prunusetin) 是一种O-甲基化异黄酮，具有抗炎的作用。它是人醛脱氢酶的有效抑制剂。
T10085	20(S)-Hydroxycholesterol 20α-Hydroxycholesterol	Smo	Stem Cells
	20(S)-Hydroxycholesterol (20α-Hydroxycholesterol) 是平滑 (smo) 癌蛋白的变构激活剂。
T8363	DL-Serine	PKM	Metabolism
	DL-Serine 是 D-丝氨酸和 L-丝氨酸的混合物，是一种基础代谢物。它具有抗病毒作用，能抑制烟草花叶病毒的增殖。
T3318	Wogonoside 汉黄芩苷,Glychionide B,Wogonin 7-O-glucuronide,Oroxindin	GABA Receptor; Autophagy	Autophagy; Membrane transporter/Ion channel; Neuroscience
	Wogonoside (Wogonin 7-O-glucuronide) 是从黄芩中分离得到的一种黄酮类天然产物，具有抗炎作用。它是 GABAA 受体苯二氮卓位点的正变构调节剂，可通过调节 MAPK-mTOR 通路诱导乳腺癌细胞的自噬。
TN1325	(2S)-6-Prenylnaringenin (2S)-6-异戊烯基柚皮素,6-异戊二烯基柚皮素,6-Prenylnaringenin,6-PN	GABA Receptor	Membrane transporter/Ion channel; Neuroscience
	(2S)-6-Prenylnaringenin (6-Prenylnaringenin) 是强效植物雌激素 8-prenylnaringenin 的异构体，是前脑中最有效的化合物，在 α+β 结合位点上起GABAA 正变构调节剂的作用。
T0086	Galanthamine hydrobromide Galantamine hydrobromide,Galanthamine HBr,氢溴酸加兰他敏	AChR; AChE	Neuroscience
	Galanthamine hydrobromide (Galantamine hydrobromide) 是一种长效的中枢活性 AChE 抑制剂，IC50为 410 nM。它是神经元烟碱型 ACh 受体的变构增强剂，IC50值为 0.35 µM，可用于阿尔茨海默症的研究。
TN3174	6-Methoxyflavanone NSC50184	GABA Receptor	Membrane transporter/Ion channel; Neuroscience
	6-Methoxyflavanone（6-MeOF）是人重组GABA A受体GABA反应的正变构调节剂，具有抗焦虑活性和抗炎活性，可用于减轻顺铂诱导的神经性疼痛。
T2946	Tanshinone IIA sulfonate sodium 丹参酮IIA磺酸盐,丹参酮IIA-磺酸钠,Tanshinone IIA sulfonate,Sodium Tanshinone IIA sulfonate,Tanshinone IIA sodium sulfonate,sodium	CaMK; P450; Calcium Channel	Membrane transporter/Ion channel; Metabolism; Neuroscience
	Tanshinone IIA sulfonate sodium (Tanshinone IIA sodium sulfonate) 是从丹参中提取的丹参酮IIA 的水溶性衍生物，是SOCE 抑制剂，用于心血管疾病的研究。
T0069	Uracil	Others; Endogenous Metabolite	Metabolism; Others
	Uracil 是普遍存在的天然嘧啶衍生物，是 RNA 核酸中的四个碱基之一。
T10609	Brevetoxin-3 PbTx-3	Others	Others
	Brevetoxin-3 (PbTx-3) is a potent allosteric voltage-gated Na+ channel activator. Brevetoxin-3 has a high affinity to site 5 of the voltage-sensitive Na+ channels, inhibits the inactivation of Na+ channels.
T71795	Norstictic acid	Others	Others
	Norstic acid是一种有效的选择性变构转录调节剂，显示出抗癌活性、具有抗氧化活性和抗菌活性。
TN7559	Milbemectin Milbemycin A3 (~30%) and Milbemycin A4 (~70%) Mixture	Others	Others
	Milbemectin is composed of 30% milbemycin A3 and 70% milbemycin A4, exhibiting acaricidal and nematocidal properties effective against adult spider mites, their eggs, and C. elegans, with IC50 values of 5.3, 41.1, and 9.5 µg/ml, respectively. It functions as an allosteric agonist of the Drosophila RDL GABA receptor, and demonstrates efficacy against the pinewood nematode, B. xylophilus, with an LC20 of 0.0781 mg/liter.

天然产物

Cat.No: T4S0878

Synonym: 樱黄素,Prunusetin

Target: ERK, Dehydrogenase, NF-κB

20(S)-Hydroxycholesterol

Cat.No: T10085

Synonym: 20α-Hydroxycholesterol

Target: Smo

Cat.No: T8363

Target: PKM

Cat.No: T3318

Synonym: 汉黄芩苷,Glychionide B,Wogonin 7-O-glucuronide,Oroxindin

Target: GABA Receptor, Autophagy

(2S)-6-Prenylnaringenin

Cat.No: TN1325

Synonym: (2S)-6-异戊烯基柚皮素,6-异戊二烯基柚皮素,6-Prenylnaringenin,6-PN

Target: GABA Receptor

Galanthamine hydrobromide

Cat.No: T0086

Synonym: Galantamine hydrobromide,Galanthamine HBr,氢溴酸加兰他敏

Target: AChR, AChE

6-Methoxyflavanone

Cat.No: TN3174

Synonym: NSC50184

Target: GABA Receptor

Tanshinone IIA sulfonate sodium

Cat.No: T2946

Synonym: 丹参酮IIA磺酸盐,丹参酮IIA-磺酸钠,Tanshinone IIA sulfonate,Sodium Tanshinone IIA sulfonate,Tanshinone IIA sodium sulfonate,sodium

Target: CaMK, P450, Calcium Channel

Cat.No: T0069

Target: Others, Endogenous Metabolite

Cat.No: T10609

Synonym: PbTx-3

Target: Others

Norstictic acid

Cat.No: T71795

Target: Others

Cat.No: TN7559

Synonym: Milbemycin A3 (~30%) and Milbemycin A4 (~70%) Mixture

Target: Others

Species：

Expression System：

Tag：

Cat. No.	Product Name	Species	Expression System
TMPY-02707	PAH Protein, Human, Recombinant (415 Asn/Asp, His) phenylalanine hydroxylase,PH,PKU1,PKU	Human	Baculovirus Insect Cells
	PAH (phenylalanine hydroxylase), also known as PH, belongs to the biopterin-dependent aromatic amino acid hydroxylase family. It contains 1 ACT domain, N-terminal region of PAH is thought to contain allosteric binding sites for phenylalanine and to constitute an "inhibitory" domain that regulates the activity of a catalytic domain in the C-terminal portion of the molecule. In humans, PAH is expressed both in the liver and the kidney, and there is some indication that it may be differentially reg...
TMPH-01404	PYGL Protein, Human, Recombinant (GST) Glycogen phosphorylase, liver form,PYGL	Human	E. coli
	Allosteric enzyme that catalyzes the rate-limiting step in glycogen catabolism, the phosphorolytic cleavage of glycogen to produce glucose-1-phosphate, and plays a central role in maintaining cellular and organismal glucose homeostasis. PYGL Protein, Human, Recombinant (GST) is expressed in E. coli expression system with N-GST tag. The predicted molecular weight is 123.9 kDa and the accession number is P06737.
TMPY-04474	PFKFB3 Protein, Human, Recombinant (His & GST) IPFK2,6-phosphofructo-2-kinase/fructose-2,6-biphosphatase 3,...	Human	Baculovirus Insect Cells
	Fructose-2,6-biphosphatase 3, also known as 6-phosphofructo-2-kinase or PFK2 or PFKFB3, is a potent activator of phosphofructokinase, which is a rate-limiting enzyme of glycolysis. Highly phosphorylated PFKFB3 protein was found in human tumor cells, vascular endothelial cells, and smooth muscle cells. Fructose 2,6-bisphosphate (Fru-2,6-BP) is an allosteric activator of 6-phosphofructo-1-kinase (PFK-1), a rate-limiting enzyme and essential control point in glycolysis. The concentration of PFK2 de...
TMPY-03868	ARF5 Protein, Human, Recombinant (His) ARF5,ADP ribosylation factor 5	Human	E. coli
	ARF5, also known as ADP-ribosylation factor 5, belongs to the small GTPase superfamily, Arf family. Members of this family stimulate the ADP-ribosyltransferase activity of cholera toxin and play a role in vesicular trafficking and as activators of phospholipase D. ARF5 functions as an allosteric activator of the cholera toxin catalytic subunit, an ADP-ribosyltransferase. ARF5 Is involved in protein trafficking. ARF5 may also modulate vesicle budding and uncoating within the Golgi apparatus.
TMPY-03796	ARF3 Protein, Human, Recombinant (His) ADP-ribosylation factor 3	Human	E. coli
	ARF3, also known as ADP-ribosylation factor 3, belongs to the RAS superfamily. Members of this family include ARF1, ARF2, ARF3, ARF4, ARF5 and ARF6. ARF3 gene is a member of the human ARF gene family. These genes encode small guanine nucleotide-binding proteins that stimulate the ADP-ribosyltransferase activity of cholera toxin and play a role in vesicular trafficking and as activators of phospholipase D. ARF3 functions as an allosteric activator of the cholera toxin subunit, an ADP-ribosyltrans...
TMPY-02379	EED Protein, Human, Recombinant (His & GST) HEED,WAIT1,embryonic ectoderm development	Human	Baculovirus Insect Cells
	EED is essential for regulating the repressive histone modification, histone 3 lysine 27 tri-methylation (H3K27me3) at many developmental genes. EED depletion significantly impeded erythroid maturation. EED depletion impaired the generation of hematopoietic stem cells. The function of EED within polycomb repressive complex 2 (PRC2) is mediated by a complex network of protein-protein interactions. The targeted disruption of EED's reader function can lead to allosteric inhibition of PRC2 catalyti...
TMPJ-01055	HBA1 Protein, Human, Recombinant (His) α-globin,Hemoglobin subunit alpha,HBH,HBA-T3,Alpha-globin,He...	Human	E. coli
	Hemoglobin subunit alpha 1 (HBA1), also known as α2β2, is a hetero-tetramer consisting of two α and two β subunits held together by non-covalent interactions. Each subunit contains a heme group with an iron atom in the Fe2+ state. Cooperativity of Hemoglobin (Hb) in binding with O2 and allosteric regulatory binding properties with CO2, H+, Cl−, and 2,3-DPG (2,3-bisphosphoglycerate) are based on subunit interactions. HBA1 is the most common type of Hb in adult humans, which mediates the transport...
TMPY-04462	HK3 Protein, Human, Recombinant (His & GST) HXK3,HKIII,hexokinase 3 (white cell)	Human	Baculovirus Insect Cells
	Hexokinase-3, also known as Hexokinase type III, HKIII, and HK3, is a protein that belongs to the hexokinase family. Hexokinase-3 / HK3 is an enzyme that in humans is encoded by the HK2 gene. Hexokinases phosphorylate glucose to produce glucose 6-phosphate, committing glucose to the glycolytic pathway. In mammalian tissues, hexokinase exists as four isoenzymes encoded by distinct genes. These proteins are homologous and are organized in two homologous domains, except for hexokinase type IV which...
TMPH-02638	HSPA5 Protein, Mouse, Recombinant (E. coli, His) Hspa5,Heat shock protein 70 family protein 5,Endoplasmic ret...	Mouse	E. coli
	Endoplasmic reticulum chaperone that plays a key role in protein folding and quality control in the endoplasmic reticulum lumen. Involved in the correct folding of proteins and degradation of misfolded proteins via its interaction with DNAJC10/ERdj5, probably to facilitate the release of DNAJC10/ERdj5 from its substrate. Acts as a key repressor of the ERN1/IRE1-mediated unfolded protein response (UPR). In the unstressed endoplasmic reticulum, recruited by DNAJB9/ERdj4 to the luminal region of ER...

重组蛋白

PAH Protein, Human, Recombinant (415 Asn/Asp, His)

Cat.No: TMPY-02707

Species: Human

Expression System: Baculovirus Insect Cells

PYGL Protein, Human, Recombinant (GST)

Cat.No: TMPH-01404

Species: Human

Expression System: E. coli

PFKFB3 Protein, Human, Recombinant (His & GST)

Cat.No: TMPY-04474

Species: Human

Expression System: Baculovirus Insect Cells

ARF5 Protein, Human, Recombinant (His)

Cat.No: TMPY-03868

Species: Human

Expression System: E. coli

ARF3 Protein, Human, Recombinant (His)

Cat.No: TMPY-03796

Species: Human

Expression System: E. coli

EED Protein, Human, Recombinant (His & GST)

Cat.No: TMPY-02379

Species: Human

Expression System: Baculovirus Insect Cells

HBA1 Protein, Human, Recombinant (His)

Cat.No: TMPJ-01055

Species: Human

Expression System: E. coli

HK3 Protein, Human, Recombinant (His & GST)

Cat.No: TMPY-04462

Species: Human

Expression System: Baculovirus Insect Cells

HSPA5 Protein, Mouse, Recombinant (E. coli, His)

Cat.No: TMPH-02638

Species: Mouse

Expression System: E. coli

Cat. No.	Product Name	Target	Signaling Pathways
T22301	L-838417 D9 CTP354,CTP354 (C-21191),C-21191	GABA Receptor	Membrane transporter/Ion channel; Neuroscience
	L-838417 D9 (C-21191) 是 L-838417 的氘代物。其中L-838417 是亚型选择性GABAA 正变构调节剂，在 α2, α3 和 α5 亚型中作为部分激动剂。
T14687	Deucravacitinib BMS-986165	Tyrosine Kinases; JAK; IFNAR; Interleukin	Angiogenesis; Chromatin/Epigenetic; Immunology/Inflammation; JAK/STAT signaling; Stem Cells; Tyrosine Kinase/Adaptors
	Deucravacitinib (BMS-986165) 是一种高选择性、口服生物可利用的变构 TYK2 抑制剂，用于治疗自身免疫性疾病。它通过稳定调节 JH2 结构域来阻断受体介导的 Tyk2 激活，可抑制IL-12/23和 I 型IFN 途径。它选择性结合 TYK2 假激酶 (JH2) 结构域，IC50为1.0 nM。
T70394	Deucravacitinib HCl
	Deucravacitinib HCl is a Highly Potent and Selective Allosteric Inhibitor of TYK2. BMS-986165 Blocks Il-12, IL-23 and type I Interferon Signaling and Provides for Robust Efficacy in Preclinical Models of Inflammatory Bowel Disease. MS-986165 potently binds to the Tyk2 pseudokinase domain (Ki = 0.02 nM), and is highly selective against a panel of 265 kinases and pseudokinases. The compound potently inhibited IL-23-, IL-12-, and Type I interferon-driven cellular signaling and transcriptional resp...

同位素标记化合物

Cat.No: T22301

Synonym: CTP354,CTP354 (C-21191),C-21191

Target: GABA Receptor

Deucravacitinib

Cat.No: T14687

Synonym: BMS-986165

Target: Tyrosine Kinases, JAK, IFNAR, Interleukin

Deucravacitinib HCl

Cat.No: T70394

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