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抑制剂 & 化合物

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Cat. No.	Product Name	Target	Signaling Pathways
TP1913	BA 1
	Potent bombesin receptor agonist (IC50 values are 0.26, 1.55 and 2.52 nM for BB1, BB2 and BB3 respectively). Enhances glucose transport in obese and diabetic primary myocytes. Also stimulates NCI-H1299 lung cancer cell proliferation in vitro.
TP1913L1	BA 1 acetate(183241-31-8 free base)	Bombesin Receptor	GPCR/G Protein
	BA 1 acetate(183241-31-8 free base) 是一种有效的铃蟾肽受体激动剂（BB1、BB2 和 BB3 的 IC50 值分别为 0.26、1.55 和 2.52 nM）。它增强肥胖和糖尿病原发性肌细胞中的葡萄糖转运，还可在体外刺激 NCI-H1299 肺癌细胞增殖。
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。
T75945	BA 1 TFA
	BA 1 TFA是一种bombesin (BB)受体家族的激动剂，与Bombesin受体亚型3 (BRS3)、胃泌素释放肽受体 (GRPR)以及神经调节素B受体 (NMBR)具有高度亲和力，其IC50值分别为6、0.4、2.5 nM。
T2490	Osimertinib AZD-9291,Mereletinib,奥希替尼	EGFR	Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	Osimertinib (AZD-9291) 是一种 EGFR 三代抑制剂，抑制二代 EGFR 抑制剂产生的 T790M 耐药突变，具有不可逆性和口服活性。Osimertinib 具有抗肿瘤活性，用于治疗 EGFR 突变的非小细胞肺癌。
T3634	Osimertinib mesylate 甲磺酸奥希替尼,Mereletinib mesylate,奥希替尼甲磺酸盐,AZD-9291 mesylate	EGFR	Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	Osimertinib mesylate (Mereletinib mesylate) 是一种不可逆的突变选择性 EGFR 抑制剂，对EGFRL858R 和EGFRL858R/T790M 的IC50值分别为 12 和 1 nM。
T35900	JAK2-IN-7 JAK2-IN-7	JAK	Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells
	JAK2-IN-7 是一种选择性 JAK2抑制剂，对 JAK2，SET-2 和 Ba/F3V617F 细胞的IC50为 3、11.7 和 41 nM。 JAK2-IN-7 的选择性是 JAK1, JAK3，FLT3 的 14 倍以上。JAK2-IN-7 刺激细胞周期停滞在 G0/G1 期，并诱导肿瘤细胞凋亡 (apoptosis)，具有抗肿瘤活性。
T17927	(S,R,S)-AHPC TFA VH032-NH2 TFA,VHL ligand 1 TFA	Others; Ligand for E3 Ligase	Others; PROTAC
	(S,R,S)-AHPC TFA (VHL ligand 1 TFA) 是一种 VH032-based VHL ligand，可用于募集 von Hippel-Lindau (VHL)蛋白。它能够利用 linker 与靶蛋白配体连接，形成 PROTAC 分子。
T14307	Aplaviroc AK 602,GW 873140,GSK 873140	HIV Protease; CCR	Immunology/Inflammation; Microbiology/Virology; Proteases/Proteasome
	Aplaviroc (AK 602), a SDP derivative, is a CCR5 antagonist. With IC50s of 0.1-0.4 nM for HIV-1Ba-L, HIV-1JRFL and HIV-1MOKW.
T78713	SARS-CoV-2-IN-40	SARS-CoV	Microbiology/Virology
	SARS-CoV-2-IN-40（Compound 19）为SARS-CoV-2抑制剂。该化合物在Calu3肺细胞中针对SARS-CoV-2 BA.1及BA.5变体的感染具有抑制作用，其IC50s分别为100 nM与160 nM。
T78720	SARS-CoV-2-IN-48	SARS-CoV	Microbiology/Virology
	SARS-CoV-2-IN-48 (compound 19)是针对SARS-CoV-2的抑制剂，对Omicron BA.1的IC50值为2.7 μM，展现出了抗病毒活性。
T83146	ALK-IN-27
	ALK-IN-27（化合物1）是一种有效的ALK抑制剂，展现出抗肿瘤活性。在Ba/F3 CLIP1-LTK细胞中，ALK-IN-27的IC50为2.7 nM。
T15480	HG6-64-1 HMSL 10017-101-1	Others	Others
	HG6-64-1 is a potent and selective inhibitor of B-Raf (IC50: 0.09 μM on B-raf V600E transformed Ba/F3 cells).
T62531	TRK-IN-12
	TRK-IN-12 (Compound 9e) 是一种大环衍生的有效TRK抑制剂，具有显著的TRKG595R抑制活性 (IC50= 13.1 nM)。在Ba/F3-LMNA-NTRK1细胞系中具有出色的抗增殖效果 (IC50= 0.080 μM)，并且在Ba/F3-LMNA-NTRK1-G595R细胞系中展示了超过对照活性分子LOXO-101的抑制能力 (IC50= 0.646 μM)。
T35629	ATRA-BA Hybrid
	ATRA-BA hybrid is a mutual prodrug form of all-transretinoic acid and butyric acid .1ATRA-BA hybrid is cleaved to release ATRA and BA in isolated mouse plasma. It inhibits the growth of MDA-MB-231 breast and PC3 prostate cancer cells with GI50values of 0.01 and 1.02 μM, respectively. ATRA-BA (20 μM) has 15-fold greater antiproliferative activity in PC3 cells compared to an equimolar concentration of ATRA and BA. 1.Gediya, L.K., Khandelwal, A., Patel, J., et al.Design, synthesis, and evaluation o...
T73690	Abaloparatide
	Abaloparatide (BA 058) 是一种甲状旁腺激素受体 1 (PTHR1) 类似物。Abaloparatide 也是一种选择性 PTHR1激活剂。Abaloparatide 增强 Gs/cAMP 信号和β-arrestin 募集。Abaloparatide 可增强小鼠的骨形成和皮质结构。Abaloparatide 具有用于骨质疏松症研究的潜力。
T78968	TRK-IN-23	Trk receptor	Tyrosine Kinase/Adaptors
	TRK-IN-23 (compound 24b) 是一款口服活性TRK抑制剂，对TRKA、TRKC、TRKAG595R、TRKAF589L和TRKAG667C 表现出高效的抑制作用，其IC50值分别为0.5 nM、9 nM、14 nM、4.4 nM和4.8 nM。此外，TRK-IN-23 能够诱导含有TRKAG595R和TRKAG667C突变的Ba/F3细胞系进行细胞凋亡(apoptosis)。
T80990	Thrombostatin cont-1
	Thrombostatin cont-1为缓激肽代谢物，归属于凝血抑制素类似物。该化合物在犬颈动脉球囊成形术损伤模型中，能有效减少血小板活化。
T78719	SARS-CoV-2-IN-47	SARS-CoV	Microbiology/Virology
	SARS-CoV-2-IN-47（Compound 13）是一种具有针对SARS-CoV-2变体抑制活性的化合物，显示出对Omicron BA.1的IC50值为0.77 μM，以及对Delta病毒株的IC50值为0.93 μM。该化合物可应用于抗病毒研究领域。
T72289	Type II TRK inhibitor 1	Trk receptor	Tyrosine Kinase/Adaptors
	Type II TRK inhibitor 1 是有效抑制多种TRK融合蛋白及野生型的TRK抑制剂。对携有CD74-TRKAG667C及ETV6-TRKCG696C融合蛋白的Ba/F3细胞表现出抗增殖活性，其IC50值分别为6 nM与1.7 nM。
T7499	TAK-779 Takeda 779	HIV Protease; CXCR; CCR	Autophagy; GPCR/G Protein; Immunology/Inflammation; Microbiology/Virology; Proteases/Proteasome
	TAK-779 (Takeda 779) 是一种非肽类CCR5和CXCR3 拮抗剂，对CCR5的Ki 值为 1.1 nM，并选择性抑制R5 HIV-1。
T72364	SARS-CoV-2 3CLpro-IN-5	SARS-CoV	Microbiology/Virology
	SARS-CoV-2 3CLpro-IN-5 是一种针对 3C样蛋白酶3CLpro 的共价抑制剂，其抑制活性的 IC50 为 3.8 nM。该化合物的口服生物利用度（BA）为 9.0%，可用于 COVID-19 研究。
T79420	FLT3-IN-22
	FLT3-IN-22（化合物22f）是一款高效的FLT3抑制剂，具有针对FLT3和FLT3/D835Y极低的IC50值，分别为0.941 nM和0.199 nM。在MV4-11细胞和携带FLT3变异的Ba/F3细胞系中（涵盖FLT3-D835Y及FLT3-F691L），此抑制剂显示出显著的抗增殖能力。
T80457	ω-Conotoxin Bu8	Calcium Channel	Membrane transporter/Ion channel; Metabolism
	ω-Conotoxin Bu8为含25个氨基酸残基和3个二硫键的ω-芋螺毒素。该化合物能选择性地抑制HEK293T细胞内表达的大鼠CaV2.2介导的Ba2+去极化激活电流，表现出高效的IC50值为89 nM。
T79376	SARS-CoV-2 3CLpro-IN-19	SARS-CoV	Microbiology/Virology
	SARS-CoV-2 3CLpro-IN-19 (Compound C5a)为非共价、非肽类SARS-CoV-2 3CLpro抑制剂，具IC50s值为0.7μM。该化合物对Omicron亚变体（包括BA.5、BQ.1.1及XBB.1.5）在人细胞内的感染显示出具有广谱抗病毒活性，其EC50值介于30-69 nM。
T79706	TRK-IN-24	Trk receptor	Tyrosine Kinase/Adaptors
	TRK-IN-24（compound 10g）是一种针对Trk Receptor的抑制剂，它对TRKA、TRKC、TRKAG595R、TRKAG667C和TRKAF589L的抑制作用的IC50值分别达到5.21、4.51、6.77、1.42和6.13 nM。该化合物在BaF3-CD74-NTRK1G595R和BaF3-CD74-NTRK1G667C异种移植模型中显示出明显的抗肿瘤活性。此外，TRK-IN-24 能有效抑制携带SF、GK、xDFG等单点突变的Ba/F3细胞增殖，其IC50范围为1.43至47.56 nM。
T37443	Aspochalasin D
	Aspochalasin D is a co-metabolite originally isolated from A. microcysticus with aspochalasins A, B, and C, that was initially thought to be inactive. It has antibacterial activity against Gram-positive and Gram-negative bacteria at a concentration of 1 mg/ml. Aspochalasin D is more cytotoxic, via apoptosis, to Ba/F3-V12 cells in an IL-3-free medium than in an IL-3-containing medium (IC50s = 0.49 and 1.9 μg/ml, respectively).
T36379	Halometasone
	Halometasone is a synthetic corticosteroid.1,2Formulations containing halometasone have been used in the treatment of psoriasis vulgaris and eczematous dermatoses. 1.de la Brassine, M., Kint, A., Lachapelle, J.M., et al.Halomethasone (C 48.401-Ba) for the topical treatment of common dermatosesJ. Int. Med. Res.12(5)307-309(1984) 2.Zhu, J.-W., Wu, X.-J., Lu, Z.-F., et al.Role of VEGF receptors in normal and psoriatic human keratinocytes: Evidence from irradiation with different UV sourcesPLoS One8...
T26642	Aplaviroc hydrochloride AK602,AK 602,GW873140A,GW-873140,GW873140,AK-602,Aplaviroc HCl
	Aplaviroc is a human cellular CC chemokine receptor 5 (CCR5) entry inhibitor. Aplaviroc binds specifically to CCR5 and demonstrates potent anti-human immunodeficiency virus activity in vitro in the subnanomolar range. In vitro studies show that aplaviroc
T37861	Talabostat
	Talabostat (PT100, Val-boroPro) is a potent, nonselective and orally available dipeptidyl peptidase IV (DPP-IV) inhibitor with a Ki of 0.18 nM. Talabostat is a nonselective DPP-IV inhibitor, inhibiting DPP8/9, FAP, DPP2 and some other DASH family enzymes essentially as potently as it inhibits DPP-IV[1]. Talabostat stimulates the immune system by triggering a proinflammatory form of cell death in monocytes and macrophages known as pyroptosis. The inhibition of two serine proteases, DPP8 and DPP9,...

化合物

Cat.No: TP1913

BA 1 acetate(183241-31-8 free base)

Cat.No: TP1913L1

Target: Bombesin Receptor

Cat.No: T9072

Synonym: BDTX-189

Target: EGFR, HER, BTK, RIP kinase

Cat.No: T75945

Cat.No: T2490

Synonym: AZD-9291,Mereletinib,奥希替尼

Target: EGFR

Osimertinib mesylate

Cat.No: T3634

Synonym: 甲磺酸奥希替尼,Mereletinib mesylate,奥希替尼甲磺酸盐,AZD-9291 mesylate

Target: EGFR

Cat.No: T35900

Synonym: JAK2-IN-7

Target: JAK

(S,R,S)-AHPC TFA

Cat.No: T17927

Synonym: VH032-NH2 TFA,VHL ligand 1 TFA

Target: Others, Ligand for E3 Ligase

Cat.No: T14307

Synonym: AK 602,GW 873140,GSK 873140

Target: HIV Protease, CCR

SARS-CoV-2-IN-40

Cat.No: T78713

Target: SARS-CoV

SARS-CoV-2-IN-48

Cat.No: T78720

Target: SARS-CoV

Cat.No: T83146

Cat.No: T15480

Synonym: HMSL 10017-101-1

Target: Others

Cat.No: T62531

Cat.No: T35629

Cat.No: T73690

Cat.No: T78968

Target: Trk receptor

Thrombostatin cont-1

Cat.No: T80990

SARS-CoV-2-IN-47

Cat.No: T78719

Target: SARS-CoV

Type II TRK inhibitor 1

Cat.No: T72289

Target: Trk receptor

Cat.No: T7499

Synonym: Takeda 779

Target: HIV Protease, CXCR, CCR

SARS-CoV-2 3CLpro-IN-5

Cat.No: T72364

Target: SARS-CoV

Cat.No: T79420

ω-Conotoxin Bu8

Cat.No: T80457

Target: Calcium Channel

SARS-CoV-2 3CLpro-IN-19

Cat.No: T79376

Target: SARS-CoV

Cat.No: T79706

Target: Trk receptor

Cat.No: T37443

Cat.No: T36379

Aplaviroc hydrochloride

Cat.No: T26642

Synonym: AK602,AK 602,GW873140A,GW-873140,GW873140,AK-602,Aplaviroc HCl

Cat.No: T37861

Cat. No.	Product Name	Target	Signaling Pathways
T23772	Balanol Ophiocordin,BA1,Azepinostatin,(-)-Balanol,(3R-trans)-Balanol
	Balanol is an ATP-competitive Protein Kinase C and Protein Kinase A inhibitor.

天然产物

Cat.No: T23772

Synonym: Ophiocordin,BA1,Azepinostatin,(-)-Balanol,(3R-trans)-Balanol

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