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51

抑制剂 & 化合物

6

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T74884	RNA splicing modulator 1
	RNA splicing modulator 1 (compound 233) 是一种 RNA 剪接调节剂，AC50值 <100 nM。
T74885	RNA splicing modulator 2
	RNA splicing modulator 2 (compound 256) 是 RNA 拼接调节剂。
T74886	RNA splicing modulator 3
	RNA splicing modulator 3 (compound 236) 是一种 RNA 剪接调节剂，AC50值 <100 nM。
T62612	CD33 splicing modulator 1
	CD33 splicing modulator 1 (Compound 1) 是一种 CD33 splicing modulator。CD33/Siglec 3 是一种已知可调节小胶质细胞活性的髓系细胞表面受体。CD33 splicing modulator 1 加强了细胞 mRNA 池中外显子 2 的跳跃。CD33 splicing modulator 1 具有潜力进行包括阿尔茨海默病在内的神经退行性疾病的研究。
T82763	CD33 splicing modulator 1 hydrochloride
	"CD33splicing modulator 1 (Compound 1) hydrochloride 是一种调节CD33/Siglec 3活性的化合物。CD33/Siglec 3 为髓系细胞表面受体，涉及小胶质细胞功能。该化合物通过提升细胞mRNA池中外显子2的剪接变异，展现在神经退行性疾病研究中的应用潜力，包括阿尔茨海默病。"
T4641	Branaplam LMI 070,NVS-SM1	Others; Potassium Channel; DNA/RNA Synthesis	Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Membrane transporter/Ion channel; Others
	Branaplam (LMI 070) 是一种高效、选择性和口服活性的小分子 SMN2 剪接调节剂，对 SMN 的 EC50为 20 nM。它可提高全长 SMN 蛋白并延长其生存期，也抑制 hERG，IC50为 6.3 μM。
T9854	HIV-1 inhibitor-6 3-Pyridinecarboxamide, 1,4-dihydro-1-methyl-N-(5-nitro-1,2-benzisothiazol-3-yl)-4-oxo-	HIV Protease	Microbiology/Virology; Proteases/Proteasome
	HIV-1 inhibitor-6 (3-Pyridinecarboxamide, 1,4-dihydro-1-methyl-N-(5-nitro-1,2-benzisothiazol-3-yl)-4-oxo-) 是一种有效的HIV-1 pre-mRNA 选择性剪接抑制剂，可以阻断HIV 复制。
T12718L	RG7800 RO6885247	Others; DNA/RNA Synthesis	Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Others
	RG7800 (RO6885247) 是一种 SMN2 拼接修饰剂，有用于治疗脊髓性肌萎缩的研究潜力。
T12935	SMN-C3 MV8T2MCK57	DNA/RNA Synthesis	Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	SMN-C3 (MV8T2MCK57) 是口服有效的 SMN2 剪接调节剂。SMN-C3可用于脊椎肌肉萎缩 (SMA) 的研究。
T73475	SMN-C2	DNA/RNA Synthesis	Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	SMN-C2 是一种选择性的 SMN2 基因剪接调节剂，是risdiplam类似物，是调节前 mRNA 剪接的选择性 RNA 结合配体，通过结合 SMN2 pre-mRNA 来发挥作用。SMN-C2 具有研究脊髓性肌萎缩症 (SMA) 的潜力。
T3628	Madrasin DDD00107587	DNA/RNA Synthesis	Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	Madrasin (DDD00107587) 是剪接抑制剂，在体外能够阻止剪接中间体和产物的形成，并干扰剪接体组装途径中的一个或多个早期步骤。它能在体外抑制 pre-mRNA 的剪接，并修饰细胞中内源性 pre-mRNA 的剪接。
T16757	Risdiplam RO7034067,RG7916	DNA/RNA Synthesis	Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	Risdiplam (RO7034067) 是一种中枢和外周分布的 SMN2 前 mRNA 剪接修饰剂，可增加运动神经元存活 (SMN) 蛋白水平。
T9005	VPC-80051 racemate	Others	Others
	VPC-80051 是一种有效的 hnRNP A1 剪接活性抑制剂，靶向 hnRNP A1 RBD 并降低 22Rv1 CRPC 细胞系中的 AR-V7 信使水平。
T14847	B I09	Others; IRE1	Cell Cycle/Checkpoint; Others
	B I09是一种 IRE-1 RNase 抑制剂，IC50为1230 nM，对人 WaC3细胞中 XBP1 mRNA 的剪接和 LPS 刺激的 B 细胞中 xbp -1的表达有抑制作用。B I09可用于 CLL 细胞模拟XBP-1缺陷的研究。
T74186	PROTAC-O4I2	Apoptosis; PROTACs	Apoptosis; PROTAC
	PROTAC-O4I2 是一种靶向剪接因子 3B1 (SF3B1) 的 PROTAC连接体，在 K562 细胞中促使 FLAG-SF3B1 降解，IC50 值为 0.244 μM。PROTAC-O4I2 促使 K562 WT 细胞凋亡 (apoptosis)。
T23897	CLK1/2-IN-3 CLK1/2 inhibitor 3,CLK1/2-inhibitor-3,CLK1/2 IN 3,CLK1/2IN3	CDK	Cell Cycle/Checkpoint
	CLK1/2-IN-3(Cpd-3) 是一种具有高效性和选择性的 CLK1 和 CLK2 抑制剂，抗增殖活性，抑制 CLK1、CLK2、SRPK1、SRPK2、SRPK3 的的活性。CLK1/2-IN-3 可诱导核斑点扩大，可诱导S6K pre-mRNA选择性剪接和随后抑制多种癌细胞类型细胞生长。
T16551	Pladienolide B	Apoptosis	Apoptosis
	Pladienolide B 是一种有效的剪接体抑制剂，是从钝顶链霉菌 Mer-12 中分离出的大环内酯类化合物，其作用靶向剪接体的 SF3B1 亚单位。Pladienolide B 通过抑制前 mRNA 剪接发挥抗肿瘤作用，诱导调亡。Pladienolide B 具有抗肿瘤活性，可用于研究白血病和淋巴肿瘤。
T38889	Thailanstatin A
	Thailanstatin A 是真核 RNA 剪接抑制剂，IC50为650 nM，通过非共价结合到剪接体的 U2 snRNA 亚复合物的 SF3b 亚单位发挥作用。Thailanstatin A 对多种癌细胞系的抑制显示 nM 级别的 IC50。它与 Trastuzumab 上的赖氨酸结合，可产生“无连接子” ADC。
T12718	RG7800 hydrochloride (1449598-06-4 free base) RO6885247 hydrochloride,RG7800 hydrochloride	Others	Others
	RG7800 hydrochloride is an orally active modulator of SMN2 splicing.
T27058	cp028 cp 028,Compound-028,cp-028,Compound028,Compound 028
	cp028 inhibits pre-mRNA splicing in vitro.
T27562	Hydroxyellipticine-1a
	Hydroxyellipticine-1a, a selective r(CGG)exp probe, improves pre-mRNA splicing defects, inhibits formation of nuclear inclusions and RANT in a FXTAS cellular mode.l
T24647	PKR-IN-C51 PKRINC51,PKR IN C51,PKR-inhibitor-C51,PKR inhibitor C51
	PKR-IN-C51 is an inhibitor of protein kinase R. It acts by correcting the aberrant splicing of MBNL1-dependent pre-mRNAs in DM1 cells without affecting the splicing pattern in normal non-DM1 cells.
T64288	RG7800 hydrochloride
	RG7800 hydrochloride 是一种口服具有活力的 SMN2 剪接调节剂，能够作用于 SMN2 剪接 (EC1.5x: 23 nM) 及 SMN 蛋白 (EC1.5x: 87 nM)。
T26893	Branaplam mesylate (1562338-42-4 free base) LMI070,Branaplam mesylate,LMI 070,LMI-070
	Branaplam is a highly potent, selective and orally active SMN2 splicing modulator. Branaplam increases the amount of functional SMN protein produced by the SMN2 gene through modifying its splicing.
T69688	Erythromycin Gluceptate
	Erythromycin Gluceptate is an inhibitor of protein translation and mammalian mRNA splicing. It inhibits growth of gram negative and gram positiove bacteria.
T70696	Erythromycin hydrochloride
	Erythromycin hydrochloride is an inhibitor of protein translation and mammalian mRNA splicing. It inhibits growth of gram negative and gram positiove bacteria.
T39455	Viltolarsen NS-065,NCNP-01
	Viltolarsen (NS-065/NCNP-01) is a phosphorodiamidate morpholino antisense oligonucleotide that specifically targets the splicing of exon 53 in the dystrophin gene. It is utilized in research related to Duchenne muscular dystrophy (DMD).
T38656	Nusinersen
	Nusinersen is an antisense oligonucleotide drug that modifies pre–messenger RNA splicing of the SMN2 gene and thus promotes increased production of full-length SMN protein.
T60412	BPN-15477
	BPN-15477 是一种剪接调节剂化合物 (SMC)，可恢复 ELP1 外显子 20 的正确剪接。它可用作于额颞叶痴呆研究。 BPN-15477 纠正了 ELP1 转录本的剪接，显着提高了体内所有组织（包括大脑）中功能蛋白的水平。
T78046	RG7800 tetrahydrochloride RO6885247 tetrahydrochloride	DNA/RNA Synthesis	Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	RG7800 hydrochloride为一可口服SMN2剪接调节剂，其对SMN2剪接及SMN蛋白的EC1.5x值分别为23 nM及87 nM。
T33764	NVS-SM2
	NVS-SM2 is an effective small molecule splicing enhancer of SMN2 with oral activity. NVS-SM2 showed increased exon 7 inclusion and upregulated SMN protein expression in SMA fibroblasts and SMN cells Δ7 5025 mouse myoblasts.
T81356	PTBP1-RNA-binding inhibitor P6 TFA PTBP1 α3-helix derived peptide P6 TFA
	PTBP1-RNA-binding inhibitor P6 (PTBP1 α3-helix derived peptide P6) TFA 为剪接因子PTBP1的特定钉合肽抑制剂，用于抑制PTBP1调控的RNA选择性剪接事件。该抑制剂通过与PTBP1的RNA识别基序相结合，从而发挥其作用。
T13723	Homocarbonyltopsentin PK4C9	Others	Others
	Homocarbonyltopsentin is a small-molecule TSL2-binding compound, binds to pentaloop conformations of TSL2 and promotes a shift to triloop conformations that display enhanced SMN2 exon 7 (E7) splicing (EC50: 16 μM).
T69308	Spliceostatin A	Apoptosis	Apoptosis
	Spliceostatin A 是抗癌剂和剪接抑制剂，抑制剪接体剪接机制，抑制有丝分裂克隆扩增和脂肪生成。Spliceostatin A 诱导细胞周期停滞在 G1 和 G2/M 期，诱导细胞凋亡。
T23506	Viomycin	Others	Others
	Viomycin is a member of the tuberactinomycin family of antibiotics. Viomycin also inhibits group I intron splicing and prokaryotic protein synthesis. Freezes bacterial ribosomes in either the pre- or post-translational state. Facilitates trans-cleavage of
T79865	Votoplam	DNA/RNA Synthesis	Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	Votoplam作为一种基因剪接调节剂，其应用主要在于抑制亨廷顿病。
T81826	Meayamycin D
	Meayamycin D, 作为FR901464的类似物，能够诱导MCL-1的选择性剪接，并在小鼠血浆中展现出较长的半衰期。
TP2032	des-Gln14-Ghrelin des-Gln14-Ghrelin (rat)
	An endogenous ligand for the ghrelin receptor (GHS-R1a), produced by alternative splicing of the rat ghrelin gene. Potently induces Ca2+ release in cells expressing ghrelin receptors (EC50 = 2.4 nM) and stimulates GH release in vivo.
T38841	IRE1α kinase-IN-2 IRE1α kinase-IN-2
	IRE1α kinase-IN-2 is a highly potent inhibitor of IRE1α kinase, demonstrating an EC50 of 0.82 μM. It effectively impedes IRE1α kinase autophosphorylation with an IC50 of 3.12 μM. Additionally, IRE1α kinase-IN-2 effectively inhibits the splicing of XBP1 mRNA in wild-type cell lines.
T74475	m7GpppGpG
	m7GpppGpG 是 M7GpppNpG 三核苷酸帽类似物的一种寡核苷酸。它能够防止 5'-外切核酸酶过早的降解作用，并能够募集前 mRNA 剪接、mRNA 转运以及蛋白质生物合成启动所需的蛋白质。
T79717	mHTT-IN-2	Huntingtin	Neuroscience
	mHTT-IN-2（化合物27）作为mHTT的一种有效抑制剂，具有EC50值为0.066 μM，能够降低HTT RNA外显子[49-50]的规范剪接，从而调节HTT基因的剪接。在人类HD干细胞和BACHD小鼠模型上，mHTT-IN-2已显示出明显的体外及体内活性。此外，该化合物也被应用于研究与branaplam相关的周围神经病变。
T64183	PAIR2
	PAIR2 是一种有效和选择性的 IRE1α RNase 的部分拮抗剂。PAIR2 可以完全占据细胞中 IRE1α 的 ATP 结合位点，并阻断强效 KIRA 抑制 XBP1 剪接的能力。
T81912	LSP-GR3	iGluR	Membrane transporter/Ion channel; Neuroscience
	LSP-GR3为一种新型化学修饰RNA寡核苷酸，亦即剪接调控寡聚体(SMOs)，可特异性调控中枢神经系统内GluR的选择性剪接及GluR3-flip表达。
T81355	PTC258
	PTC258为针对伸长复合体蛋白1基因（ELP1）的特异性口服基因剪接调节剂，能促进ELP1在体外和体内的表达增加，并在小鼠模型中显示出良好的耐受性。
T79640	ZNL-05-044	CDK	Cell Cycle/Checkpoint
	ZNL-05-044为CDK11抑制剂，在NanoBRET实验中展现对CDK11A与CDK11B的高度选择性，其IC50分别为0.23 μM及0.27 μM。该化合物诱导G2/M细胞周期阻滞，并对RNA剪接产生破坏作用。
T61991	HTT-D3
	HTT-D3 是有效的，具有口服活性的亨廷顿蛋白 (HTT) 剪接调节剂。 HTT-D3 促进 HTT mRNA 降解和 HTT 水平降低。HTT-D3 减少 p-糖蛋白 (P-gp) 流出，在亨廷顿病中具有研究价值。
T62381	Branaplam hydrochloride
	Branaplam (LMI070; NVS-SM1) hydrochloride 是一种选择性的、口服具有活力的 SMN2 拼接调节剂，能够作用于 SMN (EC50: 20 nM)。Branaplam hydrochloride 能够抑制 hERG (IC50: 6.3 μM)。在严重的脊髓性肌萎缩症 (SMA) 小鼠模型中，Branaplam hydrochloride 能够增加全长 SMN 蛋白并提高其生存期。
T35594	Cuspin-1
	The Survival of Motor Neurons (SMN) protein participates in RNA splicing. Decreases in SMN, typically a consequence of defects in the smn1 gene, result in the death of motor neurons and lead to the neurodegenerative disease, spinal muscular atrophy (SMA). Cuspin-1 is a small molecule upregulator of SMN that has been shown in vitro to increase levels of SMN in SMA patient fibroblasts by 50% at 18 μM. Its mechanism of action is thought to involve increased phosphorylation of ERK to initiate Ras-Ra...
T79035	PRMT5-IN-28	Histone Methyltransferase	Chromatin/Epigenetic
	PRMT5-IN-28（化合物36）是一种PRMT5抑制剂，能够调控包含基因转录、mRNA剪接、DNA修复、蛋白质定位、细胞命运和信号传导等过程的蛋白质精氨酸甲基化。PRMT5的异常活性与癌症细胞的增殖、抗凋亡、侵袭转移能力增强及免疫逃逸机制的影响相关。
T36684	Ipivivint
	Ipivivint, a first-in-class, orally active and potent CDC-like kinase (CLK) inhibitor, inhibits CLK1 (IC50=1.4 μM), CLK2 (IC50=0.002 μM) and CLK3 (IC50=0.022 μM). Ipivivint reduces Wnt pathway signaling gene expression through inhibiting CLK activity and serine and arginine rich splicing factor (SRSF) phosphorylation and disrupting spliceosome activity. Ipivivint can be used for the research of cancer[1]. Ipivivint (SW480 cells; 0.01~10 μM; 1 hour) potently inhibits SRSF5/6 phosphorylation[1].Ip...

化合物

RNA splicing modulator 1

Cat.No: T74884

RNA splicing modulator 2

Cat.No: T74885

RNA splicing modulator 3

Cat.No: T74886

CD33 splicing modulator 1

Cat.No: T62612

CD33 splicing modulator 1 hydrochloride

Cat.No: T82763

Cat.No: T4641

Synonym: LMI 070,NVS-SM1

Target: Others, Potassium Channel, DNA/RNA Synthesis

HIV-1 inhibitor-6

Cat.No: T9854

Synonym: 3-Pyridinecarboxamide, 1,4-dihydro-1-methyl-N-(5-nitro-1,2-benzisothiazol-3-yl)-4-oxo-

Target: HIV Protease

Cat.No: T12718L

Synonym: RO6885247

Target: Others, DNA/RNA Synthesis

Cat.No: T12935

Synonym: MV8T2MCK57

Target: DNA/RNA Synthesis

Cat.No: T73475

Target: DNA/RNA Synthesis

Cat.No: T3628

Synonym: DDD00107587

Target: DNA/RNA Synthesis

Cat.No: T16757

Synonym: RO7034067,RG7916

Target: DNA/RNA Synthesis

VPC-80051 racemate

Cat.No: T9005

Target: Others

Cat.No: T14847

Target: Others, IRE1

Cat.No: T74186

Target: Apoptosis, PROTACs

Cat.No: T23897

Synonym: CLK1/2 inhibitor 3,CLK1/2-inhibitor-3,CLK1/2 IN 3,CLK1/2IN3

Target: CDK

Cat.No: T16551

Target: Apoptosis

Thailanstatin A

Cat.No: T38889

RG7800 hydrochloride (1449598-06-4 free base)

Cat.No: T12718

Synonym: RO6885247 hydrochloride,RG7800 hydrochloride

Target: Others

Cat.No: T27058

Synonym: cp 028,Compound-028,cp-028,Compound028,Compound 028

Hydroxyellipticine-1a

Cat.No: T27562

Cat.No: T24647

Synonym: PKRINC51,PKR IN C51,PKR-inhibitor-C51,PKR inhibitor C51

RG7800 hydrochloride

Cat.No: T64288

Branaplam mesylate (1562338-42-4 free base)

Cat.No: T26893

Synonym: LMI070,Branaplam mesylate,LMI 070,LMI-070

Erythromycin Gluceptate

Cat.No: T69688

Erythromycin hydrochloride

Cat.No: T70696

Cat.No: T39455

Synonym: NS-065,NCNP-01

Cat.No: T38656

Cat.No: T60412

RG7800 tetrahydrochloride

Cat.No: T78046

Synonym: RO6885247 tetrahydrochloride

Target: DNA/RNA Synthesis

Cat.No: T33764

PTBP1-RNA-binding inhibitor P6 TFA

Cat.No: T81356

Synonym: PTBP1 α3-helix derived peptide P6 TFA

Homocarbonyltopsentin

Cat.No: T13723

Synonym: PK4C9

Target: Others

Spliceostatin A

Cat.No: T69308

Target: Apoptosis

Cat.No: T23506

Target: Others

Cat.No: T79865

Target: DNA/RNA Synthesis

Cat.No: T81826

des-Gln14-Ghrelin

Cat.No: TP2032

Synonym: des-Gln14-Ghrelin (rat)

IRE1α kinase-IN-2

Cat.No: T38841

Synonym: IRE1α kinase-IN-2

Cat.No: T74475

Cat.No: T79717

Target: Huntingtin

Cat.No: T64183

Cat.No: T81912

Target: iGluR

Cat.No: T81355

Cat.No: T79640

Target: CDK

Cat.No: T61991

Branaplam hydrochloride

Cat.No: T62381

Cat.No: T35594

Cat.No: T79035

Target: Histone Methyltransferase

Cat.No: T36684

Cat. No.	Product Name	Target	Signaling Pathways
T4S21320	ISOGINKGETIN 异银杏素,4',4'''-Dimethylamentoflavone,异银杏双黄酮	MMP; Others	Others; Proteases/Proteasome
	ISOGINKGETIN (4',4'''-Dimethylamentoflavone) 是一种MMP9抑制剂，也是一种Pre-mRNA Splicing 抑制剂。
T4S0181	Hinokiflavone 日本扁柏黄酮,扁柏双黄酮	MMP; BCL; E1/E2/E3 Enzyme	Apoptosis; Proteases/Proteasome; Ubiquitination
	Hinokiflavone 是pre-mRNA 剪接活性的新型调节剂，通过抑制剪接体装配来阻止pre-mRNA 底物的剪接，特别是阻止 B complex 的形成。它是SUMO protease 蛋白酶抑制剂，能够抑制前哨蛋白特异性蛋白酶 1 的活性。
TN3070	4beta-Hydroxywithanolide E	PARP; HSP; NF-κB; COX	Chromatin/Epigenetic; Cytoskeletal Signaling; DNA Damage/DNA Repair; Immunology/Inflammation; Metabolism; Neuroscience; NF-κB
	4beta-Hydroxywithanolide E(4bHWE) can inhibit the growth of colon cancer monolayer and spheroid cultures, it assert its anti-tumor activity in carcinogenic progression and develop into a dietary chemopreventive agent, it affects alternative splicing by mo
T38890	Thailanstatin C
	Thailanstatin C, an antiproliferative agent derived from Burkholderia thailandensis MSMB43, functions as a potent inhibitor of pre-mRNA splicing (IC50 = 6.84 μM).
T39071	Thailanstatin D
	Thailanstatin D, an analogue of Thailanstatin A, inhibits AR-V7 gene splicing by disrupting the interaction between U2AF65 and SAP155, hindering their binding to the polypyrimidine tract situated between the branch point and the 3' splice site. This compound displays potent tumor inhibitory properties in human castration-resistant prostate cancer (CRPC) xenografts, resulting in cellular apoptosis.
T36749	Herboxidiene
	Herboxidiene is a polyketide originally isolated from S. chromofuscus that has diverse biological activities.[1],[2,][3],[4],[5] It inhibits growth of HeLa S3, SK-MEL-2, PC3, A549, and EBC-1 cells with GI50 values ranging from 7.4 to 62 nM.3 Herboxidiene is cytostatic against human umbilical vein endothelial cells (HUVECs; (IC50 = 26 nM)) and inhibits VEGF-induced invasion and tube formation of serum-starved HUVECs in a concentration-dependent manner, indicating antiangiogenic activity.[4] Herbo...

天然产物

Cat.No: T4S21320

Synonym: 异银杏素,4',4'''-Dimethylamentoflavone,异银杏双黄酮

Target: MMP, Others

Cat.No: T4S0181

Synonym: 日本扁柏黄酮,扁柏双黄酮

Target: MMP, BCL, E1/E2/E3 Enzyme

4beta-Hydroxywithanolide E

Cat.No: TN3070

Target: PARP, HSP, NF-κB, COX

Thailanstatin C

Cat.No: T38890

Thailanstatin D

Cat.No: T39071

Cat.No: T36749

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