CID-1067700
(Synonyms: 2-[[(苯甲酰基氨基)硫代甲酰]氨基]-4,7-二氢-5,5-二甲基-5H-噻吩并[2,3-C]吡喃-3-羧酸,ML-282) 目录号 : GC12948
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CID-1067700是Rab GTPases的抑制剂，特别是对Rab2和Rab7具有显著的抑制作用。
Cas No.:314042-01-8
Sample solution is provided at 25 µL, 10mM.
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CID-1067700 has significant inhibitory activity against the Rab GTPases, in particular Rab2 and Rab7. Its EC50 value for Rab GTPases is in the range of 20–500nM. CID-1067700 inhibits the binding of BODIPY-conjugated nucleotides in a dose-dependent manner, with corresponding EC50 values of 11.22±1.34nM for BODIPY-GTP and 20.96±1.34nM for BODIPY-GDP[1].
In vitro, treatment with 40μM CID-1067700 for 48h inhibited induction of CSR to IgG, IgA and IgE, hampered NF-κB activation and AID expression in human and mouse B cells[2]. Treatment with 20-100μM of CID-1067700 for 24 or 72h did not show any significant toxic effects on the viability of Adipose-derived stem cells (ASCs)[3]. A 10-day treatment with 40μM CID-1067700 induced the differentiation of ASCs into basal KLCs and promoted their differentiation into differentiated KLCs[3].
In vivo, CID-1067700 (16mg/kg/d; i.p.), administered from day 7 to day 12, did not have a therapeutic effect on tumor progression in Foxn1nu/nu mice bearing Daudi cell-derived xenografts[4]. CID-1067700 (16mg/kg/w; i.p.), administered for 10 weeks, prevented disease development in lupus disease and reduced IgG-IC deposition in MRL/Faslpr/lpr mice[2].
Reference:
[1]Agola JO, Hong L, Surviladze Z, et al. A competitive nucleotide binding inhibitor: in vitro characterization of Rab7 GTPase inhibition. ACS Chem Biol. 2012 Jun 15;7(6):1095-108.
[2] Lam T, Kulp DV, Wang R, et al. Small Molecule Inhibition of Rab7 Impairs B Cell Class Switching and Plasma Cell Survival To Dampen the Autoantibody Response in Murine Lupus. J Immunol. 2016;197(10):3792-3805.
[3] Alghazali R, Tabebi M, Elmasry M, El-Serafi A. Rab7 inhibitor enhances stem cell differentiation into keratinocyte-like cells with anti-inflammatory properties. Front Immunol. 2025;16:1503007.
[4] Fernandez M, Wang R, Wang J, et al. Targeting RAB7 in human B lymphoma by a small molecule inhibitor arrests tumor cell growth. Front Oncol. 2025;15:1616519.
CID-1067700是Rab GTPases的抑制剂，特别是对Rab2和Rab7具有显著的抑制作用。CID-1067700对Rab GTPases的EC50值在20-500nM范围内。CID-1067700以剂量依赖的方式抑制BODIPY联合核苷酸的结合，对BODIPY-GTP的EC50值为11.22±1.34nM，对BODIPY-GDP的EC50值为20.96±1.34nM[1]。
体外实验中，40μM的CID-1067700处理48小时抑制了人和小鼠B细胞中CSR对IgG、IgA和IgE的诱导，NF-κB的激活以及AID的表达[2]。20-100μM的CID-1067700处理24或72小时，对脂肪源性干细胞（ASCs）的活性均没有明显的毒性影响[3]。40μM的CID-1067700处理10天，能诱导ASCs向基底型KLCs分化，并促进其向分化型KLCs分化[3]。
体内实验中，CID-1067700（16mg/kg/d; i.p.），从第7天持续至第12天给药，对接种了Daudi的Foxn1nu/nu鼠的肿瘤进展并未产生治疗效果[4]。CID-1067700（16mg/kg/w; i.p.），连续给药10周，能够阻止狼疮病的发展，并减少MRL/Faslpr/lpr小鼠体内IgG-IC的沉积[2]。
| Cell experiment [1]: | |
Cell lines | Human and mouse B cells |
Preparation Method | CID-1067700 was diluted in DMSO and added to cell cultures to the final concentration of 40μM. CID-1067700 or DMSO (nil) was added either at the time when B cell stimulation started, or 66h after B cells were stimulated with LPS plus IL-4, TGF-β, anti–δ/dex and RA, for analysis of plasma cell survival. |
Reaction Conditions | 40μM; 48h |
Applications | CID-1067700 inhibited induction of CSR to IgG, IgA and IgE, hampered NF-κB activation and AID expression in human and mouse B cells. |
| Animal experiment [1]: | |
Animal models | MRL/Faslpr/lpr mice |
Preparation Method | CID-1067700 dissolved in DMSO (stock concentration 40mM) was diluted with the solvent to the final volume of 50μl and injected intraperitoneally (i. p.) once per week at the dose of 16mg/kg body weight, i. p. with the vehicle DMSO as contrl. Ten weeks later, survival studies and skin lesion analyses were performed. |
Dosage form | 16mg/kg/w; i.p. |
Applications | When treated with CID-1067700 for only 10 weeks, 14 of 16 MRL/Faslpr/lpr mice survived past the treatment period and half of mice were alive at 52 weeks, compared to only one in the untreated cohort. Treated mice had normal body weight, rare skin lesions and reduced lymphadenopathy and splenomegaly at 17 weeks. They had some interstitial infiltration by monocytes, but were largely free of glomerulonephritis, showing little proteinuria and decreased “crescent” formation and mesangial matrix expansion in glomeruli. IgG-IC deposition was reduced in MRL/Faslpr/lpr mice treated with CID-1067700. |
References: | |
| Cas No. | 314042-01-8 | SDF | |
| 别名 | 2-[[(苯甲酰基氨基)硫代甲酰]氨基]-4,7-二氢-5,5-二甲基-5H-噻吩并[2,3-C]吡喃-3-羧酸,ML-282 | ||
| 化学名 | 2-[[(benzoylamino)thioxomethyl]amino]-4,7-dihydro-5,5-dimethyl-5H-thieno[2,3-c]pyran-3-carboxylic acid | ||
| Canonical SMILES | O=C(NC(NC1=C(C(O)=O)C(CC(C)(C)OC2)=C2S1)=S)C3=CC=CC=C3 | ||
| 分子式 | C18H18N2O4S2 | 分子量 | 390.5 |
| 溶解度 | ≤10mg/ml in DMSO | 储存条件 | Store at 2-8°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5608 mL | 12.8041 mL | 25.6082 mL |
| 5 mM | 512.2 μL | 2.5608 mL | 5.1216 mL |
| 10 mM | 256.1 μL | 1.2804 mL | 2.5608 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
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